Injectable formulations for non-naturally occurring melanocortin antagonist analogs for modulating weight gain

Abstract

Provided herein are stable aqueous pharmaceutical compositions and formulation comprising non-naturally occurring melanocortin antagonist analogs. The non-naturally occurring melanocortin antagonist analogs may be antagonists of the melanocortin 3 receptor and / or melanocortin 4 receptor.

Description

Docket No. 183B-412975-WOINJECTABLE FORMULATIONS FOR NON-NATURALLY OCCURRING MELANOCORTIN ANTAGONIST ANALOGS FOR MODULATING WEIGHT GAINCROSS-REFERENCE TO RELATED APPLICATIONS

[0001] This application claims the benefit of U.S. Provisional Patent Application No. 63 / 704,508, filed October 7, 2024, the contents of which are incorporated herein by reference in their entirety.INCORPORATION BY REFERENCE OF SEQUENCE LISTING

[0002] This application contains an ST.26 compliant Sequence Listing, which is submitted concurrently in xml format and is hereby incorporated by reference in its entirety. The .xml copy, created on October 03, 2025 is titled “183B-412975-WO_SL.xml” and is 2,043,1 12 bytes in size.TECHNICAL FIELD

[0003] The present technology generally relates to pharmaceutical compositions comprising non-naturally occurring melanocortin analogs formulated for delivery to a subject in need thereof by injection.BACKGROUND

[0004] A major challenge in the development of peptide-based therapeutics formulations is maintaining solubility, stability, and potency of the peptide. It is particularly desirable to avoid aggregates and particulates in liquid formulations that require sterile filtration before administration (e.g., parenteral injection). Further, the formation of aggregates in injectable formulations may cause adverse reactions at the injection site.

[0005] Melanocortin analogs have been synthesized for the potential regulation and treatment of many conditions, including weight regulation (e.g., obesity, anorexia, and cachexia), hormonal secretion, and hyposecretion of many exocrine glands. Despite recent advances, there is still a need for melanocortin analog-containing compositions that areDocket No. 183B-412975-WO stable, effective, and suitable for parenteral administration, including subcutaneous injection.SUMMARY

[0006] Provided herein are pharmaceutical compositions and formulations of non- naturally occurring melanocortin antagonist analogs.

[0007] In some aspects, provided herein is a pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0008] In some aspects, provided herein is a pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue and no anionic amino acid residues, an osmolyte, a pH adjusting agent, and a buffer, wherein at least one of the one or more cationic amino acid residues is protonated and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp- Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0009] In some aspects, provided herein is a pharmaceutical composition comprising a cyclic non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp- Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0010] In some aspects, provided herein is a pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue and an isoelectric point of about 10 to about 12.5, an osmolyte, a pH adjusting agent, and aDocket No. 183B-412975-WO buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0011] In some aspects, provided herein is a pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of at least about 10, an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp- Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0012] In some aspects, provided herein is a pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having a cyclic region with an arginine residue positioned therein and an isoelectric point of at least about 10 and a pharmaceutically acceptable carrier comprising a base and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro- dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0013] In some aspects, provided herein is a pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an isoelectric point of at least about 10 and a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog comprises moiety (A):X1-R1-R2-R3-R4-R5-R6-R7-Y1 (A), wherein:R1 is absent or is an amino acid or amino acid derivative;R4 is selected from the group consisting of optionally substituted dNal(2’), Phe, Bip, and dBip; at least one of R2-R7 is a cationic amino acid residue;Docket No. 183B-412975-WOXi is an optionally present N-terminus;Yi is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a side chain linkage between R2 and R7; provided that: moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0014] In some aspects, provided herein is a pharmaceutical formulation comprising a peptide composition and a pharmaceutically acceptable carrier composition, the peptide composition comprising a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 in an aqueous solution, the pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0015] In some aspects, provided herein is a pharmaceutical composition comprising an osmolyte, a pH adjusting agent, a histidine buffer, and a non-naturally occurring melanocortin antagonist analog having an isoelectric point of at least about 10 and comprising a cyclic region with an arginine residue positioned therein, wherein the non- naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac- Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0016] In some aspects, provided herein is a pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an isoelectric point of about 10 to about 12.5 and a pharmaceutically acceptable carrier comprising an osmolyte, a pH adjusting agent, and a histidine buffer, wherein the non-naturally occurring melanocortin antagonist analog comprises moiety (A):X1-R1-R2-R3-R4-R5-R6-R7-Y1 (A), wherein:R1 is absent or is an amino acid or amino acid derivative;Docket No. 183B-412975-WOF is selected from the group consisting of optionally substituted dNal(2’), Phe, Bip, and dBip; at least one of R2-R7 is a cationic amino acid residue;Xi is an optionally present N-terminus;Y1 is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a side chain linkage between R2 and R7; provided that: moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0017] In some aspects, provided herein is a pharmaceutical formulation having a pH of about 4.0 to about 6.5 and comprising a non-naturally occurring melanocortin antagonist analog, the formulation produced by combining an aqueous peptide composition comprising the antagonist analog, and a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 1 1 .0 comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical formulation such that no local region of the antagonist analog has a pH equal to the isoelectric point of the analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5 and does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]- dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0018] In some aspects, provided herein is a pharmaceutical formulation having a pH of about 4.0 to about 6.5 and comprising a non-naturally occurring melanocortin antagonist analog, the formulation produced by combining an aqueous peptide composition comprising the non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of at least about 10, and a pharmaceutically acceptable carrier composition comprising a base and a buffer and having a pH of about 5.5 to about 1 1.0, wherein the non-naturally occurring melanocortin antagonist analog does not comprise aDocket No. 183B-412975-WO sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0019] Further provided herein are methods of preparing pharmaceutical compositions and formulations described herein.

[0020] In some aspects, provided herein is a method of producing a pharmaceutical composition of a non-naturally occurring melanocortin antagonist analog, the method comprising combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 with a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 1 1 .0 and comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non- naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac- Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.

[0021] In other aspects, provided herein is a method of producing a pharmaceutical formulation having a pH of about 4.0 to about 6.5, the method comprising combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical composition such that no local region has a pH that is equal to the isoelectric point of the antagonist analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5, and does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)- Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond, and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 1 1 .0.

[0022] In still other aspects, provided herein is a method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog having a pH of about 4.0 to about 6.5, the method comprising combining an aqueous peptide composition of theDocket No. 183B-412975-WO non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog has an arginine residue and an isoelectric point of at least about 10 and does not comprise a sequence of Ac-Nle-c[Asp- Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 11 .0.

[0023] In yet other aspects, provided herein is a method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog, the method comprising: providing a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a histidine buffer; dissolving a non-naturally melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 in water to provide an aqueous peptide composition; and adding the pharmaceutically acceptable carrier composition to the aqueous peptide composition while mixing to maintain dissolution of the non-naturally occurring melanocortin antagonist analog, wherein the pharmaceutical formulation has a pH of about 4.0 to about 6.5 and the non- naturally occurring melanocortin analog does not comprise a sequence of Ac-Nle-c[Asp-Pro- dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represent cyclization via a lactam bond.DETAILED DESCRIPTION

[0024] The present technology provides stable aqueous pharmaceutical compositions of non-naturally occurring melanocortin antagonist analogs, also referred to herein as “non- naturally occurring melanocortin analogs,” “melanocortin analogs,” and “antagonist analogs.” Pharmaceutical compositions described herein have a pH of less than 7.0 and include a non-naturally occurring melanocortin analog and one or more pharmaceutically acceptable carriers and / or excipients. In some embodiments, the pharmaceutical compositions have a pH of about 4.0 to about 6.5.

[0025] Pharmaceutical compositions comprising non-naturally occurring melanocortin antagonist analogs of the present technology may be administered to a subject in needDocket No. 183B-412975-WO thereof to treat and / or prevent conditions associated with weight regulation, such as, for example, cachexia. To achieve desired therapeutic outcomes, the pharmaceutical compositions may be formulated for specific routes of administration, such as parenteral delivery, including, but not limited to, subcutaneous delivery. Accordingly, the one or more pharmaceutically acceptable carriers and / or excipients included in the pharmaceutical compositions described herein may be useful for subcutaneous delivery of the non-naturally occurring melanocortin peptides. In some embodiments, the one or more carriers and / or excipients are selected based on desirable properties, such as reduced or lack of delivery site reactions, solubility, stability (e.g., shelf-life), pH, buffering, pharmacokinetics, bioavailability, or the like, of the pharmaceutical composition. In some embodiments, the one or more pharmaceutically acceptable carriers and / or excipients may include a buffer, an osmolyte, and a pH adjusting agent.

[0026] Methods of preparing the stable aqueous pharmaceutical compositions are also described herein. In some embodiments, the pharmaceutical compositions are prepared by combining an aqueous peptide composition with a pharmaceutically acceptable carrier composition.

[0027] The following description is merely exemplary in nature and is not intended to limit the present technology, its applications, or its uses. It should be understood that throughout the drawings, corresponding reference numerals indicate like or corresponding parts and features. The description of specific examples indicated in various embodiments of the present technology are intended for purposes of illustration only and are not intended to limit the scope of the present technology disclosed herein. Moreover, recitation of multiple embodiments having stated features is not intended to exclude other embodiments having additional features or other embodiments incorporating different combinations of the stated features.

[0028] Furthermore, the detailed description of various embodiments herein makes reference to the accompanying drawing / FIGS, which show various embodiments by way of illustration. While the embodiments are described in sufficient detail to enable those skilled in the art to practice the present technology, it should be understood that other embodiments may be realized, and that logical changes may be made without departing from the spiritDocket No. 183B-412975-WO and scope of the present technology. Thus, the detailed description herein is presented for purposes of illustration only and not of limitation. For example, steps recited in any method or process, may be executed in any order and are not limited to the order presented. Moreover, any of the steps thereof may be outsourced to or performed by one or more third parties.Definitions

[0029] Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by those of ordinary skill in the art to which the present technology belongs. For the purposes of the present technology, the following terms are defined below.

[0030] The articles “a” and “an” are used herein to refer to one or to more than one (i.e., to at least one) of the grammatical object of the article. By way of example, “an element” means one element or more than one element.

[0031] The term “about” means a quantity, level, value, number, frequency, percentage, dimension, size, amount, weight, or length that varies by acceptable levels in the art. Typically, such variation may be as much 10% above and below a reference quantity, level, value, number, frequency, percentage, dimension, size, amount, weight or length and such variation may be influenced by standard applicable measurement practices. When the term “about” is used in conjunction with a numerical range, it modifies that range by extending the boundaries above and below the numerical values set forth.

[0032] As used herein, a “composition” or a “pharmaceutical composition” refers to a mixture of the active ingredient with other chemical components, such as pharmaceutically acceptable carriers and / or excipients.

[0033] As used herein, a “pharmaceutically acceptable carrier” refers to a carrier or diluent that does not cause significant irritation to an organism, does not abrogate the biological activity and properties of the administered active ingredient, and / or does not interact in a deleterious manner with the other components of the composition in which it is contained.Docket No. 183B-412975-WO

[0034] “Melanocortin analogs,” “melanocortin peptides,” or “melanocortins,” are used interchangeably and refer to melanocortin-receptor ligands, which are macromolecules containing at least one melanocortin pharmacophore. Melanocortin analogs are typically peptides that bind melanocortin receptors under physiological conditions. Melanocortin analogs include non-naturally occurring melanocortin peptides and truncated and / or modified versions of melanocortin full-length protein or peptides. For example, the full-length pro-opiomelanocortin protein (POMC), prior to proteolytic cleavage of “sub-peptides,” consists of 241 amino acids. Tissue-specific proteolytic cleavage of POMC yields peptides ranging in size from 13 amino acids to 76 amino acids. See Bicknell and Lawry, Encyclopedia of Stress, vol. 3, 257-265, Academic Press (2000). Synthesized, non- naturally occurring melanocortin analogs having increased melanocortin receptor activity as discussed herein are approximately 7-12 amino acids in size. Melanocortin analogs exhibit binding functionality with melanocortin receptors. In addition to peptides, the melanocortin analogs include small molecule analogs of melanocortin or portions thereof comprised of organic compounds, inorganic compounds, or combinations of peptide and small molecule — i.e., peptide mimetics, or various combinations thereof. “Melanocortin peptides” can be structurally similar and / or functionally similar to biological melanocortin proteins in their ability to bind melanocortin receptors. Further, the melanocortin analogs generally contain the pharmacophore: His-Phe-Arg-Trp (SEQ ID NO: 1 ) or a modified version thereof, or a structural or functional peptide mimetic thereof.

[0035] A “pharmacophore” is the minimum set of amino acid residues necessary to achieve a physiological effect; or a small molecule that is (with respect to a receptor) a structural mimic of the amino acid residues required for binding to and activation of a receptor. His-Phe-Arg-Trp (SEQ ID NO: 1 ) and their analogs are the pharmacophore of melanocortin for the regulated physiological effect. Therefore, non-naturally occurring melanocortin pharmacophore analogs can be small peptides or organic molecules designed to mimic the appearance or function (including activation or deactivation of receptor activity) of the melanocortin pharmacophore core sequence peptide.

[0036] A melanocortin receptor “antagonist” or “melanocortin antagonist” is a naturally occurring substance or manufactured drug substance or composition that opposes theDocket No. 183B-412975-WO melanocortin receptor-associated responses normally induced by a melanocortin receptor agonist agent.

[0037] The terms “bind,” “binding,” “complex,” and “complexing,” refer to all types of physical and chemical binding, reactions, complexing, attraction, chelating and the like.

[0038] The “peptides” described herein can be (a) naturally occurring, (b) produced by chemical synthesis, (c) produced by recombinant DNA technology, (d) produced by biochemical or enzymatic fragmentation of larger molecules, (e) produced by methods resulting from a combination of methods (a) through (d) listed above, or (f) produced by any other means for producing peptides.

[0039] The term “peptide” as used herein includes any structure comprised of two or more amino acids, including chemical modifications and derivatives of amino acids. The amino acids forming all or a part of a peptide may be naturally occurring amino acids, stereoisomers and modifications of such amino acids, non-protein amino acids, post- translationally modified amino acids, enzymatically modified amino acids, constructs or structures designed to mimic amino acids, and the like, so that the term “peptide” includes pseudopeptides and peptidomimetics, including structures which have a non-peptidic backbone. The term “peptide” also includes dimers or multimers of peptides. A “manufactured” peptide includes a peptide produced by chemical synthesis, recombinant DNA technology, biochemical, or enzymatic fragmentation of larger molecules, combinations of the foregoing or, in general, made by any other method. The term “peptide” includes peptides containing a variable number of amino acid residues, optionally with nonamino acid residue groups at the N- and C-termini, such groups including acyl, acetyl, alkenyl, alkyl, N-alkyl, amine, or amide groups, among others.

[0040] By employing chemical synthesis, a useful means of production, it is possible to introduce various amino acids which do not naturally occur along the chain, modify the N- or C-terminus, and the like, thereby providing for improved stability and formulation, resistance to protease degradation, and the like.

[0041] “Amino acids” are molecules containing an amine group, a carboxylic acid group, and a side-chain that is specific to each amino acid. The key elements of an aminoDocket No. 183B-412975-WO acid are carbon, hydrogen, oxygen, and nitrogen and have the generic formula H2N — CHR — COOH, wherein R represents a side chain group. The various a-amino acids differ in the side-chain moiety that is attached to the a-carbon. The “amino acids” of the present technology include the known naturally occurring protein amino acids, which are referred to by both their common three letter abbreviation and single letter abbreviation. See generally Synthetic Peptides: A User’s Guide, G. A. Grant, editor, W.H. Freeman & Co., New York (1992), the teachings of which are incorporated herein by reference, including the text and table set forth at pages 11 through 24. As set forth above, the term “amino acid” also includes stereoisomers and modifications of naturally occurring protein amino acids, nonprotein amino acids, post-translationally modified amino acids, enzymatically synthesized amino acids, derivatized amino acids, constructs or structures designed to mimic amino acids, and the like. Modified and unusual amino acids are described generally in Synthetic Peptides: A User’s Guide, supra; Hruby et al., Biochem. J. 268:249-262 (1990); and Toniolo, Int. J. Peptide Protein Res. 35:287-300 (1990); the teachings of all of which are incorporated herein by reference.

[0042] The phrase “amino acid side chain moiety” used herein, including as used in the specification and claims, includes any side chain of any amino acid, as the term “amino acid” is defined herein. This thus includes the side chain moiety present in naturally occurring amino acids. It further includes side chain moieties in modified naturally occurring amino acids, such as glycosylated amino acids. It further includes side chain moieties in stereoisomers and modifications of naturally occurring protein amino acids, non-protein amino acids, post-translationally modified amino acids, enzymatically synthesized amino acids, derivatized amino acids, constructs, or structures designed to mimic amino acids, and the like. For example, the side chain moiety of any amino acid disclosed herein is included within the definition. A “derivative” of an amino acid side chain moiety is included within the definition of an amino acid side chain moiety.

[0043] The “derivative” of an amino acid side chain moiety includes any modification to or variation in any amino acid side chain moieties, including a modification of naturally occurring amino acid side chain moieties. By way of example, derivatives of amino acid sideDocket No. 183B-412975-WO chain moieties include straight chain or branched, cyclic or noncyclic, substituted or unsubstituted, saturated or unsaturated, alkyl, aryl or aralkyl moieties.

[0044] In the peptides described herein, conventional amino acid residues have their conventional meaning as given in Chapter 2400, of the Manual of Patent Examining Procedure, 8th Ed. Thus, “Ala” is alanine; “Arg” is arginine; “Asn” is asparagine; “Asp” is aspartic acid; “Cys” is cysteine; “Gin” is glutamine; “Glu” is glutamic acid; “His” is histidine; “lie” is isoleucine; “Leu” is leucine; “Lys” is lysine; “Met” is methionine; “Phe” is phenylalanine; “Pro” is proline; “Ser” is serine; Thr is threonine; “Trp” is tryptophan; “Tyr” is tryosine; and “Vai” is valine. Unless otherwise indicated, all amino acids abbreviations represent either isomer, i.e., the L-isomer, the D-isomer, or combinations thereof can be used. Thus, for example, “L-Phe” or “IPhe” is L-phenylalanine; “D-Phe” or “dPhe” is D- phenylalanine; dVal is D-valine; dPro is D-proline; “D- / L-Phe” or “d / IPhe” is D-phenylalanine, L-phenylalanine, or combinations thereof; “Phe” is also D-phenylalanine, L-phenylalanine, or combinations thereof, and so on.

[0045] An alpha (cc)-amino acid has the generic formula H2N — CaHR — COOH, where R is a side chain moiety and the amino group is attached to the carbon atom immediately adjacent to the carboxylate group (i.e., the a-carbon). Other types of amino acids exist when the amino group is attached to a different carbon atom, such as, for example p-amino acids and y-amino acids.

[0046] When p-amino acids are incorporated into peptides, two main types of 0- peptides exist: those with the side chain residue, R, on the carbon next to the amine are called p3peptides and those with the side chain residue on the carbon next to the carbonyl group are called p2amino acids. Further, p-amino acids may adopt L- or D- stereochemistry. Unless otherwise indicated, all p-amino acid abbreviations represent either isomer, i.e., the L-isomer, the D-isomer, or combinations thereof.

[0047] Gamma (y)-amino acids are amino acids with the carbon atom to which the amino group attaches is separated from the carboxylate moiety by two carbon atoms.

[0048] For additional modified and unusual amino acids, see §2422 of the MPEP, particularly Table 4 at 2400-24. Additionally, “Ac” indicates N-acetyl and “cyclo” and “c”Docket No. 183B-412975-WO refers to a cyclic structure. “NH2” indicates an amine group, typically added on the C- terminus of a polypeptide. Accordingly, as used herein, an — NH2 moiety on the C-terminus of a peptide indicates an amidated C-terminus.

[0049] The term “acyl” includes a group RCO — , where R is an organic group. An example is the acetyl group CH3CO — , referred to herein as “Ac.”

[0050] A peptide is “acylated” when an alkyl or substituted alkyl group as defined above is bonded through one or more carbonyl { — (C=O) — } groups. A peptide is most usually acylated at the N-terminus.

[0051] An “amine” includes compounds that contain an amine group ( — NH2).

[0052] An “amide” includes compounds that have a trivalent nitrogen attached to a carbonyl group (i.e., — CO — NH2), such as for example methylamide, ethylamide, propylamide, and the like. A peptide is most usually amidated at the C-terminus by the addition of an amine ( — NH2) moiety to the C-terminal carboxyl group.

[0053] As used herein, sugar alcohols are polyols, typically derived from sugars. The term “sugar” refers to monosaccharides, disaccharides, and / or polysaccharides. Examples of sugars include, but are not limited to, sucrose, lactose, trehalose, maltose, dextrose, and the like.

[0054] The terms “active ingredient” and “active compound” refer to a biologically active substance, whether naturally or non-naturally occurring, that is the main component of the pharmaceutical composition which elicits the intended effect of an administered therapeutic. This can be any component that drives the pharmacological activity or direct effect in the diagnosis, cure, mitigation, treatment, or prevention of disease, such as cachexia.

[0055] A “formulation” or “formula” refers to the combination of substances including an active ingredient and a component, such as a pharmaceutically acceptable carrier, to form a pharmaceutical composition. The pharmaceutical composition can be formulated by any means known in the art, including but not limited to formulation as, suspensions, powders, lyophilized preparations, and may be mixed and formulated with buffers, binders, excipients, stabilizers, lubricants, oils, adjuvants, antioxidants and other agents known in the art to yield a formulation suitable for subcutaneous administration.Docket No. 183B-412975-WO

[0056] The formulations of the present technology are injected parenterally, such as subcutaneously. The terms “administering” or “administer” include delivery of the formulations of the present technology to a subject by parenteral administration, such as subcutaneous administration.

[0057] “Cachexia” refers to a state of general ill health and malnutrition characterized by loss of body mass including loss of weight, loss of muscle mass (skeletal, smooth, and / or cardiac muscle), loss of fat mass, or a combination thereof, and wasting. It is often associated with and induced by certain diseases or conditions such as, but not limited to, cancer, cystic fibrosis, or AIDS. The term “cancer cachexia” refers to cachexia induced by cancer.

[0058] “Anorexia” refers to a loss of appetite, whether brought on by medical, physiological, or psychological factors. Anorexia is often closely associated with, and generally contributes to, cachexia seen in patients with advanced cancers and other conditions.

[0059] As used herein, the term “isotonic” refers to fluids such as a solution having the same effective osmotic pressure as another solution, especially one in a cell or a body fluid. In some instances, an isotonic solution has the same concentration of solutes as the blood, such as an isotonic saline solution.

[0060] The terms “treat,” “treatment,” and “treating” refer to a manner of providing a pharmaceutical composition and / or melanocortin analog to alleviate disease outcomes. This includes utilizing administration techniques as described in the context of the present technology. Efficacy of treatment can be determined by measuring biomarkers as described in the context of the present technology.

[0061] The terms “subject” and “patient” refer to anyone being evaluated for disease or being administered a therapeutic or pharmaceutical composition. This includes people without diagnosed or confirmed disease. This also includes people with diagnosed or confirmed disease, such as cachexia.Docket No. 183B-412975-WO

[0062] The disclosure of all publications, patents, and published patent applications listed herein are hereby incorporated by reference in their entireties, including but not limited to U.S. Patent Nos. 8,541 ,545 and 9,534,018 and PCT Publication No. WO2025123055.Pharmaceutical Compositions and Formulations

[0063] The present technology provides pharmaceutical compositions and formulations comprising a non-naturally occurring melanocortin antagonist analog and one or more pharmaceutically acceptable carriers and / or excipients.

[0064] Non-naturally occurring melanocortin analogs described herein may be selective for the melanocortin 4 receptor and / or melanocortin 3 receptor over other melanocortin receptors, i.e., the melanocortin 1 , melanocortin 2, and melanocortin 5 receptors. Some of the melanocortin analogs bind the melanocortin 3 receptor with greater affinity than the melanocortin 4 receptor, whereas other melanocortin analogs bind the melanocortin 4 receptor with greater affinity than the melanocortin 3 receptor. Certain melanocortin analogs bind the melanocortin 3 receptor with the same or generally similar affinity as the melanocortin 4 receptor.

[0065] The non-naturally occurring melanocortin analogs of the present technology may be full antagonists for one or more melanocortin receptors. A full antagonist may comprise a non-naturally occurring melanocortin analog having a maximum effect (Emax) agonist value of greater than or equal to 80%.

[0066] The non-naturally occurring melanocortin analogs of the present technology may be partial agonists or partial antagonists of one or more melanocortin receptor. A partial agonist or antagonist may comprise a non-naturally occurring melanocortin analog having a maximum effect Emax agonist value of less than 80%.

[0067] If a non-naturally occurring melanocortin analog’s Emax antagonist value is greater than its Emax agonist value, then the non-naturally occurring melanocortin analog may be classified as an agonist (e.g., a full agonist or a partial agonist). Similarly, if a non- naturally occurring melanocortin analog’s Emaxagonist value is greater than it’s Emaxantagonist value, then the non-naturally occurring melanocortin analog may be classified as an antagonist (e.g., a full antagonist or a partial antagonist).Docket No. 183B-412975-WO

[0068] The non-naturally occurring melanocortin analogs of the present technology may be one or more of (i) a full MC3R antagonist and a full MC4R antagonist; (ii) a full MC3R antagonist and a partial MC4R antagonist; (iii) a full MC3R antagonist having no MC4R agonist or antagonist activity; (iv) a full MC3R antagonist and a partial MC4R agonist; (v) a partial MC3R antagonist and a full MC4R antagonist; (vi) a partial MC3R antagonist and a partial MC4R antagonist; (vii) a partial MC3R antagonist having no MC4R agonist or antagonist activity; or (viii) a partial MC3R antagonist and a partial MC4R agonist.

[0069] The non-naturally occurring melanocortin analogs in accordance with the present technology may have structural features that impart specific properties on the analogs, such as, for example, degradation resistance, enhanced epithelial, gastrointestinal, and / or blood brain barrier transport, and binding affinity for the MC4R and / or MC3R. For example, in some embodiments, the non-naturally occurring melanocortin analogs comprise one or more of (i) blood brain barrier passage capabilities, (ii) enhanced epithelial and / or gastrointestinal transport; (iii) degradation resistance; or (iv) equipotency on MC3R and MC4R activity. In some embodiments, the non-naturally occurring melanocortin analogs comprise two or more of (i)-(iv). In some embodiments, the non-naturally occurring melanocortin analogs comprise each of (i)-(iv). Accordingly, in some embodiments, the melanocortin analogs include a stabilizing N-terminus, and / or a C-terminus that provides enhanced transport of the analog. In some embodiments, melanocortin analogs include a D-valine-D-proline (dVal-dPro) chain as their C-terminus, which may provide enhanced transport and resistance to degradation Additionally, in some embodiments, the melanocortin analogs have one or more beta hairpin (p-hairpin) and / or beta turn (p-turn) structures. In general, cyclization and D-amino acids may induce and / or stabilize beta-turns.

[0070] The presence of certain structural features may impart the non-naturally occurring melanocortin analogs of the present technology with specific binding properties. For example, inclusion of large amino acids like dNal(2’) at the R4position may result in enhanced inhibition of the melanocortin 4 and the melanocortin 3 receptors. Accordingly, melanocortin analogs having amino acids like and dNal(2’) at R4may be full antagonists on MC3R and MC4R. Additionally, smaller amino acids, such as p(F)dPhe, may confer inhibitory activity on the melanocortin analogs when Pro is included at the R3Docket No. 183B-412975-WO position. Such melanocortin analogs may by full antagonists on MC3R and have no activity or partial activity (agonist or antagonist) on MC4R.

[0071] The non-naturally occurring melanocortin antagonist analogs included in the pharmaceutical compositions and formulations of the present technology may be any melanocortin analog that has antagonist activity on the melanocortin 3 receptor and / or melanocortin 4 receptor, provided that the melanocortin analog does not comprise the sequence Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0072] In some embodiments, the non-naturally occurring melanocortin antagonist analog has at least one cationic amino acid residue. As used herein, the term “cationic amino acid residue” refers to an amino acid residue with a side chain that may adopt a positive charge in solution. For example, when lysine exists in a free form, i.e., when the side chain amine is not engaged in a bond or otherwise unable to adopt a positive charge, lysine is a cationic amino acid residue.. On the other hand, when the amine side chain of lysine is engaged in an intramolecular bond or otherwise unable to adopt a positive change,, lysine is not a cationic residue. Likewise, an “anionic amino acid residue” refers to an amino acid residue with a side chain that may adopt a negative charge in solution. For example, when aspartic acid exists in a free form, e.g., when the side chain carboxylic acid is not engage in a bond or otherwise unable to adopt a positive charge, aspartic acid is an anionic amino acid residue. On the other hand, when the carboxylic acid side chain of aspartic acid is engaged in a bond or otherwise unable to adopt a negative charge, aspartic acid is not an anionic residue.

[0073] In some embodiments, the non-naturally occurring melanocortin antagonist analog has at least one cationic amino acid residue and no anionic amino acid residues.

[0074] The non-naturally occurring melanocortin antagonist analog may be linear or cyclized. In some embodiments, the non-naturally occurring melanocortin analog is linear. In some embodiments, the non-naturally occurring melanocortin analog is cyclized. In further embodiments, the non-naturally occurring melanocortin analog is cyclized through a sidechain linkage between an acidic amino acid residue and a basic amino acid residue.Docket No. 183B-412975-WO

[0075] In some embodiments, the non-naturally occurring melanocortin antagonist analog has an isoelectric point (pl) of at least about 10 in an aqueous solution. In some embodiments, the non-naturally occurring melanocortin analog has a pl of about 10 to about 12.5 in an aqueous solution. In further embodiments, the non-naturally occurring melanocortin analog has at least one cationic amino acid residue and a pl of about 10 to about 12.5. In still further embodiments, the non-naturally occurring melanocortin analog has an arginine residue and a pl of about 10 to about 12.5. In still further embodiments, the non- naturally occurring melanocortin analog has a cyclic region with an arginine residue positioned therein and a pl of at least about 10. In yet further embodiments, the non-naturally occurring melanocortin analog has a cyclic region with an arginine residue positioned therein and a pl of about 10 to about 12.5.

[0076] In some embodiments, the non-naturally occurring melanocortin antagonist analog comprises moiety (A),X1-R1-R2-R3-R4-R5-R6-R7-Y1 (A), wherein:R1 is absent or is an amino acid or amino acid derivative;R4 is selected from the group consisting of optionally substituted dNal(2’), Phe, Bip, and dBip; at least one of R2-R7 is a cationic amino acid residue;Xi is an optionally present N-terminus;Y1 is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a side chain linkage between R2 and R7; provided that: moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0077] In some embodiments, moiety (A) is cyclized through a lactam bond between R2and R7. In some embodiments, Xi is absent. In some embodiments, Y1 is a C-terminus comprising two amino acids. In further embodiments, Y1 is a C-terminus comprising a dVal- dPro moiety.Docket No. 183B-412975-WO

[0078] In some embodiments, the non-naturally occurring melanocortin analog comprises moiety (A) and has an isoelectric point of at least about 10 in aqueous solution. In further embodiments, the non-naturally occurring melanocortin analog comprises moiety (A) and has an isoelectric point of about 10 to about 12.5 in aqueous solution.

[0079] In some embodiments, the non-naturally occurring melanocortin antagonist analog comprises a sequence of Formula (I),X1-X2-R1-R2-R3-R4-R5-R6-R7-R8-R9-Y1-Y2-Y3-Y4-Y5-Y6-Y7(I), wherein:X1is absent or norlecuine (Nle);X2is absent, Nle, or phenylalanine (Phe);R1is selected from the group consisting of Nle, Phe, trans-4-guanidinyl-proline (transPro(guan)), cis-4-guanidinyl-proline (cisPro(guan)), arginine (Arg), D-arginine (dArg), D-methionine (dMet), D-isoleucine (dlle), D-leucine (dLeu), D-valine (dVal), D-alanine (dAla), alanine (Ala), tertleucine (Tie), D-tertleucine (dTle), D-norleucine (dNIe), norvaline (Nva), glycine (Gly), D-cysteine (dCys), D-phenylalanine (dPhe), tyrosine (Tyr), D-tyrosine (dTyr), D-glutamine (dGIn), D-asparagine (dAsn), dimethyltyrosine (Dmt), glutamic acid (Glu), lysine (Lys), D-lysine (dLys), histidine (His), D-histidine (dHis), and D-proline (dPro);R2is selected from the group consisting of dCys, aspartic acid (Asp), D-aspartic acid (dAsp), penicillamine (Pen), D-penicillamine (dPen), Glu, and cysteine (Cys);R3is absent or selected from the group consisting of proline (Pro), octohydroindole- 2-carboxylic acid (Oic), phenylalanyl-histidine (Phe-His), prolyl-histidine (Pro-His), phenylalanyl-phenylalanine (Phe-Phe), transPro(guan), cisPro(guan), 4-amino-1 ,2,4,5- tetrahydro-2-benzazepin-3-one (Aba), 4-amino-1 ,4,5,6-tetrahydroazepino[4,3-b]indol- 3(2H)-one (Aia), 7-amino-7,8-dihydro-4H-[1 ,2,3]triazolo-[1 ,5-a][1 ,4]diazepin-6(5H)-one (Ata), 2-aminoindone-2-carboxylic acid (Aic), D-alanyl-histidine (dAla-His), histidine (His), dHis, Ala, Gly, leucine (Leu), isoleucine (lie), valine (Vai), histidyl-arginine (His-Arg), prolylarginine (Pro-Arg), indoline-2-carboxylic acid (loc), 1 ,2,3,4-tetrahydroisoquinoline-3- carboxylic acid (Tic), Glu, glutamyl-histidine (Glu-His), alanyl-histidine (Ala-His), Phe, biphenylalanine (Bip), tryptophan (Trp), Tyr, glutamine (Gin), and hydroxyproline (Hyp);R4is selected from the group consisting of Pro, D-2’-naphthylalanine (dNal(2’)), D- phenylalanine (dPhe), para-iodo-D-phenylalanine (p(l)dPhe), para-bromo-D-phenylalanineDocket No. 183B-412975-WO(p(Br)dPhe), para-fluoro-D-phenylalanine (p(F)dPhe), para-trifluoromethyl-D-phenylalanine (p(CFs)dPhe), and para-chloro-D-phenylalanine (p(CI)dPhe);R5is absent, or selected from the group consisting of transPro(guan), cisPro(guan), Lys, ornithine (Orn), His, Ala, and Arg;R6is selected from the group consisting Trp, tryptyl-proline (Trp-Pro), tryptyl-glycine (Trp-Gly), D-tryptophan (dTrp), dNal(2’), Aia, Aba, Ata, 1 ’-napthylalanine (Nal(1 ’)), Phe, Tyr, dPhe, dTyr, 2’-napthylalanine (Nal(2’)), D-1 ’-naphthylalanine (dNal(1 ’)), and Tic;R7is absent or selected from the group consisting of Arg, Lys, dLys, Cys, dCys, Orn, D-ornithine (dOrn), Pen, and dPen;R8is absent or Trp;R9is absent or Lys;Y1is absent or selected from the group consisting of Vai, dVal, dLeu, d He, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; andDocket No. 183B-412975-WO a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, a lactam bond between R2and R9, when R2is Asp and R9is Lys; provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then either (i) R3is Pro, R4is dNal(2’) or p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn or dOrn, or (ii) R3is His and R4is p(Br)dPhe and when R1is Arg, then R3is His or Pro-His, when R4is dPhe, then either R3is Oic or R6is dNal(2’), when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R5is Arg or His, R6is not dTrp, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent and, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, when R4is p(F)dPhe, then R3is Pro, Trp, or Tyr, wherein when R3is Pro, then either (i) R2is Cys or (ii) R6is dNal(2’), when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal, when R4is dNal(2’) and R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated, (iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly, (iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from transPro(guan), cisPro(guan), Arg, dArg, dMet, dlle, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, when R4is dNal(2’) and R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Asp or Glu, and R5is selected from transPro(guan), cisPro(guan), and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Phe-His, Hyp, Pro-His, Phe- Phe, transPro(guan), cisPro(guan), Aba, Aia, Ata, Aic, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, lie, Vai, and Trp.Docket No. 183B-412975-WO

[0080] In some embodiments, the non-naturally occurring melanocortin antagonist comprises a sequence of Formula (I), wherein:X1is absent or norlecuine (Nle);X2is absent, Nle, or phenylalanine (Phe);R1is selected from the group consisting of Nle, Phe, trans-4-guanidinyl-proline (transPro(guan)), cis-4-guanidinyl-proline (cisPro(guan)), arginine (Arg), D-arginine (dArg), D-methionine (dMet), D-isoleucine (dlle), D-leucine (dLeu), D-valine (dVal), D-alanine (dAla), alanine (Ala), tertleucine (Tie), D-tertleucine (dTle), D-norleucine (dNIe), norvaline (Nva), glycine (Gly), D-cysteine (dCys), D-phenylalanine (dPhe), tyrosine (Tyr), D-tyrosine (dTyr), D-glutamine (dGIn), D-asparagine (dAsn), dimethyltyrosine (Dmt), glutamic acid (Glu), lysine (Lys), D-lysine (dLys), histidine (His), D-histidine (dHis), and D-proline (dPro);R2is selected from the group consisting of dCys, aspartic acid (Asp), D-aspartic acid (dAsp), penicillamine (Pen), D-penicillamine (dPen), Glu, and cysteine (Cys);R3is absent or selected from the group consisting of proline (Pro), octohydroindole- 2-carboxylic acid (Oic), phenylalanyl-histidine (Phe-His), prolyl-histidine (Pro-His), phenylalanyl-phenylalanine (Phe-Phe), transPro(guan), cisPro(guan), 4-amino-1 ,2,4,5- tetrahydro-2-benzazepin-3-one (Aba), 4-amino-1 ,4,5,6-tetrahydroazepino[4,3-b]indol- 3(2H)-one (Aia), 7-amino-7,8-dihydro-4H-[1 ,2,3]triazolo-[1 ,5-a][1 ,4]diazepin-6(5H)-one (Ata), 2-aminoindone-2-carboxylic acid (Aic), D-alanyl-histidine (dAla-His), histidine (His), dHis, Ala, Gly, leucine (Leu), isoleucine (lie), valine (Vai), histidyl-arginine (His-Arg), prolylarginine (Pro-Arg), indoline-2-carboxylic acid (loc), 1 ,2,3,4-tetrahydroisoquinoline-3- carboxylic acid (Tic), Glu, glutamyl-histidine (Glu-His), alanyl-hsitidine (Ala-His), Phe, biphenylalanine (Bip), tryptophan (Trp), Tyr, glutamine (Gin), and hydroxyproline (Hyp);R4is selected from the group consisting of Pro, D-2’-naphthylalanine (dNal(2’)), D- phenylalanine (dPhe), para-iodo-D-phenylalanine (p(l)dPhe), para-bromo-D-phenylalanine (p(Br)dPhe), para-fluoro-D-phenylalanine (p(F)dPhe), para-trifluoromethyl-D-phenylalanine (p(CFs)dPhe), and parachloro-D-phenylalanine (p(CI)dPhe);R5is absent, or selected from the group consisting of transPro(guan), cisPro(guan), Lys, ornithine (Orn), His, Ala, and Arg;Docket No. 183B-412975-WOR6is selected from the group consisting Trp, D-tryptophan (dTrp), dNal(2’), Aia, Aba, Ata, 1 ’-napthylalanine (Nal(1 ’)), Phe, Tyr, dPhe, dTyr, 2’-napthylalanine (Nal(2’)), D-T- naphthylalanine (dNal(1 ’)), and Tic;R7is absent or selected from the group consisting of Arg, Pro, Gly, Lys, dLys, Cys, dCys, Orn, D-ornithine (dOrn), Pen, and dPen;R8is absent, Trp, or Lys;R9is absent or Lys;Y1is absent or selected from the group consisting of Vai, dVal, dLeu, d He, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and a lactam bond between R2and R9, when R2is Asp and R9is Lys,Docket No. 183B-412975-WO provided that the non-naturally occurring melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 3);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 4);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 6);Ac-Nle-c[Glu-His-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 7);Ac-dGln-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dGln-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 9);Ac-dGln-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 10);Ac-dGln-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 1 1 );Ac-dAsn-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-dAsn-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 13);Ac-dAsn-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 14);Ac-dAsn-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 15);Ac-Nle-c[Glu-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 16);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 17);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Ac-Ala-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 19);Ac-Ala-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 20);Ac-Ala-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 21 );Ac-Nle-c[Glu-Oic-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 22);Ac-Nle-c[Glu-Oic-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 23);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Docket No. 183B-412975-WODmt-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 25);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Ac-dAla-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 27);Ac-dAla-c[Glu-His-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 28);Ac-dAla-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 29);Ac-Nle-c[Glu-Pro-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 31 );Ac-Nle-c[Glu-His-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 32);Ac-Nle-c[Glu-His-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 33);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 34);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 35);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 37);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 38);Ac-Arg-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 39);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 40);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Glu-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 42);Ac-Nle-c[Asp-Trp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 43);Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 44);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 45);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 46);Ac-Nle-c[Asp-Aba-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 47);Ac-Nle-c[Asp-Aia-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 48);Docket No. 183B-412975-WOAc-Nle-c[Asp-Ata-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 49);Ac-Nle-c[Asp-His-dPhe-transPro(guan)-Trp-Lys]-d\ / al-dPro-NH2(SEQ ID NO: 50);Ac-Nle-c[Asp-His-dPhe-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 51 );Ac-Nle-c[Asp-Pro-dPhe-transPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 52);Ac-Nle-c[Asp-Pro-dPhe-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 53);Ac-Nle-c[Asp-Pro-dPhe-Arg-Aia-Lys]-dVal-dPro-NH2 (SEQ ID NO: 54);Ac-Nle-c[Asp-Pro-dPhe-Arg-Aba-Lys]-dVal-dPro-NH2(SEQ ID NO: 55);Ac-Nle-c[Asp-Pro-dPhe-Arg-Ata-Lys]-dVal-dPro-NH2 (SEQ ID NO: 56);Ac-Nle-c[Asp-Pro-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 57);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 58);Ac-dLeu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 59);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 60);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 61 );Ac-dNle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 62);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 63);Ac-dTyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 64);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 65);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Nle-c[Asp-Leu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 67);Ac-Nle-c[Asp-Pro-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 68);Ac-Nle-c[Asp-Pro-dPhe-Lys-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 69);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 70);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-Pro-NH2(SEQ ID NO: 71 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 72);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 73);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-NH2(SEQ ID NO: 74);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Pro-NH2(SEQ ID NO: 75);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Arg-NH2(SEQ ID NO: 76);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dArg-NH2(SEQ ID NO: 77);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 78);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 79);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 80);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Pro-Val-NH2(SEQ ID NO: 81 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dPro-NH2(SEQ ID NO: 82);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Val-Pro-NH2(SEQ ID NO: 83);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dVal-dPro-NH2(SEQ ID NO: 84);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dVal-dPro-NH2(SEQ ID NO: 85);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Pro-Val-NH2(SEQ ID NO: 86);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Val-Pro-NH2(SEQ ID NO: 87);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2(SEQ ID NO: 88);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 89);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dPro-NH2(SEQ ID NO: 90);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 91 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dTle-NH2(SEQ ID NO: 92);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dPro-NH2(SEQ ID NO: 93);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 94);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 95);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-dVal-dPro-NH2(SEQ ID NO: 96);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 97);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 98);Ac-Nle-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 99);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Trp-NH2(SEQ ID NO: 100);Ac-Nle-c[Asp-loc-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 101 );Ac-Nle-c[Asp-Tic-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 102);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 103);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 104);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-dLys-dAsp-NH2(SEQ ID NO: 105);Ac-Nle-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 106);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 107);Ac-dArg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 108);Ac-Nle-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 109);Ac-Arg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 10);Ac-dArg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 111 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 12);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-dVal-NH2(SEQ ID NO: 1 13);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAla-NH2(SEQ ID NO: 114);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-NH2(SEQ ID NO: 115);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dHyp-NH2(SEQ ID NO: 116);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dAsn-NH2(SEQ ID NO: 117);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Asp-NH2(SEQ ID NO: 1 18);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-dPro-NH2(SEQ ID NO: 119);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Hyp-NH2 (SEQ ID NO: 120);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Ala-Ala-NH2 (SEQ ID NO: 121 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-Gly-NH2(SEQ ID NO: 122);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-dPro-NH2 (SEQ ID NO: 123);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-dPro-NH2 (SEQ ID NO: 124);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-NH2 (SEQ ID NO: 125);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-NH2 (SEQ ID NO: 126);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-NH2 (SEQ ID NO: 127);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-NH2 (SEQ ID NO: 128);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-OH (SEQ ID NO: 129);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 130);Ac-Nle-c[dAsp-Pro-dPhe-Arg-Trp-dl_ys]-dPro-dVal-NH2(SEQ ID NO: 131 );Ac-Nle-c[Asp-Phe-Phe-Pro-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 132);Ac-Nle-Phe-Phe-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 133);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dLeu-dPro-NH2 (SEQ ID NO: 134);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 135);Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 136);His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 137); dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 138); dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 139);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 140);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 141 );Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 142);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 143);Docket No. 183B-412975-WOAc-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 144);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 145);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2(SEQ ID NO: 146);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dVal-dPro-NH2(SEQ ID NO: 147);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 148);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dPro-NH2 (SEQ ID NO: 149);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 150);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 151 );Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 152);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 153);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 154);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 155);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 156);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 157);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 158);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 159);Ac-Nle-c[Asp-dHis-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 160);Ac-Nle-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 161 );Ac-Nle-c[Asp-Tyr-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 162);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2 (SEQ ID NO: 163);Ac-Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 164);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 165);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 166);Ac-Nle-c[Asp-Val-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 167);Docket No. 183B-412975-WOAc-Nle-c[Asp-lle-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 168);Ac-Nle-c[Asp-Gly-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 169);Ac-Nle-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 170);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 171 );Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-dPro-NH2(SEQ ID NO: 172);Ac-Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 173);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 174);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 175);Ac-Arg-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 176);Ac-Arg-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 177);Ac-Lys-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 178);Ac-Lys-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 179);Ac-Lys-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 180);Ac-Glu-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 181 );Ac-His-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 182);Ac-Glu-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 183);Ac-His-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 184);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 185);Ac-His-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 186);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 187);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 188);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 189);Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 190);Ac-Nle-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 191 );Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 192);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 193);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 194);Ac-Arg-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 195);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 196);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 197);Ac-Nle-c[Asp-His-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 198);Ac-dGln-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 199);Ac-dGln-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 200);Ac-dAsn-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 201 );Ac-dAsn-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 202);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 203);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 204);Ac-Ala-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 205);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 206);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 207);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 208);Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 209);Ac-dAla-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 210);Ac-Nle-c[Asp-Pro-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 211 );Ac-Nle-c[Asp-His-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 212);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 213);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 214);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 215);Docket No. 183B-412975-WOAc-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 216);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 217);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 218);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 219);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 220);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 221 );Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 222);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 223);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2 (SEQ ID NO: 224);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 225);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2 (SEQ ID NO: 226);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2 (SEQ ID NO: 227);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2 (SEQ ID NO: 228);Ac-Nle-c[Asp-His-dPhe-Ala-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 229);Ac-Nle-c[Asp-Pro-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 230);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 231 );Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 232);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 233);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 234);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 235);Ac-Nle-c[Asp-Pro-dPhe-Arg-dNal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 236);Ac-Nle-c[Asp-Pro-dPhe-Arg-Phe-Lys]-dVal-dPro-NH2(SEQ ID NO: 237);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro (SEQ ID NO: 239);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 240);Ac-Nle-c[Asp-Phe-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 241 );Ac-Nle-c[Asp-Bip-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 242);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 243);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Nle-c[Asp-Aba-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 244);Ac-Nle-c[Asp-Aia-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 245);Ac-Nle-c[Asp-Ata-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 246);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 247);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 248);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 249);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 250);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 251 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 252);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 253);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 254);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 255);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 256);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 257);Ac-Lys-c[Asp-His-p(CI)dP e-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 258);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 259);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 260);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 261 );Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 262);Ac-Tyr-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 263);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 264);Ac-Nle-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 265);Ac-Arg-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 266);Ac-Arg-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 267);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 268);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 269);Ac-dGln-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 270);Ac-dGln-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 271 );Ac-dAsn-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 272);Ac-dAsn-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 273);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 274);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 275);Ac-Ala-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 276);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 277);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 278);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 279);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 280);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 281 );Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 282);Ac-Nle-c[Asp-Oic-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 283);Dmt-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 284);Ac-dAla-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 285);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-p(CI)dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 286);Ac-Glu-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 287);Ac-Glu-c[Asp-His-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 288);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 289);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 290);Ac-Nle-c[Asp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 291 );Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 292);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 293);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 294);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 295);Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 296);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 297);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 298);Ac-Nle-c[Asp-Pro-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 299);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 300);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 301 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 302);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 303);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 304);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 305);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 306);Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 307);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 308);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 309);Docket No. 183B-412975-WOAc-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 310);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 311 );Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 312);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 313);Ac-Nle-c[Cys-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 314);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 315);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 316);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 317);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 318);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 319);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 320);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 321 );Ac-Nle-c[Asp-His-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 322);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 323);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 324);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 325);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 326);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 327);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 328);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 329);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 330);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 331 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 332);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 333);Docket No. 183B-412975-WOAc-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 334);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 335);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 336);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 337);Ac-Nle-c[Asp-dHis-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 338);Ac-Nle-c[Asp-Gln-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 339);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 340);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 341 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 342);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 343);Ac-dGln-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 344);Ac-dGln-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 345);Ac-dAsn-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 346);Ac-dAsn-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 347);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 348);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 349);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 350);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 351 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 352);Ac-Nle-c[Asp-Oic-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 353);Dmt-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 354);Ac-dAla-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 355);Ac-Nle-c[Asp-Pro-d(F)Phe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 356);Ac-Glu-c[Asp-Pro-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 357);Docket No. 183B-412975-WOAc-Glu-c[Asp-His-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 358);Ac-dPhe-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 359);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 360);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 361 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 362);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-NH2(SEQ ID NO: 363);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 364);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-NH2(SEQ ID NO: 365);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 366);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 367);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 368);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 369);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 370);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 371 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 372);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-OH (SEQ ID NO: 373);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 374);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-OH (SEQ ID NO: 375);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 376);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 377);Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 378);Ac-Nle-c[dAsp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 379);Ac-Arg-c[Asp-Gln-p(F)dPhe-Arg-Trp-Gly-Orn]-NH2(SEQ ID NO: 380);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 381 );Docket No. 183B-412975-WOAc-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 382);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 383);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 384);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 385);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 386);Ac-Nle-c[Asp-Phe-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 387);Ac-Nle-c[Asp-Bip-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 388);Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 389);Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 390);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 391 );Ac-Nle-c[Asp-Bip-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 392);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dOys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 395);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 396);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 397);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 398);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 399);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 400);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 401 );Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Ala-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 404);Ac-Nle-c[dPen-Leu-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 405);Docket No. 183B-412975-WOAc-Nle-c[dPen-Gly-dNal(2’)-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 406);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 414);Ac-Nle-c[Asp-Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 415);Ac-Nle-c[Asp-His-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 416);Ac-dGln-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 417);Ac-dAsn-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 418);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 419);Ac-Ala-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 420);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 421 );Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 422);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 423);Ac-dAla-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 424);Ac-Nle-c[Asp-His-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 425);Ac-Glu-c[Asp-His-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 426);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 427);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 428);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 429);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-dNal(2’)-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 430);Ac-dGln-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 431 );Ac-dAsn-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 432);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 433);Ac-Nle-c[dAsp-dNal(2')-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 434);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 435);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 436);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 437);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Nle-Asp-Pro-dNal(2')-Arg-Trp-Lys-NH2(SEQ ID NO: 440);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-dGln-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 449);Ac-dGln-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 450);Ac-dGln-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 451 );Ac-dGln-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 452);Ac-dAsn-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 453);Docket No. 183B-412975-WOAc-dAsn-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 454);Ac-dAsn-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 455);Ac-dAsn-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 456);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-NH2(SEQ ID NO: 460);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dArg-dPro-NH2(SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.

[0081] In some embodiments of the sequence of Formula (I), R9is absent. In further embodiments, R8is absent. In still further embodiments, Y1is present. Accordingly, in some embodiments, the sequence of Formula (I) is a sequence of Formula (IA):X1-X2- R1- R2- R3- R4- R5- R6- R7- Y1-Y2- Y3-Y4-Y5- Y6- Y7( I A) , wherein:X1is absent or Nle;Docket No. 183B-412975-WOX2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, Lys, dLys, His, dHis, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, His, dHis, Ala, Gly, Leu, He, Vai, His-Arg, Pro-Arg, loc, Tic, Glu, Glu-His, Ala-His, Phe, Bip, Trp, Tyr, Gin, and Hyp;R4is selected from the group consisting of dNal(2’), dPhe, p(l)dPhe, p(Br)dPhe, p(F)dPhe, p(CF3)dPhe, and p(CI)dPhe;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, Trp-Pro, Trp-Gly dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, Nal(2’), dNal(1 ’), and Tic;R7is selected from the group consisting ofLys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen;Docket No. 183B-412975-WO a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then either (i) R3is Pro, R4is dNal(2’) or p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn or dOrn, or (ii) R3is His and R4is p(Br)dPhe and when R1is Arg, then R3is His or Pro-His, when R4is dPhe, then either R3is Oic or R6is dNal(2’), when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R5is Arg or His, R6is not dTrp, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent and, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, when R4is p(F)dPhe, then R3is Pro, Trp, or Tyr, wherein when R3is Pro, then either (i) R2is Cys or (ii) R6is dNal(2’), when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal, when R4is dNal(2’) and R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated, (iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly, (iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from Arg, dArg, dMet, dlle, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, when R4is dNal(2’) and R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Glu, and R5is and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected fromDocket No. 183B-412975-WOAla, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Hyp, Pro-His, Phe-Phe, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, lie, Vai, and Trp.

[0082] In some embodiments, the non-naturally occurring melanocortin antagonist comprises a sequence of Formula (IA):X1-X2- R1- R2- R3- R4- R5- R6- R7- Y1-Y2- Y3-Y4-Y5- Y6- Y7( I A) , wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, Lys, dLys, His, dHis, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, His, dHis, Ala, Gly, Leu, He, Vai, His-Arg, Pro-Arg, loc, Tic, Glu, Glu-His, Ala-His, Phe, Bip, Trp, Tyr, Gin, and Hyp;R4is selected from the group consisting of dNal(2’), dPhe, p(l)dPhe, p(Br)dPhe, p(F)dPhe, p(CF3)dPhe, and p(CI)dPhe;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, Trp-Pro, Trp-Gly dTrp, dNal(2’), Nal(1 Phe, Tyr, dPhe, dTyr, Nal(2’), dNal(T), and Tic;R7is selected from the group consisting ofLys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Docket No. 183B-412975-WOY5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then either (i) R3is Pro, R4is dNal(2’) or p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn or dOrn, or (ii) R3is His and R4is p(Br)dPhe and when R1is Arg, then R3is His or Pro-His, when R4is dPhe, then either R3is Oic or R6is dNal(2’), when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R5is Arg or His, R6is not dTrp, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent and, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, when R4is p(F)dPhe, then R3is Pro, Trp, or Tyr, wherein when R3is Pro, then either (i) R2is Cys or (ii) R6is dNal(2’), when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal, when R4is dNal(2’) and R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, andDocket No. 183B-412975-WOR6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated, (iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly, (iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from Arg, dArg, dMet, dlle, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, when R4is dNal(2’) and R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Glu, and R5is and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Hyp, Pro-His, Phe-Phe, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, lie, Vai, and Trp.

[0083] In some embodiments, the non-naturally occurring melanocortin antagonist comprises a sequence of Formula (IA), wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, Lys, dLys, His, dHis, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, His, dHis, Ala, Gly, Leu, He, Vai, His-Arg, Pro-Arg, loc, Tic, Glu, Glu-His, Ala-His, Phe, Bip, Trp, Tyr, Gin, and Hyp;R4is selected from the group consisting of dNal(2’), dPhe, p(l)dPhe, p(Br)dPhe, p(F)dPhe, p(CF3)dPhe, and p(CI)dPhe;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, Nal(2’), dNal(T), and Tic;R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn,Pen, and dPen;R8is absent or Lys;Docket No. 183B-412975-WOY1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 3);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 4);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 6);Ac-Nle-c[Glu-His-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 7);Docket No. 183B-412975-WOAc-dGln-c[Glu-Pro-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dGln-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 9);Ac-dGln-c[Glu-His-dNal(2')-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 10);Ac-dGln-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 1 1 );Ac-dAsn-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 12);Ac-dAsn-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 13);Ac-dAsn-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 14);Ac-dAsn-c[Glu-His-p(CI)dPhe-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 15);Ac-Nle-c[Glu-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 16);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 17);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 18);Ac-Ala-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 19);Ac-Ala-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 20);Ac-Ala-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 21 );Ac-Nle-c[Glu-Oic-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 22);Ac-Nle-c[Glu-Oic-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 23);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 24);Dmt-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 25);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 26);Ac-dAla-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 27);Ac-dAla-c[Glu-His-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 28);Ac-dAla-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 29);Ac-Nle-c[Glu-Pro-dNal(2’)-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 30);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 31 );Docket No. 183B-412975-WOAc-Nle-c[Glu-His-dNal(2’)-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 32);Ac-Nle-c[Glu-His-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 33);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 34);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 35);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 37);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 38);Ac-Arg-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 39);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 40);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Glu-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 42);Ac-Nle-c[Asp-Trp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 43);Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 44);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 45);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 46);Ac-Nle-c[Asp-Pro-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 57);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 58);Ac-dLeu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 59);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 60);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 61 );Ac-dNle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 62);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 63);Ac-dTyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 64);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 65);Docket No. 183B-412975-WOAc-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Nle-c[Asp-Leu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 67);Ac-Nle-c[Asp-Pro-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 68);Ac-Nle-c[Asp-Pro-dPhe-Lys-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 69);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 70);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-Pro-NH2(SEQ ID NO: 71 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 72);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 73);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-NH2(SEQ ID NO: 74);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Pro-NH2(SEQ ID NO: 75);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Arg-NH2(SEQ ID NO: 76);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dArg-NH2(SEQ ID NO: 77);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 78);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 79);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 80);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Pro-Val-NH2(SEQ ID NO: 81 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dPro-NH2(SEQ ID NO: 82);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Val-Pro-NH2(SEQ ID NO: 83);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dVal-dPro-NH2(SEQ ID NO: 84);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dVal-dPro-NH2(SEQ ID NO: 85);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Pro-Val-NH2(SEQ ID NO: 86);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Val-Pro-NH2(SEQ ID NO: 87);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2(SEQ ID NO: 88);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 89);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dPro-NH2 (SEQ ID NO: 90);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 91 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dTle-NH2(SEQ ID NO: 92);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dPro-NH2(SEQ ID NO: 93);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 94);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 95);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-dVal-dPro-NH2(SEQ ID NO: 96);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 97);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 98);Ac-Nle-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 99);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Trp-NH2(SEQ ID NO: 100);Ac-Nle-c[Asp-loc-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 101 );Ac-Nle-c[Asp-Tic-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 102);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 103);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 104);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-dLys-dAsp-NH2(SEQ ID NO: 105);Ac-Nle-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 106);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 107);Ac-dArg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 108);Ac-Nle-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 109);Ac-Arg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 10);Ac-dArg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 111 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 12);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-dVal-NH2(SEQ ID NO: 1 13);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAla-NH2 (SEQ ID NO: 114);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-NH2 (SEQ ID NO: 115);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dHyp-NH2 (SEQ ID NO: 116);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dAsn-NH2 (SEQ ID NO: 117);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Asp-NH2 (SEQ ID NO: 1 18);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-dPro-NH2 (SEQ ID NO: 119);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Hyp-NH2 (SEQ ID NO: 120);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Ala-Ala-NH2 (SEQ ID NO: 121 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-Gly-NH2(SEQ ID NO: 122);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-dPro-NH2(SEQ ID NO: 123);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-dPro-NH2(SEQ ID NO: 124);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-NH2(SEQ ID NO: 125);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-NH2(SEQ ID NO: 126);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-NH2(SEQ ID NO: 127);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-NH2(SEQ ID NO: 128);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-OH (SEQ ID NO: 129);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 130);Ac-Nle-c[dAsp-Pro-dPhe-Arg-Trp-dLys]-dPro-dVal-NH2(SEQ ID NO: 131 );Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 136);His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 137); dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 138); dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 139);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 140);Docket No. 183B-412975-WOAc-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 141 );Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 142);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 143);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 144);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 145);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2 (SEQ ID NO: 146);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dVal-dPro-NH2 (SEQ ID NO: 147);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2 (SEQ ID NO: 148);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dPro-NH2 (SEQ ID NO: 149);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 150);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 151 );Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 152);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 153);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 154);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 155);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 156);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 157);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 158);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 159);Ac-Nle-c[Asp-dHis-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 160);Ac-Nle-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 161 );Ac-Nle-c[Asp-Tyr-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 162);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2 (SEQ ID NO: 163);Ac-Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 164);Docket No. 183B-412975-WOAc-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 165);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 166);Ac-Nle-c[Asp-Val-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 167);Ac-Nle-c[Asp-lle-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 168);Ac-Nle-c[Asp-Gly-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 169);Ac-Nle-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 170);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2 (SEQ ID NO: 171 );Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-dPro-NH2 (SEQ ID NO: 172);Ac-Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 173);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 174);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 175);Ac-Arg-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 176);Ac-Arg-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 177);Ac-Lys-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 178);Ac-Lys-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 179);Ac-Lys-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 180);Ac-Glu-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 181 );Ac-His-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 182);Ac-Glu-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 183);Ac-His-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 184);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 185);Ac-His-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 186);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 187);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 188);Docket No. 183B-412975-WOAc-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 189);Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 190);Ac-Nle-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 191 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 192);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 193);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 194);Ac-Arg-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 195);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 196);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 197);Ac-Nle-c[Asp-His-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 198);Ac-dGln-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 199);Ac-dGln-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 200);Ac-dAsn-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 201 );Ac-dAsn-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 202);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 203);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 204);Ac-Ala-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 205);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 206);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 207);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 208);Dmt-c[Asp-Pro-dPhe-Arg-Trp-l_ys]-dVal-dPro-NH2(SEQ ID NO: 209);Ac-dAla-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 210);Ac-Nle-c[Asp-Pro-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 211 );Ac-Nle-c[Asp-His-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 212);Docket No. 183B-412975-WOAc-Glu-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 213);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 214);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 215);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 218);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 219);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 223);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2 (SEQ ID NO: 224);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 225);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2 (SEQ ID NO: 226);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2 (SEQ ID NO: 227);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2 (SEQ ID NO: 228);Ac-Nle-c[Asp-His-dPhe-Ala-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 229);Ac-Nle-c[Asp-Pro-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 230);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 231 );Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 232);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 233);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 234);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 235);Ac-Nle-c[Asp-Pro-dPhe-Arg-dNal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 236);Ac-Nle-c[Asp-Pro-dPhe-Arg-Phe-Lys]-dVal-dPro-NH2(SEQ ID NO: 237);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro (SEQ ID NO: 239);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 240);Docket No. 183B-412975-WOAc-Nle-c[Asp-Phe-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 241 );Ac-Nle-c[Asp-Bip-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 242);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 243);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 247);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 248);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 249);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 250);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 251 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 252);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 253);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 254);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 255);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 256);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 257);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 258);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 259);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 260);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 261 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 262);Ac-Tyr-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 263);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 264);Ac-Nle-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 265);Ac-Arg-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 266);Docket No. 183B-412975-WOAc-Arg-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 267);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 268);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 269);Ac-dGln-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 270);Ac-dGln-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 271 );Ac-dAsn-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 272);Ac-dAsn-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 273);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 274);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 275);Ac-Ala-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 276);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 277);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 278);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 279);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 280);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 281 );Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 282);Ac-Nle-c[Asp-Oic-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 283);Dmt-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 284);Ac-dAla-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 285);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 286);Ac-Glu-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 287);Ac-Glu-c[Asp-His-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 288);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 289);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 290);Docket No. 183B-412975-WOAc-Nle-c[Asp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 291 );Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 292);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 293);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 294);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 295);Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 296);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 297);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 298);Ac-Nle-c[Asp-Pro-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 299);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 300);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 301 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 302);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 303);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 304);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 305);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 306);Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 307);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 308);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 309);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 310);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 311 );Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 312);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 313);Ac-Nle-c[Cys-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 314);Docket No. 183B-412975-WOAc-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 315);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 316);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 317);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 318);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 319);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 320);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 321 );Ac-Nle-c[Asp-His-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 322);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 323);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 324);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 325);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 326);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 327);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 328);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 329);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 330);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 331 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 332);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 333);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 334);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 335);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 336);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 337);Ac-Nle-c[Asp-dHis-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 338);Docket No. 183B-412975-WOAc-Nle-c[Asp-Gln-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 339);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 340);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 341 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 342);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 343);Ac-dGln-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 344);Ac-dGln-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 345);Ac-dAsn-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 346);Ac-dAsn-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 347);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 348);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 349);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 350);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 351 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 352);Ac-Nle-c[Asp-Oic-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 353);Dmt-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 354);Ac-dAla-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 355);Ac-Nle-c[Asp-Pro-d(F)Phe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 356);Ac-Glu-c[Asp-Pro-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 357);Ac-Glu-c[Asp-His-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 358);Ac-dPhe-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 359);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 360);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-d al-dPro-NH2(SEQ ID NO: 361 );Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 368);Docket No. 183B-412975-WOAc-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 369);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 370);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 371 );Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 378);Ac-Nle-c[dAsp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 379);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 381 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 382);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 383);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 384);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 385);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 386);Ac-Nle-c[Asp-Phe-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 387);Ac-Nle-c[Asp-Bip-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 388);Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 389);Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 390);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 391 );Ac-Nle-c[Asp-Bip-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 392);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 395);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 396);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 397);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 398);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 399);Docket No. 183B-412975-WOAc-Nle-c[Cys-dNal(2’)-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 400);Ac-Nle-c[Cys-dNal(2’)-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 401 );Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Ala-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 404);Ac-Nle-c[dPen-Leu-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 405);Ac-Nle-c[dPen-Gly-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 406);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 414);Ac-Nle-c[Asp-Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 415);Ac-Nle-c[Asp-His-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 416);Ac-dGln-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 417);Ac-dAsn-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 418);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 419);Ac-Ala-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 420);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 421 );Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 422);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 423);Docket No. 183B-412975-WOAc-dAla-c[Asp-His-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 424);Ac-Nle-c[Asp-His-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 425);Ac-Glu-c[Asp-His-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 426);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 427);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 428);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 429);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 430);Ac-dGln-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 431 );Ac-dAsn-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 432);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 433);Ac-Nle-c[dAsp-dNal(2')-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 434);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 435);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 436);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 437);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Docket No. 183B-412975-WOAc-dGln-c[Asp-Ala-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 449);Ac-dGln-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 450);Ac-dGln-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 451 );Ac-dGln-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 452);Ac-dAsn-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 453);Ac-dAsn-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 454);Ac-dAsn-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 455);Ac-dAsn-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 456);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dArg-dPro-NH2(SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.Docket No. 183B-412975-WO

[0084] In some embodiments of the sequence of Formula (I) or (IA), R4is dNal(2’). Accordingly, in some embodiments, the sequence of Formula (I) or (IA) is a sequence of Formula (IA(i)):X1-X2- R1- R2- R3-dNal(2’)- R5-R6- R7-Y1-Y2-Y3-Y4-Y5-Y6-Y7(I A(i)) wherein:X1is absent or norlecuine (Nle);X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, Ala, Gly, Leu, lie, Vai, loc, Tic, Glu, Glu-His, Ala-His, Trp, and Hyp;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(T), Phe, Tyr, dPhe, dTyr, and dNal(T);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen;Docket No. 183B-412975-WO a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then R3is Pro, R4is dNal(2’), R5is Arg, R6is Trp, and R7is Orn or dOrn, when R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated,(iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly,(iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from Arg, dArg, dMet, d He, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, and when R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Glu, and R5is and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Hyp, Pro-His, Phe-Phe, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, He, Vai, and Trp.

[0085] In some embodiments, the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(i)):X1-X2- R1- R2- R3-dNal(2’)- R5-R6- R7-Y1-Y2-Y3-Y4-Y5-Y6-Y7(I A(i)) wherein:X1is absent or norlecuine (Nle);X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;Docket No. 183B-412975-WOR3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, Ala, Gly, Leu, lie, Vai, loc, Tic, Glu, Glu-His, Ala-His, Trp, and Hyp;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then R3is Pro, R4is dNal(2’), R5is Arg, R6is Trp, and R7is Orn or dOrn, when R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a)Docket No. 183B-412975-WOR7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated,(iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly,(iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from Arg, dArg, dMet, d He, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, and when R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Glu, and R5is and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Hyp, Pro-His, Phe-Phe, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, He, Vai, and Trp.

[0086] In some embodiments, the sequence of Formula (I) or (IA) is a sequence of Formula (IA(i)), wherein:X1is absent or norlecuine (Nle);X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, Ala, Gly, Leu, He, Vai, loc, Tic, Glu, Glu-His, Ala-His, Trp, and Hyp;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(T);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Docket No. 183B-412975-WOY4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-Pro-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-Nle-c[Glu-His-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 7);Ac-dGln-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dGln-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 10);Ac-dAsn-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-dAsn-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 14);Ac-Nle-c[Glu-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 16);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Ac-Ala-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 20);Ac-Nle-c[Glu-Oic-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 22);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Docket No. 183B-412975-WOAc-dAla-c[Glu-His-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 28);Ac-Nle-c[Glu-Pro-dNal(2’)-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-His-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 32);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 37);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 38);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Glu-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 42);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 395);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 396);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 397);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 398);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 399);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 400);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 401 );Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Ala-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 404);Ac-Nle-c[dPen-Leu-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 405);Ac-Nle-c[dPen-Gly-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 406);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Docket No. 183B-412975-WOAc-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 414);Ac-Nle-c[Asp-Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 415);Ac-Nle-c[Asp-His-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 416);Ac-dGln-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 417);Ac-dAsn-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 418);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 419);Ac-Ala-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 420);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 421 );Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 422);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 423);Ac-dAla-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 424);Ac-Nle-c[Asp-His-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 425);Ac-Glu-c[Asp-His-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 426);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 427);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAsp-d al-dPro-NH2(SEQ ID NO: 428);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 429);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-l_ys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 430);Ac-dGln-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 431 );Ac-dAsn-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 432);Docket No. 183B-412975-WOAc-Nle-c[Asp-dNal(2’)-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 433);Ac-Nle-c[dAsp-dNal(2')-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 434);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 435);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 436);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 437);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-dGln-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 449);Ac-dGln-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 450);Ac-dGln-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 451 );Ac-dGln-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 452);Ac-dAsn-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 453);Ac-dAsn-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 454);Ac-dAsn-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 455);Ac-dAsn-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 456);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2 (SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dArg-dPro-NH2 (SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2 (SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Asp-dVal-dPro-NH2 (SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2 (SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.

[0087] In some embodiments of the sequence of any one of Formulae (l)-(IA(i)), R3is Pro. In further embodiments, Y5-Y7are absent. Accordingly, in some embodiments, the sequence of any one of Formulae (l)-(IA(i)) is a sequence of Formula (IA(ii)):X1-X2-R1-R2-Pro-dNal(2’)-R5-R6-R7-R8-Y1-Y2-Y3-Y4-Y5(IA(ii)) wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Glu, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;Docket No. 183B-412975-WOR6is selected from the group consisting Trp, Trp-Gly, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y4are absent, provided that: when R2is Glu, then R1is Nle, R5is Arg, R6is Trp, and R7is Orn or dOrn, when R1is Nle, then R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, when R1is Tyr, Gly, or dAla, then X1is absent, and the N-terminus is acetylated, when R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla then either R2is dPen or R6is Trp-Gly, and when R1is dNIe or dPhe, then R2is Asp.Docket No. 183B-412975-WO

[0088] In some embodiments, the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(ii)):X1-X2-R1-R2-Pro-dNal(2’)-R5-R6-R7-R8-Y1-Y2-Y3-Y4-Y5(IA(ii)) wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Glu, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, Trp-Gly, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y4are absent,Docket No. 183B-412975-WO provided that: when R2is Glu, then R1is Nle, R5is Arg, R6is Trp, and R7is Orn or dOrn, when R1is Nle, then R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, when R1is Tyr, Gly, or dAla, then X1is absent, and the N-terminus is acetylated, when R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla then either R2is dPen or R6is Trp-Gly, and when R1is dNIe or dPhe, then R2is Asp.

[0089] In some embodiments, the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(ii)), wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(T), Phe, Tyr, dPhe, dTyr, and dNal(T);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dValandDocket No. 183B-412975-WO the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-Pro-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-dGln-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dAsn-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Ac-Nle-c[Glu-Pro-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Docket No. 183B-412975-WOAc-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-NH2(SEQ ID NO: 460);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dArg-dPro-NH2(SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.

[0090] In some embodiments of the sequence of Formula (I) or (IA), R4is an amino acid other than dNal(2’). In some embodiments, R4is a derivative of dPhe. In further embodiments, R4is selected from the group consisting of p(l)dPhe, p(Br)dPhe, p(CF3)dPhe, and p(CI)dPhe. In still further embodiments, X2and Y5-Y7are absent. Accordingly, in some embodiments, the sequence of Formula (I) or (IA) a sequence of Formula (IB):X1-X2- R1- R2- R3- R4- R5- R6- R7- Y1- Y2- Y3-Y4(IB) wherein:X1is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, Ala, Lys, dLys, His, and dHis;R2is selected from the group consisting of Asp, Glu, and Cys;R3is absent or selected from the group consisting of Pro, His, dHis, His-Arg, Pro-Arg, Phe, Bip, Trp, Tyr, and Gin;R4is selected from the group consisting of p(l)dPhe, p(Br)dPhe, p(CFs)dPhe, and p(CI)dPhe;R5is His or Arg;R6is selected from the group consisting Trp, dNal(2’), Nal(2’), and Tic;R7is selected from the group consisting of Lys, Cys, and Orn;Y1is selected from the group consisting of dVal, dPro, and dTle;Y2is selected from the group consisting of dPro, dVal, and dTle;Y3is absent, dVal, or dPro;Y4is absent or dPro; andDocket No. 183B-412975-WO the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2and R7are both Cys; a lactam bond between R2and R7, when R2is Asp and R7is Lys; and a lactam bond between R2and R7, when R2is Glu, and R7is Orn, provided that: when R2is Glu, then R1is Nle and either (i) R3is Pro, R4is p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn, or (ii) R3is His and R4is p(Br)dPhe, when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, and when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal.

[0091] In some embodiments, the non-naturally occurring melanocortin analog comprises a sequence of Formula (IB):X1-X2- R1- R2- R3- R4- R5- R6- R7- Y1-Y2- Y3-Y4(IB) wherein:X1is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, Ala, Lys, dLys, His, and dHis;R2is selected from the group consisting of Asp, Glu, and Cys;R3is absent or selected from the group consisting of Pro, His, dHis, His-Arg, Pro-Arg, Phe, Bip, Trp, Tyr, and Gin;R4is selected from the group consisting of p(l)dPhe, p(Br)dPhe, p(CFs)dPhe, and p(CI)dPhe;R5is His or Arg;R6is selected from the group consisting Trp, dNal(2’), Nal(2’), and Tic;R7is selected from the group consisting of Lys, Cys, and Orn;Y1is selected from the group consisting of dVal, dPro, and dTle;Y2is selected from the group consisting of dPro, dVal, and dTle;Docket No. 183B-412975-WOY3is absent, dVal, or dPro;Y4is absent or dPro; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2and R7are both Cys; a lactam bond between R2and R7, when R2is Asp and R7is Lys; and a lactam bond between R2and R7, when R2is Glu, and R7is Orn, provided that: when R2is Glu, then R1is Nle and either (i) R3is Pro, R4is p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn, or (ii) R3is His and R4is p(Br)dPhe, when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, and when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal.

[0092] In some embodiments, the non-naturally occurring melanocortin analog comprises a sequence of Formula (IB), wherein:X1is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, Ala, Lys, dLys, His, and dHis;R2is selected from the group consisting of Asp, Glu, and Cys;R3is selected from the group consisting of Pro, His, dHis, His-Arg, Pro-Arg, Phe, Bip, Trp, Tyr, and Gin;R4is selected from the group consisting of p(l)dPhe, p(Br)dPhe, p(CFs)dPhe, and p(CI)dPhe;R5is His or Arg;R6is selected from the group consisting Trp, dNal(2’), Nal(2’), and Tic;R7is selected from the group consisting of Lys, Cys, and Orn;Y1is selected from the group consisting of dVal, dPro, and dTle;Y2is selected from the group consisting of dPro, dVal, and dTle;Docket No. 183B-412975-WOY3is absent, dVal, or dPro;Y4is absent or dPro; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2and R7are both Cys; a lactam bond between R2and R7, when R2is Asp and R7is Lys; and a lactam bond between R2and R7, when R2is Glu, and R7is Orn, provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 3);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 17);Ac-Ala-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 19);Ac-Ala-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 21 );Ac-Nle-c[Glu-Pro-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 31 );Ac-Nle-c[Glu-His-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 33);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 34);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 35);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 247);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 248);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 249);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 250);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 251 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 252);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 253);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 254);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 255);Docket No. 183B-412975-WOAc-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 256);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 257);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 258);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 259);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 260);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 261 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 262);Ac-Arg-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 267);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 274);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 275);Ac-Ala-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 276);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 281 );Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 282);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 286);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 289);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 290);Ac-Nle-c[Asp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 291 );Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 390);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 391 ); andAc-Nle-c[Asp-Bip-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 392), wherein c represents cyclization via a lactam or disulfide bond.

[0093] As will be appreciated by the skilled artisan, non-naturally occurring melanocortin agonists comprising a sequence of any one of Formulae (l)-(IB), have an N- terminus and a C-terminus. The melanocortin agonists of the present technology are written beginning with the N-terminus at the left-most amino acid residue and ending with the C-Docket No. 183B-412975-WO terminus at the right most residue. Accordingly, the N-terminus of a non-naturally melanocortin agonist comprising a sequence of any one of Formulae (l)-(IB) may be at X2, X1, or R1. Analogously, the C-terminus of a non-naturally occurring melanocortin agonist comprising a sequence of any one of Formulae (l)-(IB) may be at any of R7, R8, R9, Y1, Y2, Y3, Y4, Y5, Y6, and Y7.

[0094] In some embodiments, the N-terminus of the non-naturally occurring melanocortin agonist is modified by an acyl group. In some embodiments, the acyl group is acetyl group

[0095] In some embodiments, the N-terminus of the non-naturally occurring melanocortin agonist is not modified.

[0096] In the sequence of any one of Formulae (l)-(IB), Y1Y2Y3Y4Y5Y6Y7represents a C-terminus of the non-naturally occurring melanocortin agonist. In some embodiments, Y1- Y7are absent. In some embodiments, Y1is present and Y2-Y7are absent.

[0097] In some embodiments, Y1and Y2are present and Y3-Y7are absent. In some embodiments, Y3-Y7are absent, and Y1is dVal and Y2is dPro. In some embodiments, Y3- Y7are absent, and Y1is dPro and Y2is dVal. In some embodiments, Y3-Y7are absent, and Y1is dTle and Y2is dPro. In some embodiments, Y1-Y3are present and Y4-Y7are absent. In some embodiments, Y1-Y4are present and Y5-Y7are absent.

[0098] In some embodiments, the C-terminus of the non-naturally occurring melanocortin agonist is modified by an amide groupthe sequence of any one of Formulae (l)-(IB), a non-naturally occurring melanocortin agonist with a C- terminus modified by an amide may be represented by a terminal -NH2.

[0099] In some embodiments, the C-terminus of the non-naturally occurring melanocortin analog is not modified. In the sequence of any one of Formulae (l)-( IB) , a nonDocket No. 183B-412975-WO naturally occurring melanocortin analog with an unmodified C-terminus may be represented by -OH.

[0100] Non-naturally occurring melanocortin analogs comprising a sequence of any one of Formulae (l)-(IB) may be cyclized. For example, the non-naturally occurring melanocortin analog may be cyclized through a moiety selected from the group consisting of: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and a lactam bond between R2and R9, when R2is Asp and R9is Lys.

[0101] In some embodiments, the non-naturally occurring melanocortin analog is cyclized through a lactam bond. In some embodiments, the sequence of any one of Formulae (l)-(IB) is cyclized through a lactam bond between R2and R7.

[0102] In some embodiments of the sequence of any one of Formulae (l)-(IB), R4is dNal(2’). In further embodiments, R1is Nle, R2is Asp or Glu, R3is Pro, R5is Arg, R6is Trp, and R7is Lys, dOrn, or Orn. In some embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 509);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 510);Ac-Nle-c[dAsp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 511 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 473);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 560); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 561 ), wherein c represents cyclization through R2and R7via a lactam bond.Docket No. 183B-412975-WO

[0103] In some embodiments R4is dNal(2’), R2is Glu, R3is Pro-His or His, R5is His, R6is Trp, and R7is Orn. In further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is:Ac-Arg-c[Glu-His-dNal(2')-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 483); orAc-Arg-c[Glu-Pro-His-dNal(2')-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 484), wherein c represents cyclization through R2and R7via a lactam bond.

[0104] Alternatively, in some embodiments of the sequence of any one of Formulae (I)- (IB), R4is p(l)dPhe, p(CI)dPhe, p(Br)dPhe, or p(CF3)dPhe. In further embodiments, R1is Nle, R2is Asp or Glu, R3is Pro or His, R5is Arg, R6is Trp, and R7is Lys, dOrn, or Orn. In some embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-p(l)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 676);Ac-Nle-c[Asp-His-p(l)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 658);Ac-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 672);Ac-Nle-c[Asp-His-p(CF3)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 654);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 674);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 677);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 656);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 651 );Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 652);Ac-Nle-c[Glu-His-p(Br)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 636);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 673); andAc-Nle-c[Asp-Pro-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 668), wherein c represents cyclization through R2and R7via a lactam bond.

[0105] In some embodiments of the sequence of any one of Formulae (l)-(IB), X1and / or X2are absent. Alternatively, in some embodiments, at least one of X1and X2is present. InDocket No. 183B-412975-WO some embodiments, X1is present. In some embodiments, X1and X2is present. In further embodiments, X1is Nle or Phe and X2is absent or Nle. In still further embodiments, R1is Nle or Phe, R4is dNal(2’), Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 476);Ac-Nle-Nle-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 477); andAc-Nle-Phe-Phe-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 478); wherein c represents cyclization through a lactam bond between R2and R7.

[0106] In some embodiments, X1is present and R4is p(Br)dPhe or p(CI)dPhe. In further embodiments, R1is Nle, R3is His, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is:Ac-Nle-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 694); orAc-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 695), wherein c represents cyclization through a lactam bond between R2and R7.

[0107] In some embodiments, R1is Nle. Alternatively, in some embodiments, R1is an amino acid other than Nle. In further embodiments, R1is Arg, dArg, transPro(guan), cisPro(guan), dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, Nva, Gly, dCys, dPhe, dTyr, dGIn, dAsn, dTyr, Tyr, Dmt, dPro, dNIe, or Glu. In further embodiments, R3is Pro and R4is dNal(2’). In still further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(B) is selected from the group consisting of:Ac-Ala-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 479);Ac-cisPro(guan)-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 485);Ac-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 486);Ac-dArg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 457);Ac-dAsn-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 489);Ac-dCys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 490);Docket No. 183B-412975-WOAc-dGln-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 491 );Ac-dlle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 492);Ac-dLeu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 493);Ac-dMet-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 494);Ac-dNle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 495);Ac-dPhe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 496);Ac-dPro-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 497);Ac-dTle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 498);Ac-dTyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 499);Ac-dVal-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 500);Ac-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 502);Ac-Nva-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 503);Ac-Tle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 504);Ac-transPro(guan)-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 505);Dmt-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 506); dTyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 507); andTyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 508), wherein c represents cyclization through a lactam bond between R2and R7.

[0108] Alternatively, in some embodiments, R1is an amino acid other than Nle, R3is His and R4is p(CI)dPhe or p(Br)dPhe. In further embodiments, R1is Ala, Arg, dArg, Lys, dLys, His, or dHis. In still further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(B) is selected from the group consisting of:Ac-Ala-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 641 );Ac-Ala-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 642);Docket No. 183B-412975-WOAc-Arg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 643);Ac-dArg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 644);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 645);Ac-dLys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 646);Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 647); andAc-Lys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 648), wherein c represents cyclization through a lactam bond between R2and R7.

[0109] In still further embodiments, Y1is dTle and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(B) is selected from the group consisting of:Ac-Ala-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 659);Ac-Ala-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 660);Ac-Arg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 661 );Ac-dArg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 662);Ac-dLys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 663); andAc-Lys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 664), wherein c represents cyclization through a lactam bond between R2and R7.

[0110] In some embodiments, R3is Pro or His. Alternatively, in some embodiments, R3is an amino acid other than Pro or His. In further embodiments, R3is absent, transPro(guan), cisPro(guan), Aba, Aia, Ata, Aic, Hyp, Pro-His, Ala, Gly, Leu, He, Vai, Trp, Oic, loc, Tic, Glu, dAla, Ala, Hyp, or Phe. In still further embodiments, R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IA(iii)) is selected from the group consisting of:Ac-Nle-c[Asp-Aba-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 514);Ac-Nle-c[Asp-Aia-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 515);Ac-Nle-c[Asp-Aic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 516);Docket No. 183B-412975-WOAc-Nle-c[Asp-Ala-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 517);Ac-Nle-c[Asp-Ata-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 519);Ac-Nle-c[Asp-cisPro(guan)-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 520);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 522);Ac-Nle-c[Asp-Glu-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 524);Ac-Nle-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 526);Ac-Nle-c[Asp-Hyp-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 527);Ac-Nle-c[Asp-lle-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 529);Ac-Nle-c[Asp-loc-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 530);Ac-Nle-c[Asp-Leu-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 531 );Ac-Nle-c[Asp-Oic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 532);Ac-Nle-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 538);Ac-Nle-c[Asp-transPro(guan)-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 539);Ac-Nle-c[Asp-Trp-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 540); andAc-Nle-c[Asp-Val-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 541 ), wherein c represents cyclization through a lactam bond between R2and R7.

[0111] Alternatively, in some embodiments, R3is an amino acid other than Pro or His, and R4is dPhe, p(F)dPhe, p(CI)dPhe or p(Br)dPhe. In further embodiments, R3is dHis, Oic, Phe, Bip, Trp, Tyr, and Gin. In still further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Oic-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 472);Ac-Nle-c[Asp-Bip-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 678);Ac-Nle-c[Asp-dHis-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 679);Ac-Nle-c[Asp-dHis-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 680);Docket No. 183B-412975-WOAc-Nle-c[Asp-Gln-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 681 );Ac-Nle-c[Asp-Gln-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 682);Ac-Nle-c[Asp-Phe-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 683);Ac-Nle-c[Asp-Phe-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 684);Ac-Nle-c[Asp-Trp-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 686);Ac-Nle-c[Asp-Trp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 687);Ac-Nle-c[Asp-Trp-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 688);Ac-Nle-c[Asp-Tyr-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 689);Ac-Nle-c[Asp-Tyr-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 690); andAc-Nle-c[Asp-Tyr-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 691 ), wherein c represents cyclization through a lactam bond between R2and R7.

[0112] In some embodiments, R3is a dipeptide. In some embodiments, R3is a dipeptide comprising His and / or Pro. In further embodiments, R3is Phe-His, Pro-His, Ala- His, or dAla-His. In still further embodiments, R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dlle-dPro-NH2(SEQ ID NO: 533);Ac-Nle-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dLeu-dPro-NH2(SEQ ID NO: 534);Ac-Nle-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 535);Ac-Nle-c[Asp-Pro-His-dNal(2')-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 536);Ac-Nle-c[Asp-Pro-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 537);Ac-Nle-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 521 );Ac-Arg-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 481 );Ac-dArg-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 488);Ac-Nle-c[Asp-Ala-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 518);Ac-Arg-c[Asp-Ala-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 480);Docket No. 183B-412975-WOAc-dArg-c[Asp-Ala-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 487); andAc-Arg-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-NH2(SEQ ID NO: 482), wherein c represents cyclization through a lactam bond between R2and R7.

[0113] In some embodiments, R5is Arg. Alternatively, in some embodiments, R5is an amino acid other than Arg. In further embodiments, R5is absent, Ala, cisPro(guan), His, Lys, Orn, or transPro(guan). In still further embodiments, R3is Pro or His and R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-His-dNal(2')-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 512);Ac-Nle-c[Asp-His-dNal(2')-transPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 513);Ac-Nle-c[Asp-Pro-dNal(2')-Ala-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 542);Ac-Nle-c[Asp-Pro-dNal(2')-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 543);Ac-Nle-c[Asp-Pro-dNal(2')-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 544);Ac-Nle-c[Asp-Pro-dNal(2')-Lys-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 545);Ac-Nle-c[Asp-Pro-dNal(2')-Orn-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 546);Ac-Nle-c[Asp-Pro-dNal(2')-transPro(guan)-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 547); andAc-Nle-c[Asp-Pro-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 548), wherein c represents cyclization through R2and R7via a lactam bond.

[0114] In some embodiments, R5is an amino acid other than Arg and R4is p(Br)dPhe or p(CI)dPhe. In further embodiments, R5is His. In still further embodiments, R3is His. In some embodiments, the sequence of any one of Formulae (l)-(IB) is:Ac-Nle-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 657); orAc-Nle-c[Asp-His-p(Br)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 653), wherein c represents cyclization through R2and R7via a lactam bond.

[0115] In some embodiments, R6is Trp. Alternatively, in some embodiments, R6is an amino acid other than Trp. In further embodiments, R6is Aba, Aia, Ata, dNal(1 ’), dNal(2’),Docket No. 183B-412975-WO dPhe, dTrp, dTyr, Nal(1 ’), Phe, or Tyr. In still further embodiments, R3is Pro and R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Aba-Lys]-dVal-dPro-NH2(SEQ ID NO: 549);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Aia-Lys]-dVal-dPro-NH2(SEQ ID NO: 550);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Ata-Lys]-dVal-dPro-NH2(SEQ ID NO: 551 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dNal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 552);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 553);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dPhe-Lys]-dVal-dPro-NH2(SEQ ID NO: 554);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 555);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-dTyr-Lys]-dVal-dPro-NH2(SEQ ID NO: 556);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Nal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 557);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Phe-Lys]-dVal-dPro-NH2(SEQ ID NO: 558); andAc-Nle-c[Asp-Pro-dNal(2’)-Arg-Tyr-Lys]-dVal-dPro-NH2(SEQ ID NO: 559), wherein c represents cyclization through R2and R7via a lactam bond.

[0116] In some embodiments, R6is an amino acid other than Trp and R4is dPhe, p(F)dPhe, p(Br)dPhe, p(CF3)dPhe or p(CI)dPhe. In further embodiments, R6is dNal(2’), Nal(2’), Aba, Aia, or Ata. In still further embodiments, R3is His. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-dPhe-Arg-dNal(2’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 635);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 675);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 655);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 637);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 638);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 650);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Aba-Lys]-dVal-dPro-NH2(SEQ ID NO: 669);Ac-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Ata-Lys]-dVal-dPro-NH2 (SEQ ID NO: 670); andAc-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Aia-Lys]-dVal-dPro-NH2(SEQ ID NO: 671 ), wherein c represents cyclization through R2and R7via a lactam bond.

[0117] In some embodiments, R6is an amino acid other than Trp and R4is p(l)dPhe. In further embodiments, R6is Tic. In still further embodiments, R3is Pro-Arg or His-Arg. In some embodiments, the sequence of any one of Formulae (l)-(IB) is:Ac-Nle-c[Asp-His-Arg-p(l)dPhe-Arg-Tic-Lys]-dVal-dPro-NH2 (SEQ ID NO: 649); orAc-Nle-c[Asp-Pro-Arg-p(l)dPhe-Arg-Tic-Lys]-dVal-dPro-NH2 (SEQ ID NO: 685), wherein c represents cyclization through R2and R7via a lactam bond.

[0118] In some embodiments, R6is a dipeptide. In further embodiments, R6is a dipeptide comprising Trp. In some embodiments, R6is Trp-Gly or Trp-Pro. In further embodiments, R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Hyp-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 528);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 563);Ac-Nle-c[Asp-Glu-dNal(2')-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 523);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 562);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-dl_ys-dAsp-NH2 (SEQ ID NO: 564);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 565);Ac-Glu-c[Asp-Pro-dNal(2’)-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 501 ); andAc-Nle-c[Asp-Glu-His-dNal(2')-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 525), wherein c represents cyclization through R2and R7via a lactam bond.

[0119] In some embodiments, embodiments of the sequence of any one of Formulae (l)-(IB), Y1is dVal and Y2is dPro. Alternatively, in some embodiments, Y1is an amino acidDocket No. 183B-412975-WO other than dVal and / or Y2is an amino acid other than dPro. In some embodiments, Y1is dVal and Y2is an amino acid other than dPro. In some embodiments, Y1is an amino acid other than dVal and Y2is dPro. In some embodiments, Y1is an amino acid other than dVal and Y2is an amino acid other than dPro.

[0120] In some embodiments, Y1is dVal, Y2is dPro, and the C-terminus is modified by NH2. In some embodiments, Y1is an amino acid other than dVal, Y2is an amino acid other than dPro, and the C-terminus is modified by NH2. In some embodiments, Y1is dVal, Y2is an amino acid other than dPro, and the C-terminus is modified by NH2. In some embodiments, Y1is an amino acid other than dVal, Y2is dPro, and the C-terminus is modified by NH2. In some embodiments, Y1is dVal, Y2is dPro, and the C-terminus is unmodified.

[0121] In embodiments of any one of Formulae (l)-(IB) when Y1is an amino acid other than dVal, then Y1is selected from Ala, Arg, Asn, Asp, dAla, dArg, dAsn, dAsp, dHyp, dLys, dPro, dTle, dVal, Gly, Hyp, Lys, Pro, Trp, and Vai. In embodiments of any one of Formulae (l)-(IB) when Y2is an amino acid other than dPro, then Y2is selected from Pro, Vai, dAla, dVal, dTle, Arg, Asn, Asp, dArg, dAsn, dAsp, dHyp, Hyp, and Gly.

[0122] Inclusion of one or more C-terminal residues, e.g., Y1-Y7, in the non-naturally occurring melanocortin analog of the present technology may enhance transport across the epithelium, the blood-brain barrier, and or the gastrointestinal tract. For example, peptides comprising a C-terminus of dVal-dPro may have enhanced transport across the blood-brain barrier, relative to the same peptide without the dVal-dPro terminus. Accordingly, various C- terminal residue combinations provide enhanced deliverability and bioavailability of the present melanocortin analogs. In some embodiments, the C-terminus is dVal-dPro. Alternatively, in some embodiments, the C-terminus is not dVal-dPro. In further embodiments, R1is Nle, R2is Asp, R5is Arg, R6is Trp, R7is Lys. In still further embodiments, R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dVal-OH (SEQ ID NO: 474);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Ala-Ala-NH2(SEQ ID NO: 566);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Ala-NH2(SEQ ID NO: 567);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-dPro-dVal-NH2(SEQ ID NO: 568);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-dPro-NH2 (SEQ ID NO: 569);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 570);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-Pro-Val-NH2(SEQ ID NO: 571 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-Val-Pro-NH2(SEQ ID NO: 572);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asn-dPro-NH2(SEQ ID NO: 573);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asn-NH2(SEQ ID NO: 574);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-dPro-NH2(SEQ ID NO: 575);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-NH2(SEQ ID NO: 576);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAla-NH2(SEQ ID NO: 577);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-NH2(SEQ ID NO: 578);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dArg-dPro-dVal-NH2(SEQ ID NO: 579);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 580);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 581 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsn-dPro-NH2(SEQ ID NO: 582);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAsn-NH2(SEQ ID NO: 583);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dPro-NH2(SEQ ID NO: 584);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAsp-NH2(SEQ ID NO: 585);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dHyp-dVal-NH2(SEQ ID NO: 586);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dHyp-NH2(SEQ ID NO: 587);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dHyp-Val-NH2(SEQ ID NO: 588);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dLys-dPro-dVal-NH2(SEQ ID NO: 589);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dLys-dPro-NH2(SEQ ID NO: 590);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dPro-dPro-dLys-dAsp-NH2(SEQ ID NO: 591 );Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dPro-NH2(SEQ ID NO: 592);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dTle-NH2(SEQ ID NO: 593);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-NH2(SEQ ID NO: 594);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 595);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dTle-dPro-NH2(SEQ ID NO: 596);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 597);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dTle-NH2(SEQ ID NO: 598);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dVal-NH2(SEQ ID NO: 599);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-Arg-NH2(SEQ ID NO: 600);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-Asn-NH2(SEQ ID NO: 601 );Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-Asp-NH2(SEQ ID NO: 602);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dArg-NH2(SEQ ID NO: 603);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dAsn-NH2(SEQ ID NO: 604);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dAsp-NH2(SEQ ID NO: 605);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 606);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dTle-NH2(SEQ ID NO: 607);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dVal-NH2(SEQ ID NO: 608);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 609);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 610);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-NH2(SEQ ID NO: 61 1 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Hyp-dVal-NH2(SEQ ID NO: 612);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Hyp-NH2(SEQ ID NO: 613);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Hyp-Val-NH2(SEQ ID NO: 614);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-dPro-dVal-NH2(SEQ ID NO: 615);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-dPro-NH2 (SEQ ID NO: 616);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-Pro-Val-NH2(SEQ ID NO: 617);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-Val-Pro-NH2 (SEQ ID NO: 618);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Pro-NH2 (SEQ ID NO: 619);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Trp-NH2(SEQ ID NO: 620);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Val-dHyp-NH2(SEQ ID NO: 621 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Val-Hyp-NH2(SEQ ID NO: 622);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Val-NH2(SEQ ID NO: 623);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Val-Pro-NH2(SEQ ID NO: 624)Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-dVal-dPro-NH2(SEQ ID NO: 625);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dPro-NH2(SEQ ID NO: 626);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 627);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 628);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-dVal-dPro-NH2(SEQ ID NO: 629);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dArg-dVal-dPro-NH2(SEQ ID NO: 630);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dLys-dVal-dPro-NH2(SEQ ID NO: 631 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 632);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dTle-dVal-dPro-NH2(SEQ ID NO: 633); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-dVal-dPro-NH2(SEQ ID NO: 634), wherein c represents cyclization through R2and R7via a lactam bond.

[0123] Alternatively, in some embodiments, the C-terminus is not dVal-dPro and R4is p(CI)dPhe or p(Br)dPhe. In further embodiments, R1is Nle, R2is Asp, R5is Arg, R6is Trp, R7is Lys. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 666);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 667);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 639);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 640);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 665);Ac-Nle-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 692); andAc-Nle-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 693), wherein c represents cyclization through R2and R7via a lactam bond.

[0124] In some embodiments, the sequence of any one of Formulae (l)-(IB) is cyclized through a lactam bond between R2and R9. In further embodiments, R4is Pro and R6is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(IB) is: Ac-Nle- c[Asp-Phe-Phe-Pro-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 696), wherein c represents cyclization through a lactam bond between R2and R9.

[0125] In some embodiments, the non-naturally occurring melanocortin analog is cyclized through a disulfide bond. In some embodiments, the sequence of any one of Formulae (l)-(IB) is cyclized through a disulfide bond between R2and R7.

[0126] In some embodiments, R4is dNal(2’). In further embodiments, R1is Nle,R3is Pro, R5is Arg, and R6is Trp. In still further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 708);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 709);Ac-Nle-c[dCys-Pro-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 710);Ac-Nle-c[dCys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 711 );Ac-Nle-c[dCys-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 712);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 713);Docket No. 183B-412975-WOAc-Nle-c[Pen-Pro-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 714); andAc-Nle-c[Pen-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 715), wherein c represents cyclization through a disulfide bond between R2and R7.

[0127] Alternatively, in some embodiments, R4is selected from p(Br)dPhe, p(CI)dPhe, and p(F)dPhe. In further embodiments, R1is Nle, R3is His or Pro, R5is Arg, and R6is Trp. In still further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Cys-His-p(Br)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 716);Ac-Nle-c[Cys-His-p(CI)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 717); andAc-Nle-c[Cys-Pro-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 718), wherein c represents cyclization through a disulfide bond between R2and R7.

[0128] In some embodiments, R1is Nle. Alternatively, in some embodiments, R1is an amino acid other than Nle. In further embodiments, R1is selected from Arg, dArg, Ala, His, dHis, Lys, dLys, dLeu, and dTyr. In further embodiments, R3is Pro and R4is dNal(2’). In still further embodiments, Y1is dVal and Y2is dPro. In some embodiments, the sequence of any one of Formulae (l)-(B) is selected from the group consisting of:Ac-Ala-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 697);Ac-Arg-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 700);Ac-dArg-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 701 );Ac-dHis-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 702);Ac-dLeu-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 703);Ac-dLys-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 704);Ac-dTyr-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 705);Ac-His-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 706); andAc-Lys-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 707), wherein c represents cyclization through a disulfide bond between R2and R7.Docket No. 183B-412975-WO

[0129] In some embodiments, R3is His or Pro. Alternatively, in some embodiments, R3is a dipeptide. In further embodiments, R3is dAla-His. In still further embodiments, R4is dNal(2’). In some embodiments, the sequence of any one of Formulae (l)-(B):Ac-Arg-c[Cys-dAla-His-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2 (SEQ ID NO: 698); orAc-Arg-c[Cys-dAla-His-dNal(2')-Arg-Trp-Cys]-NH2(SEQ ID NO: 699), wherein c represents cyclization through a disulfide bond between R2and R7.

[0130] In some embodiments, the melanocortin analog is linear. In some embodiments, the sequence of any one of Formulae (l)-(IB) is:Ac-Nle-Asp-Pro-dNal(2')-Arg-Trp-dVal-dPro-NH2(SEQ ID NO: 719); orAc-Nle-Asp-Pro-dNal(2')-Arg-Trp-Lys-dVal-dPro-NH2(SEQ ID NO: 720).

[0131] In some embodiments, the non-naturally occurring melanocortin agonist comprises a sequence of any one of SEQ ID NOs: 457, 472-474, and 476-720.

[0132] In some embodiments, the non-naturally occurring melanocortin antagonist analog is in the form of a salt. In further embodiments, the non-naturally occurring melanocortin antagonist analog is in the form of an acetate salt. In still further embodiments, the non-naturally occurring melanocortin antagonist analog is in the form of an acetate salt and comprises a sequence of any one of Formulae (l)-(IB). In yet further embodiments, the non-naturally occurring melanocortin antagonist analog is in the form of an acetate salt and comprises a sequence of any one of the sequences provided above.

[0133] The non-naturally occurring melanocortin antagonist analog may be present in the pharmaceutical composition or formulation in an amount of about 5 mg / mL to about 200 mg / mL. In some embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 5 mg / mL to about 150 mg / mL, about 5 mg / mL to about 130 mg / mL, about 5 mg / mL to about 100 mg / mL, about 5 mg / mL to about 70 mg / mL or about 5 mg / mL to about 50 mg / mL. In some embodiments, the non- naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 10 mg / mL to about 150 mg / mL, about 10 mg / mL to about 130 mg / mL, about 10 mg / mL to about 100 mg / mL, about 10 mg / mL to about 70 mg / mL or about 10 mg / mL toDocket No. 183B-412975-WO about 50 mg / mL. In some embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 10 mg / mL to about 130 mg / mL. In some embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 10 mg / mL to about 50 mg / mL.

[0134] In some embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 10 mg / mL, about 12.5 mg / mL, about 15 mg / mL, about 20 mg / mL, about 25 mg / mL, about 30 mg / mL, about 35 mg / mL, about 40 mg / mL, about 45 mg / mL, or about 50 mg / mL. In some embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 12.5 mg / mL. In other embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 25 mg / mL. In still other embodiments, the non-naturally occurring melanocortin analog is present in the pharmaceutical composition in an amount of about 50 mg / mL.

[0135] Pharmaceutically acceptable carriers and / or excipients included in the pharmaceutical compositions and formulations of the present technology may be selected based on the carrier or excipient’s ability to confer desirable properties, such as reduced or lack of delivery site reactions, solubility, stability, pH, buffering, pharmacokinetics, bioavailability, and the like, to the pharmaceutical composition or formulation. For example, the one or more pharmaceutically acceptable carriers and / or excipients of the pharmaceutical compositions and formulations described herein may include a buffer, an osmolyte, and a pH adjusting agent.

[0136] The pharmaceutical compositions and formulations of the present technology include a buffer. The buffer may be an organic buffer, i.e., a buffer that does not comprise or chelate a metal cation. In some embodiments, the buffer comprises one or more of histidine, Tris, arginine, MES, ADA, PIPES, ACES, MOPSO, MOPS, Bes, TES, HEPES, DIPSO, TAPSO, POPSO, HEPPSO, HEPPS, TPAS, acetoamidoglycine, glycinamide, glycylglycine, tricine, and bicine. In some embodiments, the buffer comprises histidine.

[0137] Alternatively, the buffer may be an inorganic buffer, i.e., a buffer that comprises or chelates a metal ion. In some embodiments, the buffer comprises an acetate. In further embodiments, the buffer comprises sodium acetate. A sodium acetate buffer may beDocket No. 183B-412975-WO included in the pharmaceutical compositions and formulations described herein as anhydrous sodium acetate or a sodium acetate hydrate.

[0138] The buffer may be present in the pharmaceutical composition or formulation at a concentration of about 5 mM to about 150 mM. In some embodiments, the buffer is present in the pharmaceutical composition or formulation at a concentration of about 10 mM to about 100 mM, about 10 mM to about 90 mM, about 10 mM to about 80 mM, about 10 mM to about 70 mM, about 10 mM to about 6 mM, about 10 mM to about 50 mM, or about 10 mM to about 40 mM. In some embodiments, the buffer is present in the pharmaceutical composition or formulation at a concentration of about 15 mM to about 150 mM, about 15 mM to about 100 mM, about 15 mM to about 90 mM, about 15 mM to about 80 mM, about 15 mM to about 70 mM, about 15 mM to about 6 mM, about 15 mM to about 50 mM, or about 15 mM to about 40 mM. In some embodiments, the buffer may be present in the pharmaceutical composition or formulation at a concentration of about 25 mM.

[0139] In some embodiments, the buffer comprises histidine and the histidine is present in the pharmaceutical composition or formulation at a concentration of about 15 mM to about 150 mM. In some embodiments, the histidine is present in the pharmaceutical composition or formulation at a concentration of about 10 mM to about 100 mM, about 10 mM to about 90 mM, about 10 mM to about 80 mM, about 10 mM to about 70 mM, about 10 mM to about 6 mM, about 10 mM to about 50 mM, or about 10 mM to about 40 mM. In some embodiments, the histidine is present in the pharmaceutical composition or formulation at a concentration of about 15 mM to about 150 mM, about 15 mM to about 100 mM, about 15 mM to about 90 mM, about 15 mM to about 80 mM, about 15 mM to about 70 mM, about 15 mM to about 6 mM, about 15 mM to about 50 mM, or about 15 mM to about 40 mM. In some embodiments, the histidine is present in the pharmaceutical composition or formulation at a concentration of about 25 mM.

[0140] In some embodiments, the buffer comprises sodium acetate and the sodium acetate is present in the pharmaceutical composition or formulation at a concentration of about 15 mM to about 150 mM. In some embodiments, the sodium acetate is present in the pharmaceutical composition or formulation at a concentration of about 10 mM to about 100 mM, about 10 mM to about 90 mM, about 10 mM to about 80 mM, about 10 mM to about 70Docket No. 183B-412975-WO mM, about 10 mM to about 6 mM, about 10 mM to about 50 mM, or about 10 mM to about 40 mM. In some embodiments, the sodium acetate is present in the pharmaceutical composition or formulation at a concentration of about 15 mM to about 150 mM, about 15 mM to about 100 mM, about 15 mM to about 90 mM, about 15 mM to about 80 mM, about 15 mM to about 70 mM, about 15 mM to about 6 mM, about 15 mM to about 50 mM, or about 15 mM to about 40 mM. In some embodiments, the sodium acetate is present in the pharmaceutical composition or formulation at a concentration of about 25 mM.

[0141] A buffer may be included to maintain a certain pH range of the pharmaceutical composition or formulation. For example, the pharmaceutical compositions and formulations of the present technology may include a buffer to maintain a pH range that is acceptable for physiological use and that maintains dissolution of the non-naturally occurring melanocortin analog in the composition or formulation. Such pH range may be from about 4.0 to about 7.0. Accordingly, the pharmaceutical composition or formulation has a pH of about 4.0 to about 7.0. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.0 to about 6.5. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.0 to about 6.0. In some embodiments, pharmaceutical composition or formulation has a pH of about 4.0 to about 5.5. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.0 to about 5.0. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.5 to about 7.0. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.5 to about 6.5. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.5 to about 6.0. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.5 to about 5.5. In some embodiments, the pharmaceutical composition or formulation has a pH of about 5.0 to about 7.0. In some embodiments, the pharmaceutical composition or formulation has a pH of about 5.0 to about 6.5.

[0142] In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.0 to about 4.5, about 4.2 to about 4.7, about 4.4 to about 4.9, about, about 4.6 to about 5.1 , about 4.8 to about 5.3, or about 5.0 to about 5.5. In some embodiments, the pharmaceutical composition or formulation has a pH of about 5.0 to about 5.5, about 5.2 to about 5.7, about 5.4 to about 5.9, about, about 5.6 to about 6.1 , about 5.8 to about 6.3, orDocket No. 183B-412975-WO about 6.0 to about 6.5. In some embodiments, the pharmaceutical composition or formulation has a pH of about 4.9. In some embodiments, the pharmaceutical composition or formulation has a pH of about 5.3. In some embodiments, the pharmaceutical composition or formulation has a pH of about 6.3.

[0143] The pharmaceutical compositions and formulations of the present technology include an osmolyte. The osmolyte may be a sugar or derivative thereof, glycerol, glycerin, a gelatin, a propylene glycol, a propylparaben, PVP, PLGA, or PEG. In some embodiments, the osmolyte is a sugar or derivative thereof such as, for example, a sugar alcohol. Nonlimiting examples of sugar alcohols include sorbitol, mannitol, erythritol, threitol, lactitol, maltitol, glycerol, xylitol, and cellulose. In some embodiments, the osmolyte is mannitol.

[0144] The osmolyte may be present in the pharmaceutical composition or formulation in an amount of about 5 mg / mL to about 100 mg / mL. In some embodiments, the osmolyte is present in the pharmaceutical composition or formulation in an amount of about 10 mg / mL to about 100 mg / mL, about 10 mg / mL to about 90 mg / mL, about 10 mg / mL to about 80 mg / mL, about 10 mg / mL to about 70 mg / mL about 10 mg / mL to about 60 mg / mL, about 10 mg / mL to about 50 mg / mL, or about mg / mL to about 40 mg / mL. In some embodiments, the osmolyte is present in the pharmaceutical composition or formulation in an amount of about 15 mg / mL to about 50 mg / mL, about 10 mg / mL to about 45 mg / mL, about 15 mg / mL to about 45 mg / mL, about 15 mg / mL to about 40 mg / mL about 20 mg / mL to about 50 mg / mL, about 20 mg / mL to about 45 mg / mL, or about 20 mg / mL to about 40 mg / mL.

[0145] In some embodiments, the osmolyte is present in the pharmaceutical composition or formulations in an amount of about 10 mg / mL, about 15 mg / mL, about 20 mg / mL, about 25 mg / mL, about 27.5 mg / mL, about 30 mg / mL, about 32.5 mg / mL, about 35 mg / mL, about 37.5 mg / mL, about 40 mg / mL, about 45 mg / mL, or about 50 mg / mL. In some embodiments, the osmolyte is present in the pharmaceutical composition or formulation in an amount of about 25 mg / mL. In other embodiments, the osmolyte is present in the pharmaceutical composition or formulation in an amount of about 27.5 mg / mL. In still other embodiments, the osmolyte is present in the pharmaceutical composition or formulation in an amount of about 35 mg / mL. In yet other embodiments, the osmolyte is present in the pharmaceutical composition or formulation in an amount of about 37.5 mg / mL.Docket No. 183B-412975-WO

[0146] In some embodiments, the osmolyte is mannitol and the mannitol is present in the pharmaceutical composition or formulation in an amount of about 10 mg / mL to about 100 mg / mL, about 10 mg / mL to about 90 mg / mL, about 10 mg / mL to about 80 mg / mL, about 10 mg / mL to about 70 mg / mL about 10 mg / mL to about 60 mg / mL, about 10 mg / mL to about 50 mg / mL, or about 10 mg / mL to about 40 mg / mL. In some embodiments, the mannitol is present in the pharmaceutical composition or formulation in an amount of about 15 mg / mL to about 50 mg / mL, about 10 mg / mL to about 45 mg / mL, about 15 mg / mL to about 45 mg / mL, about 15 mg / mL to about 40 mg / mL about 20 mg / mL to about 50 mg / mL, about 20 mg / mL to about 45 mg / mL, or about 20 mg / mL to about 40 mg / mL.

[0147] In some embodiments, the osmolyte is mannitol and the mannitol is present in the pharmaceutical composition or formulations in an amount of about 10 mg / mL, about 15 mg / mL, about 20 mg / mL, about 25 mg / mL, about 27.5 mg / mL, about 30 mg / mL, about 32.5 mg / mL, about 35 mg / mL, about 37.5 mg / mL, about 40 mg / mL, about 45 mg / mL, or about 50 mg / mL. In some embodiments, the mannitol is present in the pharmaceutical composition or formulation in an amount of about 25 mg / mL. In other embodiments, the osmolyte is mannitol and the mannitol is present in the pharmaceutical composition or formulation in an amount of about 27.5 mg / mL. In still other embodiments, the mannitol is present in the pharmaceutical composition or formulation in an amount of about 35 mg / mL. In yet other embodiments, the mannitol is present in the pharmaceutical composition or formulation in an amount of about 37.5 mg / mL.

[0148] An osmolyte may be included in the pharmaceutical composition or formulation to achieve a certain osmolality. For example, the pharmaceutical compositions and formulations of the present technology may include an osmolyte to achieve an isotonic or hypertonic solution to minimize injection site pain and cellular damage. An isotonic solution may have an osmolality of about 250 mOsm / kg to about 350 mOsm / kg and a hypertonic solution may have an osmolality of about 350 mOsm / kg to about 600 mOsm / kg. Accordingly, in some embodiments, the osmolyte is included in the pharmaceutical composition or formulation to achieve an osmolality of about 250 mOsm / kg to about 600 mOsm / kg. In some embodiments, the osmolyte is included in the pharmaceutical composition or formulation to achieve an osmolality of about 280 mOsm / kg to about 560 m / Osm, about 280 mOsm / kg toDocket No. 183B-412975-WO about 520 m / Osm, about 280 mOsm / kg to about 500 mOsm, about 280 mOsm / kg to about 460 m / Osm, about 280 mOsm / kg to about 420 m / Osm, about 280 mOsm / kg to about 400 mOsm, about 280 mOsm / kg to about 360 m / Osm, or about 280 mOsm / kg to about 320 m / Osm.

[0149] In some embodiments, the pharmaceutical composition or formulation is isotonic. In further embodiments, the osmolality of the pharmaceutical composition of formulation is about 250 mOsm / kg to about 350 mOsm / kg. In some embodiments, the osmolality of the pharmaceutical composition or formulation is about 260 mOsm / kg to about 330 mOsm / kg, about 270 mOsm / kg to about 310 mOsm / kg, about 275 mOsm / kg to about 300 mOsm / kg, or about 280 mOsm / kg to about 290 mOsm / kg. In some embodiments, the osmolality of the pharmaceutical composition or formulation is about 280 mOsm / kg, 281 mOsm / kg, 282 mOsm / kg, 283 mOsm / kg, 284 mOsm / kg, 286 mOsm / kg, 287 mOsm / kg, 288 mOsm / kg, 289 mOsm / kg, or 290 mOsm / kg.

[0150] In some embodiments, the pharmaceutical composition or formulation is hypertonic. In further embodiments, the osmolality of the pharmaceutical composition of formulation is about 350 mOsm / kg to about 600 mOsm / kg. In some embodiments, the osmolality of the pharmaceutical composition or formulation is about 360 mOsm / kg to about 550 mOsm / kg, about 365 mOsm / kg to about 530 mOsm / kg, about 370 mOsm / kg to about 510 mOsm / kg, about 375 mOsm / kg to about 500 mOsm / kg, about 380 mOsm / kg to about 490 mOsm / kg, about 385 mOsm / kg to about 470 mOsm / kg, or about 390 mOsm / kg to about 450 mOsm / kg. In some embodiments, the osmolality of the pharmaceutical composition or formulation is about 400 mOsm / kg to about 600 mOsm / kg, about 420 mOsm / kg to about 580 mOsm / kg, about 440 mOsm / kg to about 560 mOsm / kg, about 460 mOsm / kg to about 540 mOsm / kg, or about 480 mOsm / kg to about 520 mOsm / kg.

[0151] The pharmaceutical compositions and formulations of the present technology include a pH adjusting agent. The pH adjusting agent may be an acid or a base. For example, if the pH of the pharmaceutical composition or formulation is too basic before addition of the pH adjusting agent, then the pH adjusting agent may be an acid. On the other hand, if the pH of the pharmaceutical composition or formulation is too acidic before addition of the pH adjusting agent, then the pH adjusting agent may be a base.Docket No. 183B-412975-WO

[0152] The pH adjusting agent may be present in the pharmaceutical composition or formulation in an amount of about 0.1 mg / mL to about 10 mg / mL. In some embodiments, the pH adjusting agent is present in the pharmaceutical composition or formulation in an amount of about 0.1 mg / mL to about 9.0 mg / mL, about 0.1 mg / mL to about 8.0 mg / mL, about 0.1 mg / mL to about 7.0 mg / mL, about 0.1 mg / mL to about 6.0 mg / mL, about 0.1 mg / mL to about 5.0 mg / mL, about 0.1 mg / mL to about 4.0 mg / mL, about 0.1 mg / mL to about 3.0 mg / mL, or about 0.1 mg / mL to about 2.0 mg / mL. In some embodiments, the pH adjusting agent is present in the pharmaceutical composition or formulation in an amount of about 1 .0 mg / mL to about 10 mg / mL, about 0.5 mg / mL to about 10 mg / mL, about 0.2 mg / mL to about 10 mg / mL, about 1.0 mg / mL to about 5.0 mg / mL, 0.5 mg / mL to about 5.0 mg / mL, or about 02. mg / mL to about 5 mg / mL.

[0153] When the non-naturally occurring melanocortin analog is in the form of an acetate salt, the ratio of acetate to analog may be 1 :1. Alternatively, the ratio of acetate to analog may not be 1 :1 , i.e., the ratio of acetate to analog may be less than or greater than 1 :1 . Accordingly, when a melanocortin analog acetate salt has a high ratio of acetate to analog, the pharmaceutical composition may be highly acidic and may require a greater amount of the pH adjusting agent. Alternatively, when a melanocortin analog acetate salt has a low ratio of acetate to analog, the pharmaceutical composition may be less acidic and may require a lower amount of the pH adjusting agent.

[0154] In some embodiments, the pH adjusting agent is present in the pharmaceutical composition in ana amount of about 0.1 mg / mL to about 2.0 mg / mL. In some embodiments, the pH adjusting agent is present in the pharmaceutical composition or formulation in an amount of about 0.1 mg / mL to about 1 .8 mg / mL, about 0.1 mg / mL to about 1 .6 mg / mL, about 0.1 mg / mL to about 1 .5 mg / mL, about 0.2 mg / mL to about 1 .8 mg / mL, about 0.2 mg / mL to about 1 .6 mg / mL, or about 0.2 mg / mL to about 1 .5 mg / mL. In some embodiments, the pH adjusting agent is present in the pharmaceutical composition or formulation in an amount of about 0.2 mg / mL to about 1.4 mg / mL, about 0.4 mg / mL to about 1.2 mg / mL, about 0.4 mg / mL to about 1 .0 mg / mL, about 0.4 mg / mL to about 0.8 mg / mL, about 0.4 mg / mL to about 0.6 mg / mL, about 0.8 mg / mL to about 1 .4 mg / mL about 0.9 mg / mL to about 1 .3 mg / mL, or about 1.0 mg / mL to about 1.2 mg / mL. In some embodiments, the pH adjusting agent isDocket No. 183B-412975-WO present in the pharmaceutical composition or formulation in an amount of about 0.2 mg / mL, about 0.4 mg / mL, about 0.5 mg / mL, about 0.6 mg / mL, about 0.7 mg / mL, about 0.8 mg / mL, about 0.9 mg / mL, about 1 .0 mg / mL, about 1 .1 mg / mL, about 1 .2 mg / mL, or about 1 .4 mg / mL.

[0155] In some embodiments, the pH adjusting agent is present in the pharmaceutical composition in an amount of about 1.0 mg / mL to about 5.0 mg / mL. In some embodiments, the pH adjusting agent is present in the pharmaceutical composition or formulation in an amount of about 1 .0 mg / mL to about 4.5 mg / mL, about 1 .5 mg / mL to about 4.0 mg / mL, about 2.0 mg / mL to about 3.5 mg / mL, or about 2.5 mg / mL to about 3.0 mg / mL. In some embodiments, the pH adjusting agent is present in the pharmaceutical composition or formulation in an amount of about about 1 .0 mg / mL to about 1 .5 mg / mL, about 1 .0 mg / mL to about 3.0 mg / mL, about 1.0 mg / mL to about 5.0 mg / mL about 1.0 mg / mL to about 2.5 mg / mL, or about 2.5 mg / mL to about 5.0 mg / mL.

[0156] In some embodiments, the pH adjusting agent is a base. Non-limiting examples of bases include sodium hydroxide, potassium hydroxide, ammonium hydroxide ammonium carbonate, sodium bicarbonate, sodium carbonate, and sodium borate. In some embodiments, the base is sodium hydroxide.

[0157] In some embodiments, the pH adjusting agent is sodium hydroxide and the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 0.1 mg / mL to about 10 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 0.1 mg / mL to about 9.0 mg / mL, about 0.1 mg / mL to about 8.0 mg / mL, about 0.1 mg / mL to about 7.0 mg / mL, about 0.1 mg / mL to about 6.0 mg / mL, about 0.1 mg / mL to about 5.0 mg / mL, about 0.1 mg / mL to about 4.0 mg / mL, about 0.1 mg / mL to about 3.0 mg / mL, or about 0.1 mg / mL to about 2.0 mg / mL.. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 1.0 mg / mL to about 10 mg / mL, about 0.5 mg / mL to about 10 mg / mL, about 0.2 mg / mL to about 10 mg / mL, about 1 .0 mg / mL to about 5.0 mg / mL, 0.5 mg / mL to about 5.0 mg / mL, or about 02. mg / mL to about 5 mg / mL.

[0158] In some embodiments, the sodium hydroxide is present in an amount of about 0.1 mg / mL to about 2.0 mg / mL, 0.1 mg / mL to about 1 .8 mg / mL, about 0.1 mg / mL to aboutDocket No. 183B-412975-WO1.6 mg / mL, about 0.1 mg / mL to about 1.5 mg / mL, about 0.2 mg / mL to about 1.8 mg / mL, about 0.2 mg / mL to about 1.6 mg / mL, or about 0.2 mg / mL to about 1.5 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 0.2 mg / mL to about 1 .4 mg / mL, about 0.4 mg / mL to about 1.2 mg / mL, about 0.4 mg / mL to about 1.0 mg / mL, about 0.4 mg / mL to about 0.8 mg / mL, about 0.4 mg / mL to about 0.6 mg / mL, about 0.8 mg / mL to about 1 .4 mg / mL about 0.9 mg / mL to about 1.3 mg / mL, or about 1.0 mg / mL to about 1.2 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 0.2 mg / mL, about 0.4 mg / mL, about 0.5 mg / mL, about 0.6 mg / mL, about 0.7 mg / mL, about 0.8 mg / mL, about 0.9 mg / mL, about 1 .0 mg / mL, about 1 .1 mg / mL, about 1 .2 mg / mL, or about 1 .4 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 0.4 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 0.5 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 1 .2 mg / mL.

[0159] In some embodiments, the sodium hydroxide is present in the pharmaceutical composition in an amount of about 1.0 mg / mL to about 5.0 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about 1 .0 mg / mL to about 4.5 mg / mL, about 1 .5 mg / mL to about 4.0 mg / mL, about 2.0 mg / mL to about 3.5 mg / mL, or about 2.5 mg / mL to about 3.0 mg / mL. In some embodiments, the sodium hydroxide is present in the pharmaceutical composition or formulation in an amount of about about 1 .0 mg / mL to about 1 .5 mg / mL, about 1 .0 mg / mL to about 3.0 mg / mL, about 1.0 mg / mL to about 5.0 mg / mL about 1.0 mg / mL to about 2.5 mg / mL, or about 2.5 mg / mL to about 5.0 mg / mL.

[0160] In some embodiments, the pH adjusting agent is an acid. Non-limiting examples of acids include acetic acid, citric acid, fumaric acid, hydrochloric acid, and nitric acid. In some embodiments, the acid is acetic acid, such as glacial acetic acid.

[0161] In some embodiments, the pH adjusting agent is glacial acetic acid and the glacial acetic acid is present in the pharmaceutical composition or formulation in an amountDocket No. 183B-412975-WO of about 0.1 mg / mL to about 5.0 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about 0.1 mg / mL to about 9.0 mg / mL, about 0.1 mg / mL to about 8.0 mg / mL, about 0.1 mg / mL to about 7.0 mg / mL, about 0.1 mg / mL to about 6.0 mg / mL, about 0.1 mg / mL to about 5.0 mg / mL, about 0.1 mg / mL to about 4.0 mg / mL, about 0.1 mg / mL to about 3.0 mg / mL, or about 0.1 mg / mL to about 2.0 mg / mL.. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about 1.0 mg / mL to about 10 mg / mL, about 0.5 mg / mL to about 10 mg / mL, about 0.2 mg / mL to about 10 mg / mL, about 1 .0 mg / mL to about 5.0 mg / mL, 0.5 mg / mL to about 5.0 mg / mL, or about 02. mg / mL to about 5 mg / mL..

[0162] In some embodiments, the glacial acetic acid is present in an amount of about 0.1 mg / mL to about 2.0 mg / mL, 0.1 mg / mL to about 1 .8 mg / mL, about 0.1 mg / mL to about 1.6 mg / mL, about 0.1 mg / mL to about 1.5 mg / mL, about 0.2 mg / mL to about 1.8 mg / mL, about 0.2 mg / mL to about 1.6 mg / mL, or about 0.2 mg / mL to about 1.5 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about 0.2 mg / mL to about 1 .4 mg / mL, about 0.4 mg / mL to about 1.2 mg / mL, about 0.4 mg / mL to about 1.0 mg / mL, about 0.4 mg / mL to about 0.8 mg / mL, about 0.4 mg / mL to about 0.6 mg / mL, about 0.8 mg / mL to about 1 .4 mg / mL about 0.9 mg / mL to about 1.3 mg / mL, or about 1.0 mg / mL to about 1.2 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about 0.2 mg / mL, about 0.4 mg / mL, about 0.5 mg / mL, about 0.6 mg / mL, about 0.7 mg / mL, about 0.8 mg / mL, about 0.9 mg / mL, about 1 .0 mg / mL, about 1 .1 mg / mL, about 1 .2 mg / mL, or about 1.4 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about 0.4 mg / mL, including about 0.42 mg / mL to about 0.44 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about 1 .1 mg / mL, including about 1.13 mg / mL to about 1 .15 mg / mL.

[0163] In some embodiments, the glacial acetic acid is present in the pharmaceutical composition in an amount of about 1.0 mg / mL to about 5.0 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in anDocket No. 183B-412975-WO amount of about 1 .0 mg / mL to about 4.5 mg / mL, about 1 .5 mg / mL to about 4.0 mg / mL, about 2.0 mg / mL to about 3.5 mg / mL, or about 2.5 mg / mL to about 3.0 mg / mL. In some embodiments, the glacial acetic acid is present in the pharmaceutical composition or formulation in an amount of about about 1 .0 mg / mL to about 1 .5 mg / mL, about 1 .0 mg / mL to about 3.0 mg / mL, about 1.0 mg / mL to about 5.0 mg / mL about 1.0 mg / mL to about 2.5 mg / mL, or about 2.5 mg / mL to about 5.0 mg / mL.

[0164] The pharmaceutical compositions and formulations of the present technology further comprise water. The water may be sterile water for injection (SWFI), sterile water, bacteriostatic water for injection (BWFI), distilled water, bidistilled water, deionized water, deionized distilled water, and reverse osmosis water. In some embodiments, the water present in the pharmaceutical composition or formulation is sterile water for injection.

[0165] The pharmaceutical compositions and formulations of the present technology may further comprise a surfactant. Non-limiting examples of surfactant that may be included in the pharmaceutical compositions or formulations include anionic surfactants such as alkyl carboxylate-fatty acid salts, sulfates (e.g., sodium lauryl sulfate and alkyl ether sulfates), sulfonates (e.g., dioctyl sodium sulfosuccinate and alkyl benzenesulfonates), and phosphate esters (e.g., alkyl aryl ether phosphates and alkyl ether phosphates); cationic surfactants such as quaternary ammoniums (e.g., cetrimonium bromide, cetylpyridinium chloride, and dimethyldioctadecylammonium chloride), amine-based surfactants (e.g., triethylamine hydrochloride and octenidine dihydrochloride) and pyridinium surfactants (e.g., benzethonium chloride); non-ionic surfactants such as polyol esters (e.g., fatty acid esters of sorbitan), polyoxyethylene esters (e.g., polysorbates), and poloxamers (e.g., poloxamer 188); and amphoteric surfactants such as phospholipids (e.g., phosphatidylcholine and lecithin), carboxylic acid / quaternary ammoniums (e.g., cocamidopropyl betaine and amidosulfobetaine-16), phosphoric acid / quaternary ammoniums (e.g., hexadecyl phosphocholine), and betaines (e.g., alkylamidopropyl betaine). In some embodiments, the surfactant is a non-ionic surfactant. In further embodiments, the surfactant is a polysorbate.

[0166] In some embodiments, the pharmaceutical composition or formulation comprises substantially no chloride ions. In some embodiments, the pharmaceutical composition or formulation is free from chloride ions.Docket No. 183B-412975-WO

[0167] In some embodiments, the pharmaceutical composition or formulation comprises substantially no metal ions. In some embodiments, the pharmaceutical composition or formulation is free from metal ions.

[0168] In some embodiments, the pharmaceutical composition has a pH of about 5.3, and comprises a non-naturally occurring melanocortin antagonist analog in an amount of 12.5 mg / mL, mannitol in an amount of about 30 mg / mL to about 40 mg / mL, an acid in an amount of about 1.3 mg / mL to about 1.5 mg / mL, and histidine at a concentration of about 25 mM. In further embodiments, the mannitol is present in the composition in an amount of about 37.5 mg / mL. In still further embodiments, the acid is glacial acetic acid.

[0169] In some embodiments, the pharmaceutical composition has a pH of about 5.3, and comprises a non-naturally occurring melanocortin antagonist analog in an amount of 25 mg / mL, , mannitol in an amount of about 30 mg / mL to about 40 mg / mL, an acid in an amount of about 0.42 mg / mL to about 0.44 mg / mL, and histidine at a concentration of about 25 mM. In further embodiments, the mannitol is present in the composition in an amount of about 35 mg / mL. In still further embodiments, the acid is glacial acetic acid.

[0170] In some embodiments, the pharmaceutical composition has a pH of about 4.0 to about 6.5 and comprises a non-naturally occurring melanocortin antagonist analog in an amount of 50 mg / mL, mannitol in an amount of about 25 mg / mL to about 35 mg / mL, a base in an amount of about 0.4 mg / mL to about 1 .2 mg / mL, and a buffer at a concentration of about 25 mM. In some embodiments, the mannitol is present in the composition in an amount of about 25 mg / mL. In other embodiments, the mannitol is present in the composition in an amount of about 27.5 mg / mL. In further embodiments, the base is sodium hydroxide. In some embodiments, the buffer is histidine. In other embodiments, the buffer is sodium acetate. In some embodiments, the sodium hydroxide is present in an amount of 0.4 mg / mL, the buffer is histidine, and the pH of the pharmaceutical composition is about 5.3. In other embodiments, the sodium hydroxide is present in an amount of 1 .2 mg / mL, the buffer is histidine, and the pH of the pharmaceutical composition is about 6.3. In still other embodiments, the sodium hydroxide is present in an amount of 0.5 mg / mL, the buffer is sodium acetate, and the pH of the pharmaceutical composition is about 5.0.Methods of Preparing Pharmaceutical Compositions and FormulationsDocket No. 183B-412975-WO

[0171] The present technology further provides methods of preparing pharmaceutical compositions and formulations described herein, e.g., pharmaceutical compositions comprising a non-naturally occurring melanocortin antagonist analog and one or more pharmaceutically acceptable carriers and / or excipients. In some embodiments, the method produces a pharmaceutical composition or formulation of a non-naturally occurring melanocortin antagonist analog that has a pH of about 4.0 to about 6.5.

[0172] Methods of preparing the pharmaceutical compositions and formulations comprise providing an aqueous peptide composition of the non-naturally occurring melanocortin antagonist analog. In some embodiments, the aqueous peptide composition is provided by dissolving the non-naturally occurring melanocortin antagonist analog in water. In some embodiments, when a surfactant is included in the pharmaceutical composition or formulation, the surfactant is also dissolved in the water to provide the aqueous peptide composition. A surfactant may be included in the aqueous peptide composition to prevent the peptide from adhering to the walls of the reaction vessel or tubing.

[0173] In some embodiments, the non-naturally occurring melanocortin antagonist analog has at least one cationic residue and an isoelectric point of at least about 10. In further embodiments, the non-naturally occurring melanocortin analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5. In still further embodiments, the non-naturally occurring melanocortin analog has an arginine residue and an isoelectric point of at least about 10. In yet further embodiments, the non-naturally occurring melanocortin analog has an arginine residue and an isoelectric point of about 10 to about 12.5.

[0174] In some embodiments, the aqueous peptide composition is provided by dissolving the non-naturally occurring melanocortin antagonist analog comprising a sequence of any one of Formulae (l)-(IB) in water. In some embodiments, the aqueous peptide composition is provided by dissolving the non-naturally occurring melanocortin analog comprising a sequence of any one of SEQ ID NOs: 457, 472-474, and 476-720in water. The non-naturally occurring melanocortin analog dissolved in the water may be in the form of a salt, such as, for example, an acetate salt. To achieve complete dissolution of the non-naturally occurring melanocortin analog in the water, the aqueous peptide solution mayDocket No. 183B-412975-WO be stirred for a period of time sufficient to achieve a homogenous solution. The period of time sufficient to achieve homogeneity may depend on the batch size of the pharmaceutical composition or formulation. In some embodiments, the aqueous peptide composition is stirred for about 10 minutes to about 24 hours. In some embodiments, the aqueous peptide composition is stirred for about 10 minutes to about 60 minutes, about 15 minutes to about 50 minutes, about 20 minutes to about 40 minutes. In some embodiments, the aqueous peptide composition is stirred for about 30 minutes to achieve homogeneity of the composition. Alternatively, in some embodiments, the aqueous peptide composition is stirred for about 1 hour to about 24 hours. In some embodiments, the aqueous peptide composition is stirred for about 1 hour, about 2 hours, about 4 hours, about 6 hours, about 8 hours, about 10 hours, about 12 hours, about 14 hours, about 16 hours, about 18 hours, about 20 hours, about 22 hours, or about 24 hours to achieve homogeneity of the composition. The aqueous peptide composition may be mixed and maintained at ambient temperature.

[0175] When the non-naturally occurring melanocortin antagonist analog is in the form of a salt, such as, for example, an acetate salt, the aqueous peptide composition may be acidic. In some embodiments, the aqueous peptide composition has a pH of about 2.5 to about 5.0. In some embodiments, the aqueous peptide composition has a pH of about 2.5, about 2.8, about 3.0, about 3.2, about 3.5, about 3.8, about 4.0, about 4.2, about 4.5, about 4.8, or about 5.0.

[0176] Methods of preparing the pharmaceutical compositions and formulations comprise providing a pharmaceutically acceptable carrier composition. In some embodiments, the pharmaceutically acceptable carrier composition is provided by dissolving one or more pharmaceutically acceptable carriers and / or excipients in water. In further embodiments, the pharmaceutically acceptable carrier composition is provided by dissolving an osmolyte, a pH adjusting agent, and a buffer in water. In some embodiments, when a surfactant is included in the pharmaceutical composition or formulation, the surfactant is also dissolved in the water to provide the pharmaceutically acceptable carrier composition. The pharmaceutically acceptable carrier composition may be mixed for an amount of time sufficient to achieve a homogenous composition. The period of time sufficient to achieveDocket No. 183B-412975-WO homogeneity may depend on the batch size of the pharmaceutical composition or formulation. In some embodiments, the aqueous peptide composition is stirred for about 5 minutes to about 24 hours. In some embodiments, the aqueous peptide composition is stirred for about 5 minutes to about 40 minutes, about 10 minutes to about 30 minutes, about 15 minutes to about 20 minutes. In some embodiments, the aqueous peptide composition is stirred for about 15 minutes to achieve homogeneity of the composition. Alternatively, in some embodiments, the aqueous peptide composition is stirred for about 1 hour to about 24 hours. In some embodiments, the aqueous peptide composition is stirred for about 1 hour, about 2 hours, about 4 hours, about 6 hours, about 8 hours, about 10 hours, about 12 hours, about 14 hours, about 16 hours, about 18 hours, about 20 hours, about 22 hours, or about 24 hours to achieve homogeneity of the composition. The pharmaceutically acceptable carrier composition may be mixed and maintained at ambient temperature.

[0177] The pharmaceutically acceptable carrier composition may have a pH that is sufficiently basic to neutralize the aqueous peptide composition, e.g., a pH that is sufficiently basic to produce a pharmaceutical composition or formulation having a pH of about 4.0 to about 7.0. For example, the pharmaceutically acceptable carrier composition may have a pH of about 5.0 to about 11 .0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 7.0 to about 1 1 .0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 8.0 to about 11 .0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 9.0 to about 11.0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 10.0 to about 11.0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 10.5 to about 11.0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 8.0 to about 10.5. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 8.5 to about 10.0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 9.0 to about 9.5.

[0178] In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 5.0 to about 7.0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 5.0 to about 6.5. In some embodiments, theDocket No. 183B-412975-WO pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 7.0. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 6.5. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 5.9. In some embodiments, the pharmaceutically acceptable carrier composition has a pH of about 6.2 to about 6.6.

[0179] Methods of preparing the pharmaceutical compositions and formulations comprise combining an aqueous peptide composition with a pharmaceutically acceptable carrier composition. In some embodiments, the aqueous peptide composition is added to the pharmaceutically acceptable carrier composition. In other embodiments, the pharmaceutically acceptable carrier composition is added to the aqueous peptide composition. Once the aqueous peptide composition and the pharmaceutically acceptable carrier composition are combined, the combined solution may be stirred for an amount of time sufficient to achieve a stable homogeneous composition. In some embodiments, the combined solution is stirred for about 10 minutes to about 24 hours. In some embodiments, the aqueous peptide composition is stirred for about 10 minutes to about 60 minutes, about 15 minutes to about 50 minutes, about 20 minutes to about 40 minutes. In some embodiments, the combined solution is stirred for about 30 minutes to achieve homogeneity. Alternatively, in some embodiments, the aqueous peptide composition is stirred for about 1 hour to about 24 hours. In some embodiments, the aqueous peptide composition is stirred for about 1 hour, about 2 hours, about 4 hours, about 6 hours, about 8 hours, about 10 hours, about 12 hours, about 14 hours, about 16 hours, about 18 hours, about 20 hours, about 22 hours, or about 24 hours to achieve homogeneity of the composition. The combined solution may be stirred at ambient temperature.

[0180] While the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, a local pH of the pharmaceutical composition may be maintained such that no local region has a pH that is equal to the isoelectric point of the melanocortin analog so as to prevent aggregation of the melanocortin analog. As used herein, a “local pH” refers to the pH of the composition surrounding the site where the composition is being formed, i.e., where the aqueous peptide composition and the pharmaceutically acceptable carrier composition are combined. The area of the site whereDocket No. 183B-412975-WO the local pH is maintained may be relative to the process used to combine the aqueous peptide composition and the pharmaceutically acceptable carrier composition. For example, if the pharmaceutically acceptable carrier composition is poured into the aqueous peptide composition, or vice versa, the area of the site where the local pH is maintained may be larger than the area of the site where the local pH is maintained if the pharmaceutically acceptable carrier composition is cannulated, syringed, or pipetted into the aqueous peptide composition, or vice versa. Methods described herein may prevent aggregation of the non- naturally occurring melanocortin analog by combining the aqueous peptide composition with the pharmaceutically acceptable carrier composition via slow addition, such as for example, drop-wise addition, timed addition, portioned addition, and the like.

[0181] In some embodiments, once the aqueous peptide composition and the pharmaceutically acceptable carrier composition are combined and a homogenous solution is provided, the pH of the solution is adjusted to achieve the desired pH of the pharmaceutical composition or formulation. In further embodiments, the desired pH of the pharmaceutical composition or formulation is about 4.0 to about 6.5. In other embodiments, the pH of the homogenous solution is the desired pH of the pharmaceutical composition or formulation. Accordingly, in some embodiments, the pH is not adjusted.

[0182] In some embodiments, the pharmaceutical composition or formulations produced by the methods described herein comprise substantially no precipitated non- naturally occurring melanocortin analog. In some embodiments, the pharmaceutical composition or formulations produced by the methods described herein are free from precipitated non-naturally occurring melanocortin analog.

[0183] In some embodiments, the method is a method of producing a pharmaceutical composition of a non-naturally occurring melanocortin antagonist analog, the method comprising combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 with a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 1 1 .0 and comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5.Docket No. 183B-412975-WO

[0184] In some embodiments, the method is a method of producing a pharmaceutical formulation having a pH of about 4.0 to about 6.5, the method comprising combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical composition such that no local region has a pH that is equal to the isoelectric point of the antagonist analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5 and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 11 .0.

[0185] In some embodiments, the method is a method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog having a pH of about 4.0 to about 6.5, the method comprising combining an aqueous peptide composition of the non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog has an arginine residue and an isoelectric point of at least about 10 and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 1 1 .0.EXAMPLES

[0186] The following examples are intended to illustrate various embodiments of the present technology. As such, the specific embodiments discussed are not to be construed as limitations on the scope of the present technology. It will be apparent to one skilled in the art that various equivalents, changes, and modifications may be made without departing from the scope of present technology, and it is understood that such equivalent embodiments, are to be included herein. Further, all references cited herein are hereby incorporated by reference in their entirety, as if fully set forth herein.Example 1: Peptide Synthesis-GenericDocket No. 183B-412975-WO

[0187] The non-naturally occurring melanocortin analogs described herein were synthesized by conventional procedures (e.g., solution-phase procedure, solid-phase synthesis) for the formation of a peptide linkage between amino acids. The solution-phase procedure involved a condensation between the free alpha amino group of an amino acid or derivative thereof having the carboxyl group or other reactive groups protected and the free primary carboxyl group of another amino acid or derivative thereof having the amino group or other reactive groups protected. The solid-phase synthesis utilized a variety of resins and reagents and may involve additional purification steps.

[0188] The process for synthesizing the non-naturally occurring melanocortin analogs was generally performed by a procedure as follows. Each amino acid in the desired sequence of the non-naturally occurring melanocortin analogs was added one at a time in succession to another amino acid or derivative thereof or by a procedure whereby peptide fragments with the desired amino acid sequence were first synthesized conventionally and then condensed to provide the desired peptide. In most cases, the resulting peptide was then cyclized to yield a cyclic peptide.

[0189] Solid-phase peptide synthesis was carried out by sequentially incorporating the desired amino acid residues one at a time into the growing peptide chain coupled to a solidphase support according to the general principles of solid phase methods (see Merrifield, Angew Chem. 24:799-810 (1985) and Barany et al. , The Peptides, Analysis, Synthesis and Biology, Vol. 2, Gross E. and Meienhofer J., Eds. Academic Press 1 -284 (1980)). An exemplary solid-phase synthesis of non-naturally occurring melanocortin analogs is provided below.

[0190] Initially, the C-terminal amino acid residue of the non-naturally occurring melanocortin analog was coupled to a solid-phase support, e.g., a solid-phase resin. Coupling of the C-terminal amino acid residue and the solid-phase support may be carried out according to any method know in the art. Depending on the coupling method, the alphaamine of the C-terminal amino acid residue may or may not be protected with an amine protecting group, as described below. Likewise, the carboxyl group of the amino acid residue may or may not be activated prior to coupling to the solid-phase support in order to increase its electrophilicity. Some methods of coupling rely on the formation of an ester bond betweenDocket No. 183B-412975-WO the carboxyl group of the amino acid and a reactive handle on the solid-phase resin. For example, an amino acid residue may be coupled to a p-benzyloxybenzyl alcohol resin (Wang) or a 2-chlorotrityl chloride resin via an ester linkage. Some methods of coupling rely on the formation of an aminde bond between the carboxyl group of the amino acid and a reactive handle on the solid-phase resin For example, an amino acid residue may be coupled to a benzhydrylamine (BHA) resin through an Fmoc-linker such as, for example, p- [(R,S)-a-[1 -(9H-fluor-en-9-yl)-methoxyformamido]-2,4-dimethyloxybenzyl]-phenoxyacetic acid (Rink linker) via an amide linkage.

[0191] The non-naturally occurring melanocortin analog was then synthesized by sequential amino acid addition or combination of peptide fragments. Subsequently, the peptide was cleaved from the solid-phase support and purified by methods known in the art, such as, for example, reverse phase high performance liquid chromatography (RP-HPLC) using a suitable column, such as a C18 column. Additionally, or alternatively, other methods of separation or purification were employed, including, but not limited to, methods based on the size or charge of the peptide, and affinity tag-based purification. Once purified, the peptide was characterized by methods such as high-performance liquid chromatograph (HPLC), amino acid analysis, mass spectrometry, and the like.Example 2: Peptide Synthesis-Protecting Groups

[0192] During synthesis of the non-naturally occurring melanocortin analogs, reactive side chain groups of the various amino acid residues were protected with suitable protecting groups, which prevented undesirable chemical reaction from occurring at that site until the protecting group was removed.

[0193] Additionally, protection of the alpha amino group of an amino acid residue or fragment was performed while that entity reacting with the carboxyl group, followed by the selective removal of the alpha amino protecting group to allow a subsequent reaction to take place at that site. Specific protecting groups for solid phase synthesis methods and solution phase synthesis methods are known to those having ordinary skill in the art. Alpha amino groups were protected by a suitable protecting group, including a urethane-type protecting group, such as benzyloxycarbonyl (Z) and substituted benzyloxycarbonyl, such as p- chlorobenzyloxycarbonyl, p-nitrobenzyloxycarbonyl, p-bromobenzyloxycarbonyl, p-Docket No. 183B-412975-WO biphenyl-isopropoxycarbonyl, 9-fluorenylmethoxycarbonyl (Fmoc) and p- methoxybenzyloxycarbonyl (Moz); aliphatic urethane-type protecting groups, such as t- butyloxycarbonyl (Boc), diisopropylmethoxycarbonyl, isopropoxycarbonyl, and allyloxycarbonyl. Fmoc was also used for alpha amino protection. Guanidino groups, if present, were protected by a suitable protecting group, such as nitro, p-toluenesulfonyl (Tos), Z, pentamethylchromanesulfonyl (Pmc), adamantyloxycarbonyl, pentamethyldihydrobenzofuran-5-sulfonyl (Pbf) and Boc. Pmc was used as a protecting group for Arg.

[0194] Alpha aminoprotecting groups may be removed under basic conditions, such as, for example, using a solution of piperidine, piperazine, diethylamine, or morpholine (20- 40% v / v) in N,N-dimethylformamide (DMF). In synthesis methods in which alpha amino protecting groups were used, protecting groups were removed after synthesis of the peptide and before or after cleavage of the solid-phase support.Example 3: Peptide Synthesis-Additional Modifications

[0195] If necessary, the peptides were further modified to obtain N-terminus modifications, such as acetylation, while on resin, or were removed from the resin by use of a cleaving reagent and then modified. Likewise, C-terminus modification (e.g., amidation), was performed if needed.

[0196] Additionally, the cyclized peptide structures were obtained prior to cleavage from the peptide resin. For cyclization through reactive side chain moieties, the desired side chains were deprotected, and the peptide suspended in a suitable solvent and a cyclic coupling agent added. Suitable solvents, for example DMF, dichloromethane (DOM) or 1 - methyl-2-pyrrolidone (NMP), were used for the cyclization. Suitable cyclic coupling reagents (e.g., 2-(1 H-benzotriazol-1 -yl)-1 ,1 ,3,3-tetramethyluronium tetrafluoroborate (TBTU), 2-(1 H- benzotriazol-1 -yl)-1 ,1 ,3,3-tetramethyluronium hexafluorophosphate (HBTLI), benzotriazole- 1 -yl-oxy-tris(dimethylamino)phosphoniumhexafluorophosphate (BOP), benzotriazole-1 -yl- oxy-tris(pyrrolidino)phosphoniumhexafluorophosphate (PyBOP), 2-(7-aza-1 H-benzotriazol- 1 -yl)-1 ,1 ,3,3-tetramethyluronium tetrafluoroborate (TATU), 2-(2-oxo-1 (2H)-pyridyl)-1 ,1 ,3,3- tetramethyluronium tetrafluoroborate (TPTU), N,N'-dicyclohexylcarbodiimide / 1 - hydroxybenzotriazole (DCCI / HOBt) hexafluorophosphate azabenzotriazole tetramethylDocket No. 183B-412975-WO uranium (HATU), or ethyl (hydroxyimino)cyanoacetate / diisopropylcarbodiimide (Oxyma / DIG)) were also used for the cyclization. Coupling was initiated by a suitable base, such as N,N-diispropylethylamine (DIPEA), sym-collidine or N-methylmorpholine (NMM).Example 4: Biological Data

[0197] The agonist and antagonist activity of exemplary non-naturally occurring melanocortin analogs at the melanocortin receptors (e.g., MC1 R, MC3R, MC4R, and MC5R) were measured via cAMP accumulation assay, according to the following procedure. Experimental design and execution were conducted by Epics Therapeutics S.A. EuroscreenFast (Bruxelles, Belgium).Compound Handing

[0198] Compounds were delivered as powder (1 mg) or 10 mM solutions (100 pl) in 100% DMSO. Powders were solubilized in 100% DMSO at a concentration of 10 mM (master solution) in a solvent volume defined. Serial dilutions were performed from master solution in 100% DMSO to obtain intermediate concentrations 200-, 300- or 400-fold higher than the concentrations to be tested, depending on the assay. Each sample was diluted 100- fold in the assay buffer and dispensed in a test plate. Amounts, solvents, and dilutions were estimated based on standard small-molecule drugs. Cell lines used for functional assays are shown in Table 1 .Table 1. Cell linesCompound Testing

[0199] Compounds were tested for (i) agonist and / or antagonist activity at the human MC3 (FAST-0232C) and MC4 (FAST-0233C) receptors, (ii) agonist activity at the human MC1 (FAST-0230C) receptor, and / or (iii) agonist activity at the human MC5 (FAST-0233C) receptor at the following nanomolar concentrations, in duplicate: 0.0001 , 0.001 , 0.01 , 0.03, 0.1 , 0.3, 1 , 10, 100, and 1 ,000.Docket No. 183B-412975-WOTesting Protocol

[0200] Cyclic AMP (cAMP) Homogenous Time-Resolved Fluorescence (HTRF) assay for Gs coupled receptor:

[0201] CHO-K1 cells expressing recombinant human receptor grown prior to the test in media without antibiotic were detached by gentle flushing with PBS-EDTA (5 mM EDTA), recovered by centrifugation and resuspended in assay buffer (KRH: 5 mM KCI, 1.25 mM MgSO4, 124 mM NaCI, 25 mM HEPES, 13.3 mM Glucose, 1.25 mM KH2PO4, 1.45 mM CaCI2, 0.5 g / l BSA, supplemented with 1 mM IBMX or 25pM Rolipram).

[0202] Dose response curves were performed in parallel with the reference compounds.

[0203] For agonist test (384well): 5 pl of cells were mixed with 5 pl of the test compound at increasing concentrations and then incubated 30 min at room temperature. After addition of the lysis buffer containing cAMP-d2 and anti-cAMP cryptate detection reagents, plates were incubated 1 -hour at room temperature, and fluorescence ratios were measured according to the manufacturer specification, with the HTRF kit. Reference agonist NDP-a- MSH (Ser-Tyr-Ser-Nle-Glu-His-dPhe-Arg-Trp-Gly-Lys-Pro-Val; SEQ ID NO: 721 ) was also tested as a comparator.

[0204] For antagonist test (384well): 5 pl of cells were mixed in the wells of an assay plate with 5 pl of a mix of the test compound at increasing concentrations for a final concentration corresponding to the historical EC80. The plates were then incubated 30 min at room temperature. After addition of the lysis buffer containing cAMP-d2 and anti-cAMP cryptate detection reagents, plates were incubated 1 -hour at room temperature, and fluorescence ratios were measured according to the manufacturer specification, with the HTRF kit. Reference antagonist SHU9119 (Ac-Nle-c[Asp-His-dNal(2’)-Arg-Trp-Lys]-NH2; SEQ ID NO: 722) was also tested as a comparator.Quality Control for Compound Testing

[0205] On each day of experimentation and prior to the testing of compounds, reference compounds were tested at several concentrations in duplicate (n=2) to obtain a dose-response curve and an estimated EC50 and / or IC50 values.Docket No. 183B-412975-WO

[0206] Reference values thus obtained for the test were compared to historical values obtained from the same receptor and used to validate the experimental session.

[0207] A session was considered as valid only if the reference value was found to be within a 0.5 logs interval from the historical value.

[0208] For replicate determinations, the maximum variability tolerated in the test was of + / -20% around the average of the replicates.Non-naturally occurring melanocortin analog grouping

[0209] Group A included non-naturally occurring melanocortin analogs A1 -A16, both of which are peptides comprising the motif Pro-dNal(2’)-Arg-Trp. Group A melanocortin analogs also comprise Nle at the N-terminus and dVal-dPro at the C-terminus. Certain Group A melanocortin analog are linear and certain other Group A melanocortin analogs are cyclized through a lactam or disulfide bond. Group A non-naturally occurring melanocortin analogs are provided in Table 2.Table 2. Group A Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0189] Group B included non-naturally occurring melanocortin analogs B1 to B37, all of which are cyclic peptides comprising a derivative of the motif Pro-dNal(2')-Arg-Trp.Derivatives of the motif Pro-dNal(2’)-Arg-Trp may include substitution of Pro for another amino acid, such as, for example, His, transPro(gaun) or cisPro(gaun), substitution of Arg for another amino acid, such as, for example, Ala, Orn, or Lys, substituition of Trp for another amino acid, such as, for example, Aba, Aia, Ata, dPhe, dTyr, or dNal(2’), or deletion of Pro, Arg, or Trp. Group B melanocortin analogs also comprise at least Nle at the N-terminis and dVal-dPro at the C-terminus. Group B non-naturally occurring melanocortin analogs are provided in Table 3.Table 3. Group B Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0190] Group C included non-naturally occurring melanocortin analogs C1 to C32, all of which are cyclic peptides comprising the motif Pro-dNal(2’)-Arg-Trp. Group C melanocortin analogs comprise a moiety other than Nle at the N-terminus and dVal-dPro at the C- terminus. Certain Group C melanocortin analogs comprise an amino acid other than Nle atDocket No. 183B-412975-WO the N-terminus, whereas others comprise an extended N-terminus. Group C non-naturally occurring melanocortin analogs are provided in Table 4.Table 4. Group C Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0191] Group D included non-naturally occurring melanocortin analogs D1 to D22, all of which are cyclic peptides comprising the motif Pro-dNal(2’)-Arg-Trp. Group D melanocortin analogs also have Nle at the N-terminus and a moiety other than dVal-dPro at the C- terminus. Group D non-naturally occurring melanocortin analogs are provided in Table 5.Table 5. Group D Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WO

[0192] Group E included non-naturally occurring melanocortin analogs E1 to E14, all of which are cyclic peptides comprising the motif Ala-His-dNal(2’)-Arg-Trp (SEQ ID NO: 723), or a derivative thereof. Derivatives of the moitf Ala-His-dNal(2’)-Arg-Trp may include substitution of Ala-His for His or other dipeptides including His, such as, for example, dAla- His, Phe-His, Glu-His, and Pro-His, and / or substitution of Arg for another amino acid, such as, for example, His. Group E melanocortin analogs further include Nle, Arg, or dArg at the N-terminus and an absent or dVal-dPro C-terminus. Group E non-naturally occurring melanocortin analogs are provided in Table 6.Table 6. Group E Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0193] Group F included non-naturally occurring melanocortin analogs F1 and F2, all of which are cyclic peptides comprising the motif His-dNal(2’)-Arg-Trp. Group F melanocortin analogs also comprise a also comprise Phe-Phe at the N-terminus or within the cyclic portion and a dVal-dPro moiety at the C-terminus and are cyclized through a lactam bridge. Group F non-naturally occurring melanocortin analogs are provided in Table 7.Table 7. Group F Non-naturally occurring melanocortin analogs

[0194] Group G included non-naturally occurring melanocortin analogs G1 to G7, all of which are cyclic peptides comprising the motif Pro-dNal(2')-Arg-Trp, or a derivative thereof. Derivatives of the motif Pro-dNal(2’)-Arg-Trp may include substitution of Pro with another amino acid, such as, for example, Glu or Hyp. Group G melanocortin analogs also comprise an expanded cycle with a Pro or Gly residue included after Trp, and dVal-dPro at the C- terminus. Group G non-naturally occurring melanocortin analogs are provided in Table 8.Table 8. Group G Non-naturally occurring melanocortin analogs

[0195] Group H included non-naturally occurring melanocortin analogs H1 to H4, all of which are cyclic peptides comprising the motif Pro-dPhe-Arg-Trp (SEQ ID NO: 726) or aDocket No. 183B-412975-WO derivative thereof. Derivatives of the motif Pro-dPhe-Arg-Trp (SEQ ID NO: 726) may include substitution of Pro for another amino acid, such as, for example, Oic, or substitution of Trp for another aromatic amino acid, such as for example dNal(2’), and / or substitution of dPhe for another aromatic amino acid, such as, for example, p(F)dPhe. . Group H melanocortin analogs also comprise Nle at the N-terminus and dVal-dPro at the C-terminus. Group H non-naturally occurring melanocortin analogs are provided in Table 9.Table 9. Group H Non-naturally occurring melanocortin analogs

[0196] Group I included non-naturally occurring melanocortin analogs 11 -121 , all of which are cyclic peptides comprising the motif His-p(Br)dPhe-Arg-Trp (SEQ ID NO: 727), or a derivative thereof. Derivatives of the motif His-p(Br)dPhe-Arg-Trp (SEQ ID NO: 727) may include substitution of p(Br)dPhe for another aromatic amino acid, such as, for example, p(CI)dPhe. Group I melanocortin analogs also comprise a moiety other than Nle at the N- terminus and / or a moiety other than dVal-dPro at the C-terminus. Group I non-naturally occurring melanocortin analogs are provided in Table 10.Table 10. Group I Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0197] Group J included non-naturally occurring melanocortin analogs J1 and J20, both of which are cyclic peptides comprising the motif comprising the motif His-p(Br)dPhe-Arg- Trp (SEQ ID NO: 727) or a derivative thereof. Derivatives of the motif His-p(Br)dPhe-Arg- Trp (SEQ ID NO: 727) may include substitution of p(Br)dPhe for another aromatic amino acid, such as, for example, p(CI)dPhe, p(l)dPhe, or p(CF3)dPhe, substitution of His for another amino acid, such as, for example dHis or Gin, and / or substitution of Arg for another amino acid, such as, for example, His. Group J melanocortin analogs also comprise a dVal- dPro moiety at the C-terminus and are cyclized through a lactam bridge. Group J non- naturally occurring melanocortin analogs are provided in Table 11.Table 11. Group J Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0198] Group K included non-naturally occurring melanocortin analogs K1 to K9, all of which are cyclic peptides comprising the motif Phe-p(Br)dPhe-Arg-Trp (SEQ ID NO: 729), or a derivative thereof. Derivatives of the motif Phe-p(Br)dPhe-Arg-Trp (SEQ ID NO: 729) may include substitution of Phe for another aromatic amino acid, such as, for example, Trp or Tyr, and / or substitution of p(Br)dPhe for another aromatic amino acid, such as, for example, p(CI)dPhe or p(F)dPhe. Group K melanocortin analogs further comprise Nle at the N-terminus and dVal-dPro at the C-terminus. Group K non-naturally occurring melanocortin analogs are provided in Table 12.Table 12. Group K Non-naturally occurring melanocortin analogsDocket No. 183B-412975-WO

[0199] Group L included non-naturally occurring melanocortin analog L1 -L9, which are cyclic peptides comprising the motif Pro-p(Br)dPhe-Arg-Trp (SEQ ID NO: 728), or a derivative thereof. Derivatives of the motif Pro-p(Br)dPhe-Arg-Trp (SEQ ID NO: 728) may include substitution of p(Br)dPhe with another amino acid, such as, for example, p(CI)dPhe, p(l)dPhe, or p(CF3)dPhe. Group L melanocortin analogs also include Nle at the N-terminus and dVal-dPro at the C-terminus. Group L non-naturally occurring melanocortin analogs are provided in Table 13.Table 13. Group L Non-naturally occurring melanocortin analogs

[0200] Group M included non-naturally occurring melanocortin analogs M1 and M2, which are cyclic peptides comprising the motif Arg-p(l)dPhe-Arg-Tic. Group M melanocortinDocket No. 183B-412975-WO analogs also comprise Nle at the N-terminus and dVal-dPro at the C-terminus. Group M non- naturally occurring melanocortin analogs are provided in Table 14.Table 14. Group M Non-naturally occurring melanocortin analogsAgonist activity of melanocortin analogs on melanocortin 1 receptor and melanocortin 5 receptor

[0201] Administration of all the exemplary non-naturally occurring melanocortin analogs activated melanocortin 1 receptor (MC1 R) and melanocortin 5 receptor (MC5R) activity, as measured by cAMP levels (Table 15).Table 15. Dose-response results of melanocortin analogs and control against the melanocortin 1 receptor (MC1 R) and the melanocortin 5 receptor (MC5R)Docket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WOk = < 1 nM= 1 nM to 100 nM* = > 100 nMA = > 80% EmaxB = 50 ■ 80% EmaxC = < 50% EmaxAgonist activity of melanocortin analogs on melanocortin 3 receptor and melanocortin 4 receptor

[0202] Administration of few of the non-naturally occurring melanocortin analogs activated melanocortin 3 receptor (MC3R) or melanocortin 4 receptor (MC4R) activity, as measured by cAMP levels (Table 16).Table 16. Dose-response results of melanocortin analogs and control against the melanocortin 3 receptor (MC3R) and the melanocortin 4 receptor (MC4R)Docket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WO*** = < 1 nM** = 1 nM to 100 nM* = > 100 nMA = > 80% EmaxB = 50 ■ 80% EmaxC = < 50% EmaxAntagonist activity of melanocortin analogs on melanocortin 3 receptor and melanocortin 4 receptor

[0203] Administration of all the non-naturally occurring melanocortin analogs inhibited melanocortin 3 receptor (MC3R) and / or melanocortin 4 receptor (MC4R) activity, as measured by cAMP levels (Table 17).Table 17. Dose-response results of melanocortin analogs and control against the melanocortin 1 receptor (MC3R) and the melanocortin 5 receptor (MC4R)Docket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WODocket No. 183B-412975-WO*** = < 1 nM** = 1 nM to 100 nM* = > 100 nMA = > 80% EmaxB = 50 ■ 80% EmaxC = < 50% EmaxExample 5: Stable Aqueous Compositions of Melanocortin Analog B07

[0210] B07 (Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2; SEQ ID NO: 2) was used as a comparative sequence for the non-naturally occurring melanocortin analogs of the present technology because of the various conserved structural features between B07 and the exemplary melanocortin analogs. For example, B07 and the disclosed melanocortin analogs share one or more of the following features: N-terminal Nle, lactam cyclization, core Pro-dNal(2’)-Arg-Trp scaffolds or derivatives thereof, and C-terminal dVal-dPro or other degradation resistant moiety.

[0211] Three aqueous compositions comprising 50 mg / mL of B07 were tested for stability. The details of each composition are provided in Table 18.Table 18. Aqueous Compositions of 50 mg / mL B07Docket No. 183B-412975-WO

[0212] The compositions were prepared via the following stepwise compounding process.

[0213] Step 1 : A stock solution comprising the histidine or sodium acetate buffer, the mannitol, and the glacial acetic acid or sodium hydroxide was prepared in excess. The details of the stock solution are provided in Table 19.Table 19. Stock Solution for 50 mg / mL Melanocortin Analog Formulations

[0214] The stock solution was prepared by first measuring out 85% of the batch quantity of water to a container. Then, 150 grams of mannitol and 23.28 g of histidine was transferred to the container and the solution was stirred to dissolve the solids. After all solids were dissolved, 7.2 g of sodium hydroxide (equivalent to 7.2 g of sodium hydroxide if a premade solution is being used) was added and stirred to dissolve. Complete dissolution of the added solids in the water was confirmed, then the remaining quantity of water was added while stirring to make up to the final volume. The contents were then mixed to achieve homogenous solution, and the pH of the solution was checked and adjusted to achieve a desired pH based on the desired pH of the final pharmaceutical formulation. For example, for a final pharmaceutical formulation having a pH of about 6.3 (e.g., Formulation 1 ), the pH of the carrier stock solution was adjusted to about 10.5 to about 1 1 .0, whereas for a final formulation having a pH of about 5.3 (e.g., Formulation 2), the pH of the carrier stock solution was adjusted to about 9.3. The stock solution was then kept at room temperature until the next step.Docket No. 183B-412975-WO

[0215] Step 2: The stock solution and an aqueous solution of the melanocortin analog were combined to provide a stable aqueous composition.

[0216] The aqueous solution of the melanocortin analog was prepared by measuring exactly half the batch quantity of water needed for the composition. With the contents gently mixed, the peptide was added to the water in small quantities and the solution was mixed until all solids dissolved. Foam formation was minimized by maintaining low stirring speeds and avoiding a vortex when possible. After all the melanocortin analog was added, complete dissolution of all solids was confirmed. An exact quantity of the stock solution was then added to the aqueous peptide composition while mixing the contents and the solution was then mixed for another 30 minutes to ensure homogeneity of contents. The pH of the homogenous composition was recorded and adjusted as necessary to achieve the target pH of the composition.

[0217] The appearance, pH, osmolality, and assay / impurity assay of samples at RT (Ambient), 40 °C, and 60 °C conditions at T=0, 3, 7 and 14 days were analyzed to determine the stability of the compositions and are shown in Tables 20-25.Table 20. Formulation 1 DetailsTable 21. Additional Formulation 1 DetailsTable 22. Formulation 2 DetailsDocket No. 183B-412975-WOTable 23. Additional Formulation 2 DetailsTable 24. Formulation 3 DetailsTable 25. Additional Formulation 3 Details

[0218] Two aqueous compositions comprising 25 mg / mL of B07 (Ac-Nle-c[Asp-Pro- dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2; SEQ ID NO: 2) were also tested for stability. The compositions were prepared via the following stepwise compounding process.Docket No. 183B-412975-WO

[0219] Step 1 : A stock solution comprising histidine, mannitol, and glacial acetic acid was prepared in excess. The details of the stock solution are provided in Table 26.Table 26. Stock Solution for 25 mg / mL Melanocortin Analog Formulationsa) Density of 50 mM Histidine with 70.6 mg / mL Mannitol and 0.865 mg / mL Glacial Acetic Acid STOCK solution: 1 .024 g / mL b) Adjust the batch size for 50 mM Histidine with 70.6 mg / mL Mannitol and 0.865 mg / mL Glacial Acetic Acid Stock preparation as required.

[0220] The stock solution was prepared by first measuring out 85% of the batch quantity of water to a container. Then, 21 1.80 grams of mannitol and 23.28 g of histidine was transferred to the container and the solution was stirred to dissolve the solids. After all solids were dissolved, 2.6 g of glacial acetic acid was added and stirred to dissolve. Complete dissolution of the added solids in the water was confirmed, then the remaining quantity of water was added while stirring to make up to the final volume. The contents were then mixed for at least 15 minutes to achieve homogenous solution, and the pH of the solution was checked and adjusted to achieve a pH of 6.2 to 6.6. The stock solution was then kept at room temperature until the next step.

[0221] Step 2: The stock solution and an aqueous solution of the melanocortin analog were combined to provide a stable aqueous composition.

[0222] The aqueous solution of the melanocortin analog was prepared by measuring exactly half the batch quantity of water needed for the composition. With the contents gently mixed, the peptide was added to the water in small quantities and the solution was mixed until all solids dissolved. Foam formation was minimized by maintaining low stirring speeds and avoiding a vortex when possible. After all the melanocortin analog was added, complete dissolution of all solids was confirmed. An exact quantity of the stock solution was thenDocket No. 183B-412975-WO added to the aqueous peptide composition while mixing the contents and the solution was then mixed for another 30 minutes to ensure homogeneity of contents. The pH of the homogenous composition was recorded and adjusted as necessary to achieve the target pH of the composition (target pH of 5.3).

[0223] The details of the 25 mg / mL melanocortin analog aqueous formulations are shown in Tables 27 and 28.Table 27. 25 mg / mL Melanocortin Analog Formulation Details - Small BatchTable 28. 25 mg / mL Melanocortin Analog Formulation Details - Large Batch

[0224] Additionally, two aqueous compositions comprising 12.5 mg / mL of B07 (Ac-Nle- c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2; SEQ ID NO: 2) were tested for stability. The compositions were prepared via the following stepwise compounding process.Docket No. 183B-412975-WO

[0225] Step 1 : A stock solution comprising histidine, mannitol, and glacial acetic acid was prepared in excess. The details of the stock solution are provided in Table 29.Table 29. Stock Solution for 12.5 mg / mL Melanocortin Analog Formulationsa) Density of 50 mM Histidine with 70.6 mg / mL Mannitol and 0.865 mg / mL Glacial Acetic Acid STOCK solution: 1 .024 g / mL b) Adjust the batch size for 50 mM Histidine with 70.6 mg / mL Mannitol and 0.865 mg / mL Glacial Acetic Acid Stock preparation as required.

[0226] The stock solution was prepared by first measuring out 85% of the batch quantity of water to a container. Then, 225.00 grams of mannitol and 23.28 g of histidine was transferred to the container and the solution was stirred to dissolve the solids. After all solids were dissolved, 6.89 g of glacial acetic acid was added and stirred to dissolve. Complete dissolution of the added solids in the water was confirmed, then the remaining quantity of water was added while stirring to make up to the final volume. The contents were then mixed for at least 15 minutes to achieve homogenous solution, and the pH of the solution was checked and adjusted to a pH of 5.5 to 5.9. The stock solution was then kept at room temperature until the next step.

[0227] Step 2: The stock solution and an aqueous solution of the melanocortin analog were combined to provide a stable aqueous composition.

[0228] The aqueous solution of the melanocortin analog was prepared by measuring exactly half the batch quantity of water needed for the composition. With the contents gently mixed, the peptide was added to the water in small quantities and the solution was mixed until all solids dissolved. Foam formation was minimized by maintaining low stirring speeds and avoiding a vortex when possible. After all the melanocortin analog was added, complete dissolution of all solids was confirmed. An exact quantity of the stock solution was thenDocket No. 183B-412975-WO added to the aqueous peptide composition while mixing the contents and the solution was then mixed for another 30 minutes to ensure homogeneity of contents. The pH of the homogenous composition was recorded and adjusted as necessary to achieve the target pH of the composition (target pH of 5.3).

[0229] The details of the 25 mg / mL melanocortin analog aqueous formulations are shown in Tables 30 and 31 .Table 30. 12.5 mg / mL Melanocortin Analog Formulation Details - Small BatchTable 31. 12.5 mg / mL Melanocortin Analog Formulation Details - Large BatchExample 6: Stability Data for Melanocortin Analog Formulations

[0230] Impurity formation over time in aqueous formulations comprising 50 mg / mL, 25 mg / mL, or 12.5 mg / mL non-naturally occurring melanocortin analog was performed and the corresponding impurity data was assessed. The non-naturally occurring melanocortin receptor analog present in the aqueous compositions had the sequence of: Ac-Nle-c[Asp-Docket No. 183B-412975-WOPro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (B07; SEQ ID NO: 2). The details of the analysis method and the resulting impurity information are provided below.

[0231] Total impurity regression analysis was used to determine impurity formation in drug products over time. Under this method, impurities are identified in various conditions including (a) real time stability data for drug product maintained at about 2 °C to about 8 °C; (b) accelerated stability data for drug product maintained at 25 °C; and (c) super-accelerated stability data for drug product maintained at 40 °C. The individual impurities identified in drug products subjected to the three stability data conditions for up to nine months are provided in Tables 32-34.Table 32. Individual Impurities in 50 mg B07 Drug ProductDocket No. 183B-412975-WOTable 33. Individual Impurities in 25 mg B07 Drug ProductDocket No. 183B-412975-WOTable 34. Individual Impurities in 12.5 mg B07 Drug ProductDocket No. 183B-412975-WO

[0232] FIGS. 1A-1 F show linear regression models of the total impurity data for samples maintained at 5 °C (FIGS. 1 A-1 C) and 25 °C (FIGS. 1 D-1 F) over the course of nine months.

[0233] Additionally, particulate, osmolality, and pH were tested at the same time points that the total impurity analysis was performed for each sample. The data are shown in Tables 35-37.Table 35. Particulate, Osmolality, and pH of 50 mg B07 Drug ProductTable 36. Particulate, Osmolality, and pH of 25 mg B07 Drug ProductDocket No. 183B-412975-WOExample 7: Additional Stable Aqueous Compositions of Melanocortin Analog B07

[0234] Eight aqueous formulations of B07 including sodium acetate as a buffer, as opposed to histidine, were prepared and tested for stability. Table 38 provides details of the formulations.Table 38. Second Generation Stable Aqueous Injectable Formulations of B07

[0235] The formulations were maintained at various different conditions and tested for osmolality, pH, purity, and particulate matter (via dynamic light scattering (DLS) radius) at various time points for up to four months. The results are shown in Tables 39-43.Table 39. Osmolality (mOSm / kg) of Formulations 1 -8Docket No. 183B-412975-WOTable 40. pH of Formulations 1 -8Table 41. HPLC Purity (%) of Formulations 1 -8Table 42. HPLC Assay Concentration of B07 (mg / mL) of Formulations 1 -8Docket No. 183B-412975-WOTable 43. DLS Radius (nm) of Formulations 1 -8‘Microscopic aggregation was observed at 1 and 2 months for F1 stored at 5 °C and at 1 month for F1 stored at 25 °C and 40 °C“Microscopic aggregation was observed at 2 months for F2 stored at all three temperatures.

[0236] An impurity peak at around 12.2 minutes of the HPLC assay was observed across all samples including baseline. The area of the peak for each formulation at all conditions is provided below in Table 44.Table 44. Area of impurity (area %) at around 12.2 min of HPLC Assay of Formulations 1 -8Docket No. 183B-412975-WO

[0237] Based on the results of the stability analysis for Formulations 1 -8, Formulations 9-20D were prepared to achieve even greater stability of the injectable formulation comprising melanocortin analogs (Table 45).Table 45. Third Generation Stable Aqueous Injectable Formulations of 50 mg / mL B07

[0238] Formulations 9-19 will be maintained at 5 °C, 25 °C, and 40 °C and tested for pH, osmolality, purity, and particulate matter at various time points for up to six months to determine the stability of each formulation.Additional EmbodimentsDocket No. 183B-412975-WO

[0239] Various embodiments of the present technology are set forth below in paragraphs

[0240] to

[0403] :

[0240] 1 . A pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0241] 2. A pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue and no anionic amino acid residues, an osmolyte, a pH adjusting agent, and a buffer, wherein at least one of the one or more cationic amino acid residues is protonated and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0242] 3. A pharmaceutical composition comprising a cyclic non-naturally occurring melanocortin antagonist analog having at one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal- dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0243] 4. A pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue and an isoelectric point of about 10 to about 12.5, an osmolyte, a pH adjusting agent, and a buffer, wherein the non- naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac- Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.Docket No. 183B-412975-WO

[0244] 5. A pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of at least about 10, an osmolyte, a pH adjusting agent, and a buffer wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp- Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0245] 6. A pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having a cyclic region with an arginine residue positioned therein and an isoelectric point of at least about 10 and a pharmaceutically acceptable carrier comprising a base and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0246] 7. A pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an isoelectric point of at least about 10 and a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog comprises moiety (A):X1-R1-R2-R3-R4-R5-R6-R7-Y1 (A), wherein:R1 is absent or is an amino acid or amino acid derivative;R4 is selected from the group consisting of optionally substituted dNal(2’), Rhe, dPhe, Bip and dBip; at least one of R2-R7 is a cationic amino acid residue;Xi is an optionally present N-terminus;Y1 is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a side chain linkage between R2 and R7;Docket No. 183B-412975-WO provided that: moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0247] 8. A pharmaceutical formulation comprising a peptide composition and a pharmaceutically acceptable carrier composition, the peptide composition comprising a non- naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 in an aqueous solution, the pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0248] 9. A pharmaceutical composition comprising an osmolyte, a pH adjusting agent, a histidine buffer, and a non-naturally occurring melanocortin antagonist analog having an isoelectric point of at least about 10 and comprising a cyclic region with an arginine residue positioned therein, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal- dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0249] 10. A pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an isoelectric point of about 10 to about 12.5 and a pharmaceutically acceptable carrier comprising an osmolyte, a pH adjusting agent, and a histidine buffer, wherein the non-naturally occurring melanocortin antagonist analog comprises moiety (A):XI-RI-C(R2-R3-R4-R5-R6-R7)-YI (A), wherein:Ri is absent or is an amino acid or amino acid derivative;R4 is selected from the group consisting of optionally substituted dNal(2’), Phe, dPhe, Bip and dBip; at least one of R2-R7 is a cationic amino acid residue;Docket No. 183B-412975-WOXi is an optionally present N-terminus;Yi is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a backbone or side chain linkage between R2 and R7, provided that: if one of R2-R7 is an anionic residue, then (i) one of R2 and R7 is the anionic residue and the other is a cationic residue, and the non-naturally occurring melanocortin analog is cyclized through a side-chain linkage between R2 and R7; or (ii) the at least one of R2-R7 that is the cationic residue is deprotonated in the pharmaceutical composition, and moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0250] 11 . The pharmaceutical composition or pharmaceutical formulation of any one of embodiments 8-10, wherein the pharmaceutical composition or the pharmaceutical formulation has a pH of about 4.0 to about 6.5.

[0251] 12. A pharmaceutical formulation having a pH of about 4.0 to about 6.5 and comprising a non-naturally occurring melanocortin antagonist analog, the formulation produced by: combining an aqueous peptide composition comprising the antagonist analog, and a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 11 .0 comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical formulation such that no local region of the analog has a pH equal to the isoelectric point of the antagonist analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5 and does not comprise a sequence of Ac-Nle-c[Asp-Pro- dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.Docket No. 183B-412975-WO

[0252] 13. A pharmaceutical formulation having a pH of about 4.0 to about 6.5 and comprising a non-naturally occurring melanocortin antagonist analog, the formulation produced by combining: an aqueous peptide composition comprising the non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of at least about 10, and a pharmaceutically acceptable carrier composition comprising a base and a buffer and having a pH of about 5.5 to about 7.0, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0253] 14. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 5, 8, and 13, wherein the non-naturally occurring melanocortin antagonist analog has a cyclic region and the arginine residue is positioned in the cyclic region.

[0254] 15. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -8 and 1 1 -14, wherein the buffer comprises one or more of sodium acetate, histidine, Tris, arginine, MES, ADA, PIPES, ACES, MOPSO, MOPS, Bes, TES, HEPES, DIPSO, TAPSO, POPSO, HEPPSO, HEPPS, TPAS, acetoamidoglycine, glycinamide, glycylglycine, tricine, and bicine.

[0255] 16. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -8 and 11 -15, wherein the buffer is present at a concentration of about 10 mM to about 200 mM.

[0256] 17. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -8 and 11 -15, wherein the buffer comprises histidine.

[0257] 18. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 9, 10, and 17, wherein the histidine buffer comprises about 5 mM to about 150 mM histidine.Docket No. 183B-412975-WO

[0258] 19. The pharmaceutical composition or the pharmaceutical formulation of embodiment 14 or 17, wherein the histidine buffer comprises about 10 mM to about 25 mM histidine.

[0259] 20. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -8 and 11 -15, wherein the buffer comprises sodium acetate.

[0260] 21 . The pharmaceutical composition or the pharmaceutical formulation of embodiment 20, wherein the sodium acetate buffer comprises about 5 mM to about 150 mM sodium acetate.

[0261] 22. The pharmaceutical composition or the pharmaceutical formulation of embodiment 20 or 21 , wherein the sodium acetate buffer comprises about 10 mM to about 25 mM sodium acetate.

[0262] 23. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -22, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 10 mg / mL to about 130 mg / mL.

[0263] 24. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -23, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 10 mg / mL to about 50 mg / mL.

[0264] 25. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -24, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 12.5 mg / mL.

[0265] 26. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -24, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 25 mg / mL.

[0266] 27. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -24, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 50 mg / mL.

[0267] 28. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -23, wherein the osmolyte is selected from the group consistingDocket No. 183B-412975-WO of a sugar or derivative thereof, a glycerol, a glycerin, a gelatin, a propylene glycol, a propylparaben, PVP, PLGA, and PEG.

[0268] 29. The pharmaceutical composition or pharmaceutical formulation of embodiment 28, wherein the sugar or the derivative thereof is a sugar alcohol.

[0269] 30. The pharmaceutical composition or pharmaceutical formulation of embodiment 29, where the sugar alcohol is mannitol.

[0270] 31. The pharmaceutical composition or pharmaceutical formulation of embodiment 30, wherein the mannitol is present in an amount of about 20 mg / mL to about 40 mg / mL.

[0271] 32. The pharmaceutical composition or pharmaceutical formulation of embodiment 30, wherein the mannitol is present in an amount of about 25 mg / mL.

[0272] 33. The pharmaceutical composition or pharmaceutical formulation of embodiment 30, wherein the mannitol is present in an amount of about 27.5 mg / mL.

[0273] 34. The pharmaceutical composition or pharmaceutical formulation of embodiment 30, wherein the mannitol is present in an amount of about 35 mg / mL.

[0274] 35. The pharmaceutical composition or pharmaceutical formulation of embodiment 30, wherein the mannitol is present in an amount of about 37.5 mg / mL.

[0275] 36. The pharmaceutical composition of formulation of any one of embodiments 1 -35, wherein the pH adjusting agent is present in an amount of about 0.01 mg / mL to about 10 mg / mL.

[0276] 37. The pharmaceutical composition or formulation of any one of embodiments 1 -36, wherein the pH adjusting agent is a base.

[0277] 38. The pharmaceutical composition or formulation of embodiment 37, wherein the base is sodium hydroxide.

[0278] 39. The pharmaceutical composition or formulation of embodiment 38, wherein the sodium hydroxide is present in an amount of about 0.01 mg / mL to about 5.0 mg / L.Docket No. 183B-412975-WO

[0279] 40. The pharmaceutical composition or formulation of embodiment 38 or39, wherein the sodium hydroxide is present in an amount of about 0.4 mg / mL.

[0280] 41 . The pharmaceutical composition or formulation of embodiment 38 or39, wherein the sodium hydroxide is present in an amount of about 1 .2 mg / mL.

[0281] 42. The pharmaceutical composition or formulation of embodiment 38 or39, wherein the sodium hydroxide is present in an amount of about 1 .6 mg / mL.

[0282] 43. The pharmaceutical composition or formulation of embodiment 37, wherein the base is histidine.

[0283] 44. The pharmaceutical composition or formulation of embodiment 43, wherein the histidine is present in an amount of about 0.01 mg / mL to about 5.0 mg / L.

[0284] 45. The pharmaceutical composition or formulation of any one of embodiments 1 -35, wherein the pH adjusting agent is an acid.

[0285] 46. The pharmaceutical composition or formulation of embodiment 45, wherein the acid is glacial acetic acid.

[0286] 47. The pharmaceutical composition or formulation of embodiment 46, wherein the glacial acetic acid is present in an amount of about 0.01 mg / mL to about 5.0 mg / mL.

[0287] 48. The pharmaceutical composition or formulation of any one of embodiments 1 -47, further comprising a surfactant.

[0288] 49. The pharmaceutical composition or formulation of embodiment 48, wherein the surfactant is selected from an alkyl-carboxylate-fatty acid salt, a sulfate, a sulfonate, a phosphate ester, a quaternary ammonium surfactant, a pyridinium surfactant, a polyol ester, a polyoxyethylene ester, a poloxamer, a phospholipid, and a betaine.

[0289] 50. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -49, further comprising substantially no calcium ions.

[0290] 51 . The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 1 -50, further comprising substantially no metal ions.Docket No. 183B-412975-WO

[0291] 52. The pharmaceutical composition or formulation of any one of embodiments 1 -51 , further comprising a preservative.

[0292] 53. The pharmaceutical composition or formulation of embodiment 52, wherein the preservative is selected from the group consisting of m-cresol, phenol, and benzyl alcohol.

[0293] 54. The pharmaceutical composition or formulation of embodiment 52 or53, wherein the preservative is present in an amount of about 0.1 wt% to about 1.0 wt%, relative to a total weight of the composition or formulation.

[0294] 55. A method of producing a pharmaceutical composition of a non-naturally occurring melanocortin antagonist analog, the method comprising combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 with a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 11 .0 and comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal- dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0295] 56. A method of producing a pharmaceutical formulation having a pH of about 4.0 to about 6.5, the method comprising: combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical composition such that no local region has a pH that is equal to the isoelectric point of the antagonist analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5 and does not comprise a sequence of Ac-Nle-c[Asp-Pro- dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization viaDocket No. 183B-412975-WO a lactam bond, and the pharmaceutically acceptable carrier composition has a pH of about5.5 to about 11 .0.

[0296] 57. A method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog having a pH of about 4.0 to about 6.5, the method comprising combining an aqueous peptide composition of the non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog has an arginine residue and an isoelectric point of at least about 10 and does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp- Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond, and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 1 1.0.

[0297] 58. A method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog, the method comprising: providing a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a histidine buffer; dissolving a non-naturally melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 in water to provide an aqueous peptide composition; and adding the pharmaceutically acceptable carrier composition to the aqueous peptide composition while mixing to maintain dissolution of the non-naturally occurring melanocortin antagonist analog, wherein the pharmaceutical formulation has a pH of about 4.0 to about6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

[0298] 59. The method of any one of embodiment 55-57, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition through a semi-permeable, size-selective membrane.Docket No. 183B-412975-WO

[0299] 60. The method of embodiment 59, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises tangential flow filtration.

[0300] 61 . The method of any one of embodiment 55-57, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises adding the pharmaceutically acceptable carrier composition to the aqueous peptide composition.

[0301] 62. The method of any one of embodiment 55-57, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises adding the aqueous peptide composition to the pharmaceutically acceptable carrier composition.

[0302] 63. The method of any one of embodiments 55-62, wherein the pharmaceutical composition contains substantially no precipitated non-naturally occurring melanocortin antagonist analog.

[0303] 64. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 55-57 and 56-62, wherein the buffer comprises one or more of sodium acetate, histidine, Tris, arginine, MES, ADA, PIPES, ACES, MOPSO, MOPS, Bes, TES, HEPES, DIPSO, TAPSO, POPSO, HEPPSO, HEPPS, TPAS, acetoamidoglycine, glycinamide, glycylglycine, tricine, and bicine.

[0304] 65. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 55-57 and 56-63, wherein the buffer is present at a concentration of about 10 mM to about 200 mM.

[0305] 66. The method of any one of embodiments 55-57 and 56-64, wherein the buffer comprises histidine.

[0306] 67. The method of embodiment 66, wherein the histidine buffer comprises about 5 mM to about 150 mM histidine.

[0307] 68. The method of embodiment 66 or 67, wherein the histidine buffer comprises about 10 mM to about 25 mM histidine.Docket No. 183B-412975-WO

[0308] 69. The method of any one of embodiments 55-57 and 56-64, wherein the buffer comprises sodium acetate.

[0309] 70. The method of embodiment 69, wherein the sodium acetate buffer comprises about 5 mM to about 150 mM sodium acetate.

[0310] 71 . The method of embodiment 69 or 70, wherein the sodium acetate buffer comprises about 10 mM to about 25 mM sodium acetate.

[0311] 72. The method of any one of embodiments 55-71 , wherein the aqueous peptide composition comprises the non-naturally occurring melanocortin antagonist analog at a concentration of about 10 mg / mL to about 130 mg / mL.

[0312] 73. The pharmaceutical composition or the pharmaceutical formulation of any one of embodiments 55-72, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 10 mg / mL to about 50 mg / mL.

[0313] 74. The method of any one of embodiments 55-73, wherein the non- naturally occ...

Claims

1. Docket No. 183B-412975-WOCLAIMS l / We claim:

1. A pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

2. A pharmaceutical composition having a pH of about 4.0 to about 6.5, comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue and no anionic amino acid residues, an osmolyte, a pH adjusting agent, and a buffer, wherein at least one of the one or more cationic amino acid residues is protonated and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

3. A pharmaceutical composition comprising a cyclic non-naturally occurring melanocortin antagonist analog having at one cationic amino acid residue, an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

4. A pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having at least one cationic amino acid residue and an isoelectric point of about 10 to about 12.5, an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturallyDocket No. 183B-412975-WO occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp- Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

5. A pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of at least about 10, an osmolyte, a pH adjusting agent, and a buffer wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp- Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

6. A pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having a cyclic region with an arginine residue positioned therein and an isoelectric point of at least about 10 and a pharmaceutically acceptable carrier comprising a base and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

7. A pharmaceutical composition having a pH of about 4.0 to about 6.5, the pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an isoelectric point of at least about 10 and a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog comprises moiety (A):X1-R1-R2-R3-R4-R5-R6-R7-Y1 (A), wherein:R1 is absent or is an amino acid or amino acid derivative;R4 is selected from the group consisting of optionally substituted dNal(2’), Phe, dPhe, Bip and dBip; at least one of R2-R7 is a cationic amino acid residue;Xi is an optionally present N-terminus;Docket No. 183B-412975-WOYi is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a side chain linkage between R2 and R7; provided that: moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

8. A pharmaceutical formulation comprising a peptide composition and a pharmaceutically acceptable carrier composition, the peptide composition comprising a non- naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 in an aqueous solution, the pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

9. A pharmaceutical composition comprising an osmolyte, a pH adjusting agent, a histidine buffer, and a non-naturally occurring melanocortin antagonist analog having an isoelectric point of at least about 10 and comprising a cyclic region with an arginine residue positioned therein, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

10. A pharmaceutical composition comprising a non-naturally occurring melanocortin antagonist analog having an isoelectric point of about 10 to about 12.5 and a pharmaceutically acceptable carrier comprising an osmolyte, a pH adjusting agent, and a histidine buffer, wherein the non-naturally occurring melanocortin antagonist analog comprises moiety (A):XI-RI-C(R2-R3-R4-R5-R6-R7)-YI (A), wherein:R1 is absent or is an amino acid or amino acid derivative;Docket No. 183B-412975-WOF is selected from the group consisting of optionally substituted dNal(2’), Phe, dPhe, Bip and dBip; at least one of R2-R7 is a cationic amino acid residue;Xi is an optionally present N-terminus;Y1 is a C-terminus comprising one to four amino acids or amino acid derivatives; and the non-naturally occurring melanocortin analog is optionally cyclized via a backbone or side chain linkage between R2 and R7, provided that: if one of R2-R7 is an anionic residue, then (i) one of R2 and R7 is the anionic residue and the other is a cationic residue, and the non-naturally occurring melanocortin analog is cyclized through a side-chain linkage between R2 and R7; or (ii) the at least one of R2-R7 that is the cationic residue is deprotonated in the pharmaceutical composition, and moiety (A) is not Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.1 1 . The pharmaceutical composition or pharmaceutical formulation of any one of claims 8-10, wherein the pharmaceutical composition or the pharmaceutical formulation has a pH of about 4.0 to about 6.5.

12. A pharmaceutical formulation having a pH of about 4.0 to about 6.5 and comprising a non-naturally occurring melanocortin antagonist analog, the formulation produced by: combining an aqueous peptide composition comprising the antagonist analog, and a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 11 .0 comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical formulation such that no local region of the analog has a pH equal to the isoelectric point of the antagonist analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5 and does not comprise a sequence of Ac-Nle-c[Asp-Pro-Docket No. 183B-412975-WO dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

13. A pharmaceutical formulation having a pH of about 4.0 to about 6.5 and comprising a non-naturally occurring melanocortin antagonist analog, the formulation produced by combining: an aqueous peptide composition comprising the non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of at least about 10, and a pharmaceutically acceptable carrier composition comprising a base and a buffer and having a pH of about 5.5 to about 7.0, wherein the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

14. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 5, 8, and 13, wherein the non-naturally occurring melanocortin antagonist analog has a cyclic region and the arginine residue is positioned in the cyclic region.

15. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -8 and 11 -14, wherein the buffer comprises one or more of sodium acetate, histidine, Tris, arginine, MES, ADA, PIPES, ACES, MOPSO, MOPS, Bes, TES, HEPES, DIPSO, TAPSO, POPSO, HEPPSO, HEPPS, TPAS, acetoamidoglycine, glycinamide, glycylglycine, tricine, and bicine.

16. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -8 and 1 1 -15, wherein the buffer is present at a concentration of about 10 mM to about 200 mM.

17. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -8 and 1 1 -15, wherein the buffer comprises histidine.Docket No. 183B-412975-WO18. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 9, 10, and 17, wherein the histidine buffer comprises about 5 mM to about 150 mM histidine.

19. The pharmaceutical composition or the pharmaceutical formulation of claim 14 or 17, wherein the histidine buffer comprises about 10 mM to about 25 mM histidine.

20. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -8 and 1 1 -15, wherein the buffer comprises sodium acetate.21 . The pharmaceutical composition or the pharmaceutical formulation of claim 20, wherein the sodium acetate buffer comprises about 5 mM to about 150 mM sodium acetate.

22. The pharmaceutical composition or the pharmaceutical formulation of claim 20 or 21 , wherein the sodium acetate buffer comprises about 10 mM to about 25 mM sodium acetate.

23. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -22, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 10 mg / mL to about 130 mg / mL.

24. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -23, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 10 mg / mL to about 50 mg / mL.

25. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -24, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 12.5 mg / mL.Docket No. 183B-412975-WO26. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -24, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 25 mg / mL.

27. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -24, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 50 mg / mL.

28. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -23, wherein the osmolyte is selected from the group consisting of a sugar or derivative thereof, a glycerol, a glycerin, a gelatin, a propylene glycol, a propylparaben, PVP, PLGA, and PEG.

29. The pharmaceutical composition or pharmaceutical formulation of claim 28, wherein the sugar or the derivative thereof is a sugar alcohol.

30. The pharmaceutical composition or pharmaceutical formulation of claim 29, where the sugar alcohol is mannitol.

31. The pharmaceutical composition or pharmaceutical formulation of claim 30, wherein the mannitol is present in an amount of about 20 mg / mL to about 40 mg / mL.

32. The pharmaceutical composition or pharmaceutical formulation of claim 30, wherein the mannitol is present in an amount of about 25 mg / mL.

33. The pharmaceutical composition or pharmaceutical formulation of claim 30, wherein the mannitol is present in an amount of about 27.5 mg / mL.

34. The pharmaceutical composition or pharmaceutical formulation of claim 30, wherein the mannitol is present in an amount of about 35 mg / mL.Docket No. 183B-412975-WO35. The pharmaceutical composition or pharmaceutical formulation of claim 30, wherein the mannitol is present in an amount of about 37.5 mg / mL.

36. The pharmaceutical composition of formulation of any one of claims 1 -35, wherein the pH adjusting agent is present in an amount of about 0.01 mg / mL to about 10 mg / mL.

37. The pharmaceutical composition or formulation of any one of claims 1 -36, wherein the pH adjusting agent is a base.

38. The pharmaceutical composition or formulation of claim 37, wherein the base is sodium hydroxide.

39. The pharmaceutical composition or formulation of claim 38, wherein the sodium hydroxide is present in an amount of about 0.01 mg / mL to about 5.0 mg / L.

40. The pharmaceutical composition or formulation of claim 38 or 39, wherein the sodium hydroxide is present in an amount of about 0.4 mg / mL.41 . The pharmaceutical composition or formulation of claim 38 or 39, wherein the sodium hydroxide is present in an amount of about 1 .2 mg / mL.

42. The pharmaceutical composition or formulation of claim 38 or 39, wherein the sodium hydroxide is present in an amount of about 1 .6 mg / mL.

43. The pharmaceutical composition or formulation of claim 37, wherein the base is histidine.

44. The pharmaceutical composition or formulation of claim 43, wherein the histidine is present in an amount of about 0.01 mg / mL to about 5.0 mg / L.Docket No. 183B-412975-WO45. The pharmaceutical composition or formulation of any one of claims 1 -35, wherein the pH adjusting agent is an acid.

46. The pharmaceutical composition or formulation of claim 45, wherein the acid is glacial acetic acid.

47. The pharmaceutical composition or formulation of claim 46, wherein the glacial acetic acid is present in an amount of about 0.01 mg / mL to about 5.0 mg / mL.

48. The pharmaceutical composition or formulation of any one of claims 1 -47, further comprising a surfactant.

49. The pharmaceutical composition or formulation of claim 48, wherein the surfactant is selected from an alkyl-carboxylate-fatty acid salt, a sulfate, a sulfonate, a phosphate ester, a quaternary ammonium surfactant, a pyridinium surfactant, a polyol ester, a polyoxyethylene ester, a poloxamer, a phospholipid, and a betaine.

50. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -49, further comprising substantially no calcium ions.51 . The pharmaceutical composition or the pharmaceutical formulation of any one of claims 1 -50, further comprising substantially no metal ions.

52. The pharmaceutical composition or formulation of any one of claims 1 -51 , further comprising a preservative.

53. The pharmaceutical composition or formulation of claim 52, wherein the preservative is selected from the group consisting of m-cresol, phenol, and benzyl alcohol.Docket No. 183B-412975-WO54. The pharmaceutical composition or formulation of claim 52 or 53, wherein the preservative is present in an amount of about 0.1 wt% to about 1 .0 wt%, relative to a total weight of the composition or formulation.

55. A method of producing a pharmaceutical composition of a non-naturally occurring melanocortin antagonist analog, the method comprising combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 with a pharmaceutically acceptable carrier composition having a pH of about 5.5 to about 11 .0 and comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the pharmaceutical composition has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal- dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

56. A method of producing a pharmaceutical formulation having a pH of about 4.0 to about 6.5, the method comprising: combining an aqueous peptide composition of a non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer; and preventing aggregation of the antagonist analog by maintaining a local pH of the pharmaceutical composition such that no local region has a pH that is equal to the isoelectric point of the antagonist analog while the aqueous peptide composition and the pharmaceutically acceptable carrier composition are being combined, wherein the antagonist analog has at least one cationic residue and an isoelectric point of about 10 to about 12.5 and does not comprise a sequence of Ac-Nle-c[Asp-Pro- dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond, and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 11 .0.

57. A method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog having a pH of about 4.0 to about 6.5, the methodDocket No. 183B-412975-WO comprising combining an aqueous peptide composition of the non-naturally occurring melanocortin antagonist analog with a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a buffer, wherein the non-naturally occurring melanocortin antagonist analog has an arginine residue and an isoelectric point of at least about 10 and does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp- Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond, and the pharmaceutically acceptable carrier composition has a pH of about 5.5 to about 1 1.0.

58. A method of producing a pharmaceutical formulation of a non-naturally occurring melanocortin antagonist analog, the method comprising: providing a pharmaceutically acceptable carrier composition comprising an osmolyte, a pH adjusting agent, and a histidine buffer; dissolving a non-naturally melanocortin antagonist analog having an arginine residue and an isoelectric point of about 10 to about 12.5 in water to provide an aqueous peptide composition; and adding the pharmaceutically acceptable carrier composition to the aqueous peptide composition while mixing to maintain dissolution of the non-naturally occurring melanocortin antagonist analog, wherein the pharmaceutical formulation has a pH of about 4.0 to about 6.5 and the non-naturally occurring melanocortin antagonist analog does not comprise a sequence of Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 2), wherein c represents cyclization via a lactam bond.

59. The method of any one of claim 55-57, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition through a semi-permeable, size-selective membrane.

60. The method of claim 59, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises tangential flow filtration.Docket No. 183B-412975-WO61 . The method of any one of claim 55-57, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises adding the pharmaceutically acceptable carrier composition to the aqueous peptide composition.

62. The method of any one of claim 55-57, wherein combining the aqueous peptide composition and the pharmaceutically acceptable carrier composition comprises adding the aqueous peptide composition to the pharmaceutically acceptable carrier composition.

63. The method of any one of claims 55-62, wherein the pharmaceutical composition contains substantially no precipitated non-naturally occurring melanocortin antagonist analog.

64. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 55-57 and 56-62, wherein the buffer comprises one or more of sodium acetate, histidine, Tris, arginine, MES, ADA, PIPES, ACES, MOPSO, MOPS, Bes, TES, HEPES, DIPSO, TAPSO, POPSO, HEPPSO, HEPPS, TPAS, acetoamidoglycine, glycinamide, glycylglycine, tricine, and bicine.

65. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 55-57 and 56-63, wherein the buffer is present at a concentration of about 10 mM to about 200 mM.

66. The method of any one of claims 55-57 and 56-64, wherein the buffer comprises histidine.

67. The method of claim 66, wherein the histidine buffer comprises about 5 mM to about 150 mM histidine.Docket No. 183B-412975-WO68. The method of claim 66 or 67, wherein the histidine buffer comprises about 10 mM to about 25 rnM histidine.

69. The method of any one of claims 55-57 and 56-64, wherein the buffer comprises sodium acetate.

70. The method of claim 69, wherein the sodium acetate buffer comprises about 5 mM to about 150 mM sodium acetate.71 . The method of claim 69 or 70, wherein the sodium acetate buffer comprises about 10 mM to about 25 mM sodium acetate.

72. The method of any one of claims 55-71 , wherein the aqueous peptide composition comprises the non-naturally occurring melanocortin antagonist analog at a concentration of about 10 mg / mL to about 130 mg / mL.

73. The pharmaceutical composition or the pharmaceutical formulation of any one of claims 55-72, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 10 mg / mL to about 50 mg / mL.

74. The method of any one of claims 55-73, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 12.5 mg / mL.

75. The method of any one of claims 55-73, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 25 mg / mL.

76. The method of any one of claims 55-73, wherein the non-naturally occurring melanocortin antagonist analog is present at a concentration of about 50 mg / mL.Docket No. 183B-412975-WO77. The method of any one of claims 55-76, wherein the osmolyte is selected from the group consisting of a sugar or derivative thereof, a glycerol, a glycerin, a gelatin, a propylene glycol, a propylparaben, PVP, PLGA, and PEG.

78. The method of claim 77, wherein the sugar or the derivative thereof is a sugar alcohol.

79. The method of claim 78, wherein the sugar alcohol is mannitol.

80. The method of claim 79, wherein the mannitol is present in an amount of about 20 mg / mL to about 40 mg / mL.81 . The method of claim 80, wherein the mannitol is present in an amount of about 25 mg / mL.

82. The method of claim 80, wherein the mannitol is present in an amount of about27.5 mg / mL.

83. The method of claim 80, wherein the mannitol is present in an amount of about 35 mg / mL.

84. The method of claim 80, wherein the mannitol is present in an amount of about37.5 mg / mL.

85. The pharmaceutical composition of formulation of any one of claims 1 -84, wherein the pH adjusting agent is present in an amount of about 0.01 mg / mL to about 10 mg / mL.

86. The method of any one of claims 55-85, wherein the pH adjusting agent is a base.Docket No. 183B-412975-WO87. The method of claim 86, wherein the base is sodium hydroxide.

88. The method of claim 87, wherein the sodium hydroxide is present in an amount of about 0.01 mg / mL to about 5.0 mg / L.

89. The method of claim 87 or 88, wherein the sodium hydroxide is present in an amount of about 0.4 mg / mL.

90. The method of claim 87 or 88, wherein the sodium hydroxide is present in an amount of about 1 .2 mg / mL.91 . The method of claim 87 or 88, wherein the sodium hydroxide is present in an amount of about 1 .6 mg / mL.

92. The method of claim 86, wherein the base is histidine.

93. The method of claim 92, wherein the histdine is present in an amount of about 0.01 mg / mL to about 5.0 mg / L.

94. The method of any one of claims 1 -84, wherein the pH adjusting agent is an acid.

95. The method of claim 94, wherein the acid is glacial acetic acid.

96. The method of claim 95, wherein the glacial acetic acid is present in an amount of about 0.01 mg / mL to about 5.0 mg / mL.

97. The method of any one of claims 55-96, wherein the pharmaceutical composition or formulation further comprises a surfactant.Docket No. 183B-412975-WO98. The method of claim 97, wherein the surfactant is selected from an alkylcarboxylate-fatty acid salt, a sulfate, a sulfonate, a phosphate ester, a quaternary ammonium surfactant, a pyridinium surfactant, a polyol ester, a polyoxyethylene ester, a poloxamer, a phospholipid, and a betaine.

99. The method of any one of claims 55-98, wherein the pharmaceutically acceptable carrier composition comprises substantially no calcium ions.

100. The method any one of claims 55-99, wherein the pharmaceutically acceptable carrier composition comprises substantially no metal ions.

101. The method of any one of claims 55-100, wherein the pharmaceutical composition or formulation further comprises a preservative.

102. The method of claim 101 , wherein the preservative is selected from the group consisting of m-cresol, phenol, and benzyl alcohol.

103. The method of claim 101 or 102, wherein the preservative is present in the pharmaceutical composition or formulation in an amount of about 0.1 wt% to about 1 .0 wt%, relative to a total weight of the composition or formulation.

104. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -103, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (I):X1-X2- R1- R2- R3- R4- R5- R6- R7- R8- R9- Y1- Y2- Y3- Y4- Y5- Y6- Y7( I ) , wherein:X1is absent or norlecuine (Nle);X2is absent, Nle, or phenylalanine (Phe);R1is selected from the group consisting of Nle, Phe, trans-4-guanidinyl-proline (transPro(guan)), cis-4-guanidinyl-proline (cisPro(guan)), arginine (Arg), D-arginine (dArg), D-methionine (dMet), D-isoleucine (dlle), D-leucine (dLeu), D-valine (dVal), D-alanineDocket No. 183B-412975-WO(dAla), alanine (Ala), tertleucine (Tie), D-tertleucine (dTle), D-norleucine (dNIe), norvaline (Nva), glycine (Gly), D-cysteine (dCys), D-phenylalanine (dPhe), tyrosine (Tyr), D-tyrosine (dTyr), D-glutamine (dGIn), D-asparagine (dAsn), dimethyltyrosine (Dmt), glutamic acid (Glu), lysine (Lys), D-lysine (dLys), histidine (His), D-histidine (dHis), and D-proline (dPro);R2is selected from the group consisting of dCys, aspartic acid (Asp), D-aspartic acid (dAsp), penicillamine (Pen), D-penicillamine (dPen), Glu, and cysteine (Cys);R3is absent or selected from the group consisting of proline (Pro), octohydroindole- 2-carboxylic acid (Oic), phenylalanyl-histidine (Phe-His), prolyl-histidine (Pro-His), phenylalanyl-phenylalanine (Phe-Phe), transPro(guan), cisPro(guan), 4-amino-1 ,2,4,5- tetrahydro-2-benzazepin-3-one (Aba), 4-amino-1 ,4,5,6-tetrahydroazepino[4,3-b]indol- 3(2H)-one (Aia), 7-amino-7,8-dihydro-4H-[1 ,2,3]triazolo-[1 ,5-a][1 ,4]diazepin-6(5H)-one (Ata), 2-aminoindone-2-carboxylic acid (Aic), D-alanyl-histidine (dAla-His), histidine (His), dHis, Ala, Gly, leucine (Leu), isoleucine (lie), valine (Vai), histidyl-arginine (His-Arg), prolylarginine (Pro-Arg), indoline-2-carboxylic acid (loc), 1 ,2,3,4-tetrahydroisoquinoline-3- carboxylic acid (Tic), Glu, glutamyl-histidine (Glu-His), alanyl-histidine (Ala-His), Phe, biphenylalanine (Bip), tryptophan (Trp), Tyr, glutamine (Gin), and hydroxyproline (Hyp);R4is selected from the group consisting of Pro, D-2’-naphthylalanine (dNal(2’)), D- phenylalanine (dPhe), para-iodo-D-phenylalanine (p(l)dPhe), para-bromo-D-phenylalanine (p(Br)dPhe), para-fluoro-D-phenylalanine (p(F)dPhe), para-trifluoromethyl-D-phenylalanine (p(CFs)dPhe), and para-chloro-D-phenylalanine (p(CI)dPhe);R5is absent, or selected from the group consisting of transPro(guan), cisPro(guan), Lys, ornithine (Orn), His, Ala, and Arg;R6is selected from the group consisting Trp, tryptyl-proline (Trp-Pro), tryptyl-glycine (Trp-Gly), D-tryptophan (dTrp), dNal(2’), Aia, Aba, Ata, T-napthylalanine (Nal(1 ’)), Phe, Tyr, dPhe, dTyr, 2’-napthylalanine (Nal(2’)), D-T-naphthylalanine (dNal(1 ’)), and Tic;R7is absent or selected from the group consisting of Arg, Lys, dLys, Cys, dCys, Orn, D-ornithine (dOrn), Pen, and dPen;R8is absent or Trp;R9is absent or Lys;Y1is absent or selected from the group consisting of Vai, dVal, dLeu, d He, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Docket No. 183B-412975-WOY2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and a lactam bond between R2and R9, when R2is Asp and R9is Lys; provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then either (i) R3is Pro, R4is dNal(2’) or p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn or dOrn, or (ii) R3is His and R4is p(Br)dPhe and when R1is Arg, then R3is His or Pro-His, when R4is dPhe, then either R3is Oic or R6is dNal(2’), when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R5is Arg or His, R6is not dTrp, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent and, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn,Docket No. 183B-412975-WO when R4is p(F)dPhe, then R3is Pro, Trp, or Tyr, wherein when R3is Pro, then either (i) R2is Cys or (ii) R6is dNal(2’), when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal, when R4is dNal(2’) and R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated, (iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly, (iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from transPro(guan), cisPro(guan), Arg, dArg, dMet, dlle, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, and when R4is dNal(2’) and R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Asp or Glu, and R5is selected from transPro(guan), cisPro(guan), and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Phe-His, Hyp, Pro-His, Phe- Phe, transPro(guan), cisPro(guan), Aba, Aia, Ata, Aic, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, lie, Vai, and Trp.

105. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -104, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (I), wherein:X1is absent or norlecuine (Nle);X2is absent, Nle, or phenylalanine (Phe);R1is selected from the group consisting of Nle, Phe, trans-4-guanidinyl-proline (transPro(guan)), cis-4-guanidinyl-proline (cisPro(guan)), arginine (Arg), D-arginine (dArg), D-methionine (dMet), D-isoleucine (dlle), D-leucine (dLeu), D-valine (dVal), D-alanine (dAla), alanine (Ala), tertleucine (Tie), D-tertleucine (dTle), D-norleucine (dNIe), norvaline (Nva), glycine (Gly), D-cysteine (dCys), D-phenylalanine (dPhe), tyrosine (Tyr), D-tyrosineDocket No. 183B-412975-WO(dTyr), D-glutamine (dGIn), D-asparagine (dAsn), dimethyltyrosine (Dmt), glutamic acid (Glu), lysine (Lys), D-lysine (dLys), histidine (His), D-histidine (dHis), and D-proline (dPro);R2is selected from the group consisting of dCys, aspartic acid (Asp), D-aspartic acid (dAsp), penicillamine (Pen), D-penicillamine (dPen), Glu, and cysteine (Cys);R3is absent or selected from the group consisting of proline (Pro), octohydroindole- 2-carboxylic acid (Oic), phenylalanyl-histidine (Phe-His), prolyl-histidine (Pro-His), phenylalanyl-phenylalanine (Phe-Phe), transPro(guan), cisPro(guan), 4-amino-1 ,2,4,5- tetrahydro-2-benzazepin-3-one (Aba), 4-amino-1 ,4,5,6-tetrahydroazepino[4,3-b]indol- 3(2H)-one (Aia), 7-amino-7,8-dihydro-4H-[1 ,2,3]triazolo-[1 ,5-a][1 ,4]diazepin-6(5H)-one (Ata), 2-aminoindone-2-carboxylic acid (Aic), D-alanyl-histidine (dAla-His), histidine (His), dHis, Ala, Gly, leucine (Leu), isoleucine (lie), valine (Vai), histidyl-arginine (His-Arg), prolylarginine (Pro-Arg), indoline-2-carboxylic acid (loc), 1 ,2,3,4-tetrahydroisoquinoline-3- carboxylic acid (Tic), Glu, glutamyl-histidine (Glu-His), alanyl-hsitidine (Ala-His), Phe, biphenylalanine (Bip), tryptophan (Trp), Tyr, glutamine (Gin), and hydroxyproline (Hyp);R4is selected from the group consisting of Pro, D-2’-naphthylalanine (dNal(2’)), D- phenylalanine (dPhe), para-iodo-D-phenylalanine (p(l)dPhe), para-bromo-D-phenylalanine (p(Br)dPhe), para-fluoro-D-phenylalanine (p(F)dPhe), para-trifluoromethyl-D-phenylalanine (p(CFs)dPhe), and parachloro-D-phenylalanine (p(CI)dPhe);R5is absent, or selected from the group consisting of transPro(guan), cisPro(guan), Lys, ornithine (Orn), His, Ala, and Arg;R6is selected from the group consisting Trp, D-tryptophan (dTrp), dNal(2’), Aia, Aba, Ata, T-napthylalanine (Nal(T)), Phe, Tyr, dPhe, dTyr, 2’-napthylalanine (Nal(2’)), D-1 ’- naphthylalanine (dNal(T)), and Tic;R7is absent or selected from the group consisting of Arg, Pro, Gly, Lys, dLys, Cys, dCys, Orn, D-ornithine (dOrn), Pen, and dPen;R8is absent, Trp, or Lys;R9is absent or Lys;Y1is absent or selected from the group consisting of Vai, dVal, dLeu, d He, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Docket No. 183B-412975-WOY3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and a lactam bond between R2and R9, when R2is Asp and R9is Lys, provided that the non-naturally occurring melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEO ID NO: 3);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 4);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 6);Ac-Nle-c[Glu-His-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 7);Ac-dGln-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dGln-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 9);Docket No. 183B-412975-WOAc-dGln-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 10);Ac-dGln-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 1 1 );Ac-dAsn-c[Glu-Pro-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-dAsn-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 13);Ac-dAsn-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 14);Ac-dAsn-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 15);Ac-Nle-c[Glu-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 16);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 17);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Ac-Ala-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 19);Ac-Ala-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 20);Ac-Ala-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 21 );Ac-Nle-c[Glu-Oic-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 22);Ac-Nle-c[Glu-Oic-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 23);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Dmt-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 25);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Ac-dAla-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 27);Ac-dAla-c[Glu-His-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 28);Ac-dAla-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 29);Ac-Nle-c[Glu-Pro-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 31 );Ac-Nle-c[Glu-His-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 32);Ac-Nle-c[Glu-His-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 33);Docket No. 183B-412975-WOAc-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 34);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 35);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 37);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 38);Ac-Arg-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 39);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 40);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Glu-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 42);Ac-Nle-c[Asp-Trp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 43);Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 44);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 45);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 46);Ac-Nle-c[Asp-Aba-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 47);Ac-Nle-c[Asp-Aia-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 48);Ac-Nle-c[Asp-Ata-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 49);Ac-Nle-c[Asp-His-dPhe-transPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 50);Ac-Nle-c[Asp-His-dPhe-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 51 );Ac-Nle-c[Asp-Pro-dPhe-transPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 52);Ac-Nle-c[Asp-Pro-dPhe-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 53);Ac-Nle-c[Asp-Pro-dPhe-Arg-Aia-Lys]-dVal-dPro-NH2(SEQ ID NO: 54);Ac-Nle-c[Asp-Pro-dPhe-Arg-Aba-Lys]-dVal-dPro-NH2(SEQ ID NO: 55);Ac-Nle-c[Asp-Pro-dPhe-Arg-Ata-Lys]-dVal-dPro-NH2(SEQ ID NO: 56);Ac-Nle-c[Asp-Pro-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 57);Docket No. 183B-412975-WOAc-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 58);Ac-dLeu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 59);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 60);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 61 );Ac-dNle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 62);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 63);Ac-dTyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 64);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 65);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Nle-c[Asp-Leu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 67);Ac-Nle-c[Asp-Pro-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 68);Ac-Nle-c[Asp-Pro-dPhe-Lys-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 69);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 70);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-Pro-NH2(SEQ ID NO: 71 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 72);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 73);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-NH2(SEQ ID NO: 74);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Pro-NH2(SEQ ID NO: 75);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Arg-NH2(SEQ ID NO: 76);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dArg-NH2(SEQ ID NO: 77);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 78);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 79);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 80);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Pro-Val-NH2(SEQ ID NO: 81 );Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dPro-NH2 (SEQ ID NO: 82);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Val-Pro-NH2 (SEQ ID NO: 83);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dVal-dPro-NH2 (SEQ ID NO: 84);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dVal-dPro-NH2 (SEQ ID NO: 85);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Pro-Val-NH2 (SEQ ID NO: 86);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Val-Pro-NH2 (SEQ ID NO: 87);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2 (SEQ ID NO: 88);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 89);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dPro-NH2 (SEQ ID NO: 90);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 91 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dTle-NH2(SEQ ID NO: 92);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dPro-NH2(SEQ ID NO: 93);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2 (SEQ ID NO: 94);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 95);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-dVal-dPro-NH2(SEQ ID NO: 96);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 97);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 98);Ac-Nle-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 99);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Trp-NH2(SEQ ID NO: 100);Ac-Nle-c[Asp-loc-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 101 );Ac-Nle-c[Asp-Tic-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 102);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 103);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 104);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-dLys-dAsp-NH2 (SEQ ID NO: 105);Ac-Nle-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 106);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 107);Ac-dArg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 108);Ac-Nle-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 109);Ac-Arg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 1 10);Ac-dArg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 111 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 12);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-dVal-NH2 (SEQ ID NO: 1 13);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAla-NH2(SEQ ID NO: 114);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-NH2 (SEQ ID NO: 115);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dHyp-NH2(SEQ ID NO: 116);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dAsn-NH2 (SEQ ID NO: 117);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Asp-NH2 (SEQ ID NO: 1 18);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-dPro-NH2(SEQ ID NO: 119);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Hyp-NH2 (SEQ ID NO: 120);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Ala-Ala-NH2 (SEQ ID NO: 121 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-Gly-NH2(SEQ ID NO: 122);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-dPro-NH2 (SEQ ID NO: 123);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-dPro-NH2 (SEQ ID NO: 124);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-NH2 (SEQ ID NO: 125);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-NH2 (SEQ ID NO: 126);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-NH2 (SEQ ID NO: 127);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-NH2 (SEQ ID NO: 128);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-OH (SEQ ID NO: 129);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2 (SEQ ID NO: 130);Ac-Nle-c[dAsp-Pro-dPhe-Arg-Trp-dLys]-dPro-dVal-NH2(SEQ ID NO: 131 );Ac-Nle-c[Asp-Phe-Phe-Pro-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 132);Ac-Nle-Phe-Phe-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 133);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dl_eu-dPro-NH2 (SEQ ID NO: 134);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 135);Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 136);His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 137); dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 138); dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 139);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 140);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 141 );Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 142);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 143);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 144);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 145);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2 (SEQ ID NO: 146);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dVal-dPro-NH2 (SEQ ID NO: 147);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2 (SEQ ID NO: 148);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dPro-NH2 (SEQ ID NO: 149);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 150);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 151 );Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 152);Docket No. 183B-412975-WOAc-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 153);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 154);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 155);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 156);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 157);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 158);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 159);Ac-Nle-c[Asp-dHis-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 160);Ac-Nle-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 161 );Ac-Nle-c[Asp-Tyr-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 162);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 163);Ac-Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 164);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 165);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 166);Ac-Nle-c[Asp-Val-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 167);Ac-Nle-c[Asp-lle-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 168);Ac-Nle-c[Asp-Gly-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 169);Ac-Nle-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 170);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 171 );Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-dPro-NH2(SEQ ID NO: 172);Ac-Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 173);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 174);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 175);Ac-Arg-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 176);Docket No. 183B-412975-WOAc-Arg-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 177);Ac-Lys-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 178);Ac-Lys-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 179);Ac-Lys-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 180);Ac-Glu-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 181 );Ac-His-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 182);Ac-Glu-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 183);Ac-His-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 184);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 185);Ac-His-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 186);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 187);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 188);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 189);Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 190);Ac-Nle-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 191 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 192);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 193);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 194);Ac-Arg-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 195);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 196);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 197);Ac-Nle-c[Asp-His-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 198);Ac-dGln-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 199);Ac-dGln-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 200);Docket No. 183B-412975-WOAc-dAsn-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 201 );Ac-dAsn-c[Asp-His-dPhe-Arg-Trp-Lys]-d al-dPro-NH2 (SEQ ID NO: 202);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 203);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 204);Ac-Ala-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 205);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Arg-NH2 (SEQ ID NO: 206);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dArg-NH2 (SEQ ID NO: 207);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 208);Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 209);Ac-dAla-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 210);Ac-Nle-c[Asp-Pro-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 211 );Ac-Nle-c[Asp-His-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 212);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 213);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 214);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 215);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 216);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 217);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 218);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 219);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 220);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 221 );Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 222);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 223);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 224);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 225);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2 (SEQ ID NO: 226);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2 (SEQ ID NO: 227);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2 (SEQ ID NO: 228);Ac-Nle-c[Asp-His-dPhe-Ala-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 229);Ac-Nle-c[Asp-Pro-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 230);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 231 );Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 232);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 233);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 234);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 235);Ac-Nle-c[Asp-Pro-dPhe-Arg-dNal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 236);Ac-Nle-c[Asp-Pro-dPhe-Arg-Phe-Lys]-dVal-dPro-NH2(SEQ ID NO: 237);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro (SEQ ID NO: 239);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 240);Ac-Nle-c[Asp-Phe-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 241 );Ac-Nle-c[Asp-Bip-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 242);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 243);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Nle-c[Asp-Aba-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 244);Ac-Nle-c[Asp-Aia-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 245);Ac-Nle-c[Asp-Ata-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 246);Docket No. 183B-412975-WOAc-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 247);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 248);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 249);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 250);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 251 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 252);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 253);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 254);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 255);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 256);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 257);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 258);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 259);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 260);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 261 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 262);Ac-Tyr-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 263);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 264);Ac-Nle-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 265);Ac-Arg-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 266);Ac-Arg-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 267);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 268);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 269);Ac-dGln-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 270);Docket No. 183B-412975-WOAc-dGln-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 271 );Ac-dAsn-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 272);Ac-dAsn-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 273);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 274);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 275);Ac-Ala-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 276);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 277);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 278);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 279);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 280);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 281 );Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 282);Ac-Nle-c[Asp-Oic-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 283);Dmt-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 284);Ac-dAla-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 285);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 286);Ac-Glu-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 287);Ac-Glu-c[Asp-His-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 288);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 289);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 290);Ac-Nle-c[Asp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 291 );Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 292);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 293);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 294);Docket No. 183B-412975-WOAc-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 295);Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 296);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 297);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 298);Ac-Nle-c[Asp-Pro-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 299);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 300);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 301 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 302);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 303);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 304);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 305);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 306);Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 307);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 308);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 309);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 310);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 311 );Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 312);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 313);Ac-Nle-c[Cys-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 314);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 315);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 316);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 317);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 318);Docket No. 183B-412975-WOAc-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 319);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 320);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-d al-dPro-NH2(SEQ ID NO: 321 );Ac-Nle-c[Asp-His-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 322);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 323);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 324);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 325);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 326);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 327);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 328);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 329);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 330);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 331 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 332);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 333);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 334);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 335);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 336);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 337);Ac-Nle-c[Asp-dHis-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 338);Ac-Nle-c[Asp-Gln-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 339);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 340);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 341 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 342);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 343);Ac-dGln-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 344);Ac-dGln-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 345);Ac-dAsn-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 346);Ac-dAsn-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 347);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 348);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 349);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 350);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 351 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 352);Ac-Nle-c[Asp-Oic-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 353);Dmt-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 354);Ac-dAla-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 355);Ac-Nle-c[Asp-Pro-d(F)Phe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 356);Ac-Glu-c[Asp-Pro-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 357);Ac-Glu-c[Asp-His-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 358);Ac-dPhe-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 359);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 360);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 361 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 362);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-NH2(SEQ ID NO: 363);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 364);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-NH2(SEQ ID NO: 365);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 366);Docket No. 183B-412975-WOAc-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 367);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 368);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 369);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 370);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 371 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 372);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-OH (SEQ ID NO: 373);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 374);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-OH (SEQ ID NO: 375);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 376);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-OH (SEQ ID NO: 377);Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 378);Ac-Nle-c[dAsp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 379);Ac-Arg-c[Asp-Gln-p(F)dPhe-Arg-Trp-Gly-Orn]-NH2(SEQ ID NO: 380);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 381 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 382);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 383);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 384);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 385);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 386);Ac-Nle-c[Asp-Phe-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 387);Ac-Nle-c[Asp-Bip-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 388);Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 389);Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 390);Docket No. 183B-412975-WOAc-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 391 );Ac-Nle-c[Asp-Bip-p(Bi dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 392);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 395);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 396);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 397);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 398);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 399);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 400);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 401 );Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Ala-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 404);Ac-Nle-c[dPen-Leu-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 405);Ac-Nle-c[dPen-Gly-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 406);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 414);Docket No. 183B-412975-WOAc-Nle-c[Asp-Glu-His-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 415);Ac-Nle-c[Asp-His-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 416);Ac-dGln-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 417);Ac-dAsn-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 418);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 419);Ac-Ala-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 420);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 421 );Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 422);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 423);Ac-dAla-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 424);Ac-Nle-c[Asp-His-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 425);Ac-Glu-c[Asp-His-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 426);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 427);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 428);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 429);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 430);Ac-dGln-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 431 );Ac-dAsn-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 432);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 433);Ac-Nle-c[dAsp-dNal(2')-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 434);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 435);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 436);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 437);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Docket No. 183B-412975-WOAc-Phe-dAla-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Nle-Asp-Pro-dNal(2')-Arg-Trp-Lys-NH2(SEQ ID NO: 440);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-dGln-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 449);Ac-dGln-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 450);Ac-dGln-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 451 );Ac-dGln-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 452);Ac-dAsn-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 453);Ac-dAsn-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 454);Ac-dAsn-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 455);Ac-dAsn-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 456);Ac-dArg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 457);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-NH2(SEQ ID NO: 460);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Orn]-dArg-dPro-NH2(SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.

106. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -105, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (X1-X2-wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, Lys, dLys, His, dHis, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, His, dHis, Ala, Gly, Leu, He, Vai, His-Arg, Pro-Arg, loc, Tic, Glu, Glu-His, Ala-His, Phe, Bip, Trp, Tyr, Gin, and Hyp;Docket No. 183B-412975-WOR4is selected from the group consisting of dNal(2’), dPhe, p(l)dPhe, p(Br)dPhe, p(F)dPhe, p(CF3)dPhe, and p(CI)dPhe;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, Trp-Pro, Trp-Gly dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, Nal(2’), dNal(1 ’), and Tic;R7is selected from the group consisting ofLys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and; provided that:Docket No. 183B-412975-WO when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then either (i) R3is Pro, R4is dNal(2’) or p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn or dOrn, or (ii) R3is His and R4is p(Br)dPhe and when R1is Arg, then R3is His or Pro-His, when R4is dPhe, then either R3is Oic or R6is dNal(2’), when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R5is Arg or His, R6is not dTrp, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent and, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, when R4is p(F)dPhe, then R3is Pro, Trp, or Tyr, wherein when R3is Pro, then either (i) R2is Cys or (ii) R6is dNal(2’), when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal, when R4is dNal(2’) and R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated, (iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly, (iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from Arg, dArg, dMet, dlle, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, when R4is dNal(2’) and R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Glu, and R5is and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Hyp, Pro-His, Phe-Phe, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, lie, Vai, and Trp.

107. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -106, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA), wherein:X1is absent or Nle;X2is absent or Nle;Docket No. 183B-412975-WOR1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, Lys, dLys, His, dHis, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, His, dHis, Ala, Gly, Leu, He, Vai, His-Arg, Pro-Arg, loc, Tic, Glu, Glu-His, Ala-His, Phe, Bip, Trp, Tyr, Gin, and Hyp;R4is selected from the group consisting of dNal(2’), dPhe, p(l)dPhe, p(Br)dPhe, p(F)dPhe, p(CF3)dPhe, and p(CI)dPhe;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, Nal(2’), dNal(1 ’), and Tic;R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;R8is absent or Lys;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, R4is dNal(2’), and R7is Pen or dPen;Docket No. 183B-412975-WO a disulfide bond between R2and R7, when R2is Cys or Pen, R4is dNal(2’), p(Br)dPhe, p(CI)dPhe, or p(F)dPhe and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys, R4is dNal(2’), and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R4is dNal(2’), p(CI)dPhe, or p(Br)dPhe, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and; provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEO ID NO: 3);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 4);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 6);Ac-Nle-c[Glu-His-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 7);Ac-dGln-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dGln-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 9);Ac-dGln-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 10);Ac-dGln-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 1 1 );Ac-dAsn-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-dAsn-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 13);Ac-dAsn-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 14);Ac-dAsn-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 15);Ac-Nle-c[Glu-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 16);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 17);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Docket No. 183B-412975-WOAc-Ala-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 19);Ac-Ala-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 20);Ac-Ala-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 21 );Ac-Nle-c[Glu-Oic-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 22);Ac-Nle-c[Glu-Oic-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 23);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Dmt-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 25);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Ac-dAla-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 27);Ac-dAla-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 28);Ac-dAla-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 29);Ac-Nle-c[Glu-Pro-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 31 );Ac-Nle-c[Glu-His-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 32);Ac-Nle-c[Glu-His-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 33);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 34);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 35);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 37);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 38);Ac-Arg-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 39);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 40);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Glu-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 42);Docket No. 183B-412975-WOAc-Nle-c[Asp-Trp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 43);Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 44);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 45);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 46);Ac-Nle-c[Asp-Pro-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 57);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-NH2(SEQ ID NO: 58);Ac-dLeu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 59);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 60);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 61 );Ac-dNle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 62);Ac-dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 63);Ac-dTyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 64);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 65);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Nle-c[Asp-Leu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 67);Ac-Nle-c[Asp-Pro-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 68);Ac-Nle-c[Asp-Pro-dPhe-Lys-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 69);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 70);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-Pro-NH2(SEQ ID NO: 71 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 72);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 73);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Val-NH2(SEQ ID NO: 74);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Pro-NH2(SEQ ID NO: 75);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Arg-NH2(SEQ ID NO: 76);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dArg-NH2(SEQ ID NO: 77);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2 (SEQ ID NO: 78);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2 (SEQ ID NO: 79);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-NH2 (SEQ ID NO: 80);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Pro-Val-NH2 (SEQ ID NO: 81 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dPro-NH2(SEQ ID NO: 82);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-Val-Pro-NH2(SEQ ID NO: 83);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dVal-dPro-NH2(SEQ ID NO: 84);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dLys-dVal-dPro-NH2(SEQ ID NO: 85);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Pro-Val-NH2(SEQ ID NO: 86);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-Val-Pro-NH2 (SEQ ID NO: 87);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2 (SEQ ID NO: 88);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 89);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dPro-NH2 (SEQ ID NO: 90);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 91 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dTle-NH2(SEQ ID NO: 92);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dPro-NH2(SEQ ID NO: 93);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2 (SEQ ID NO: 94);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 95);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-dVal-dPro-NH2(SEQ ID NO: 96);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 97);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 98);Ac-Nle-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 99);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Trp-NH2 (SEQ ID NO: 100);Ac-Nle-c[Asp-loc-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 101 );Ac-Nle-c[Asp-Tic-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 102);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 103);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 104);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-dLys-dAsp-NH2 (SEQ ID NO: 105);Ac-Nle-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 106);Ac-Arg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 107);Ac-dArg-c[Asp-dAla-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 108);Ac-Nle-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 109);Ac-Arg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 10);Ac-dArg-c[Asp-Ala-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 111 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 1 12);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-dVal-NH2 (SEQ ID NO: 1 13);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAla-NH2 (SEQ ID NO: 114);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-NH2 (SEQ ID NO: 115);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dHyp-NH2 (SEQ ID NO: 116);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dAsn-NH2 (SEQ ID NO: 117);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-Asp-NH2 (SEQ ID NO: 1 18);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-dPro-NH2 (SEQ ID NO: 119);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Hyp-NH2 (SEQ ID NO: 120);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Ala-Ala-NH2 (SEQ ID NO: 121 );Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-Gly-NH2(SEQ ID NO: 122);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asp-dPro-NH2 (SEQ ID NO: 123);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-dPro-NH2 (SEQ ID NO: 124);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Asn-NH2 (SEQ ID NO: 125);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-NH2 (SEQ ID NO: 126);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsn-NH2 (SEQ ID NO: 127);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Lys-dPro-NH2 (SEQ ID NO: 128);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-OH (SEQ ID NO: 129);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-NH2 (SEQ ID NO: 130);Ac-Nle-c[dAsp-Pro-dPhe-Arg-Trp-dl_ys]-dPro-dVal-NH2(SEQ ID NO: 131 );Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 136);His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 137); dPhe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 138); dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 139);Ac-Nle-c[Asp-Pro-dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 140);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 141 );Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 142);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 143);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 144);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 145);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dVal-dPro-NH2(SEQ ID NO: 146);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dl_ys-dVal-dPro-NH2(SEQ ID NO: 147);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 148);Ac-His-c[Asp-Pro-dP e-Arg-Trp-Lys]-dl_ys-dPro-NH2(SEQ ID NO: 149);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 150);Ac-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 151 );Docket No. 183B-412975-WOAc-Nle-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 152);Ac-Ala-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 153);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 154);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 155);Ac-Lys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 156);Ac-dLys-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 157);Ac-His-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 158);Ac-dHis-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dTle-dPro-NH2 (SEQ ID NO: 159);Ac-Nle-c[Asp-dHis-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 160);Ac-Nle-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 161 );Ac-Nle-c[Asp-Tyr-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 162);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 163);Ac-Phe-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 164);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 165);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 166);Ac-Nle-c[Asp-Val-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 167);Ac-Nle-c[Asp-lle-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 168);Ac-Nle-c[Asp-Gly-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 169);Ac-Nle-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 170);Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 171 );Ac-Tyr-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Arg-dPro-NH2(SEQ ID NO: 172);Ac-Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 173);Ac-dAla-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 174);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 175);Docket No. 183B-412975-WOAc-Arg-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 176);Ac-Arg-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 177);Ac-Lys-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 178);Ac-Lys-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 179);Ac-Lys-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 180);Ac-Glu-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 181 );Ac-His-c[Asp-Gln-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 182);Ac-Glu-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 183);Ac-His-c[Asp-Glu-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 184);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 185);Ac-His-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 186);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 187);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 188);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 189);Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 190);Ac-Nle-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 191 );Ac-Nle-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 192);Ac-Nle-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 193);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 194);Ac-Arg-c[Asp-His-dPhe-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 195);Ac-Arg-c[Asp-Pro-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2 (SEQ ID NO: 196);Ac-Arg-c[Asp-His-dPhe-His-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 197);Ac-Nle-c[Asp-His-dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 198);Ac-dGln-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 199);Docket No. 183B-412975-WOAc-dGln-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 200);Ac-dAsn-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 201 );Ac-dAsn-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 202);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 203);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 204);Ac-Ala-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 205);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Arg-NH2 (SEQ ID NO: 206);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dArg-NH2 (SEQ ID NO: 207);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 208);Dmt-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 209);Ac-dAla-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 210);Ac-Nle-c[Asp-Pro-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 211 );Ac-Nle-c[Asp-His-dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 212);Ac-Glu-c[Asp-Pro-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2 (SEQ ID NO: 213);Ac-Glu-c[Asp-His-dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 214);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 215);Ac-Arg-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 218);Ac-Arg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 219);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 223);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 224);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 225);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2 (SEQ ID NO: 226);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2 (SEQ ID NO: 227);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2 (SEQ ID NO: 228);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-dPhe-Ala-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 229);Ac-Nle-c[Asp-Pro-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2 (SEQ ID NO: 230);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 231 );Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 232);Ac-Nle-c[Asp-Phe-His-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 233);Ac-Nle-c[Asp-His-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 234);Ac-dArg-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 235);Ac-Nle-c[Asp-Pro-dPhe-Arg-dNal(1 ’)-Lys]-dVal-dPro-NH2(SEQ ID NO: 236);Ac-Nle-c[Asp-Pro-dPhe-Arg-Phe-Lys]-dVal-dPro-NH2(SEQ ID NO: 237);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 238);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro (SEQ ID NO: 239);Ac-Nle-c[Asp-Hyp-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 240);Ac-Nle-c[Asp-Phe-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 241 );Ac-Nle-c[Asp-Bip-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 242);Ac-Nle-c[Asp-Pro-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 243);Ac-Nle-c[Asp-Ala-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 66);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 247);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 248);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 249);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 250);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 251 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 252);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 253);Docket No. 183B-412975-WOAc-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 254);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 255);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 256);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 257);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 258);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 259);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 260);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 261 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 262);Ac-Tyr-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 263);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 264);Ac-Nle-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 265);Ac-Arg-c[Asp-Pro-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 266);Ac-Arg-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 267);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 268);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 269);Ac-dGln-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 270);Ac-dGln-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 271 );Ac-dAsn-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 272);Ac-dAsn-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-d al-dPro-NH2(SEQ ID NO: 273);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 274);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 275);Ac-Ala-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 276);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 277);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 278);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 279);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 280);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 281 );Ac-Nle-c[Asp-Pro-p(CI)dP e-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 282);Ac-Nle-c[Asp-Oic-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 283);Dmt-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 284);Ac-dAla-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 285);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 286);Ac-Glu-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 287);Ac-Glu-c[Asp-His-p(CI)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 288);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 289);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 290);Ac-Nle-c[Asp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 291 );Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 292);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 293);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 294);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 295);Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 296);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 297);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 298);Ac-Nle-c[Asp-Pro-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 299);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 300);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 301 );Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 302);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 303);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 304);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 305);Ac-Nle-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 306);Ac-Ala-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 307);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 308);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 309);Ac-Lys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 310);Ac-dLys-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 311 );Ac-His-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 312);Ac-dHis-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 313);Ac-Nle-c[Cys-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 314);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 315);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 316);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 317);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 318);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 319);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 320);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-d al-dPro-NH2(SEQ ID NO: 321 );Ac-Nle-c[Asp-His-p(F)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 322);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 323);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 324);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 325);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 326);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 327);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 328);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 329);Ac-Nle-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 330);Ac-Ala-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 331 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 332);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 333);Ac-Lys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 334);Ac-dLys-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 335);Ac-His-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 336);Ac-dHis-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 337);Ac-Nle-c[Asp-dHis-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 338);Ac-Nle-c[Asp-Gln-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 339);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 340);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 341 );Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 342);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 343);Ac-dGln-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 344);Ac-dGln-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 345);Ac-dAsn-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 346);Ac-dAsn-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 347);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 348);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 349);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 350);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 351 );Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 352);Ac-Nle-c[Asp-Oic-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 353);Dmt-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 354);Ac-dAla-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 355);Ac-Nle-c[Asp-Pro-d(F)Phe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 356);Ac-Glu-c[Asp-Pro-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 357);Ac-Glu-c[Asp-His-p(F)dPhe-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 358);Ac-dPhe-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 359);Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 360);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 361 );Ac-Nle-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 368);Ac-Arg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 369);Ac-Arg-c[Cys-dAla-His-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-OH (SEQ ID NO: 370);Ac-Arg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 371 );Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 378);Ac-Nle-c[dAsp-p(F)dPhe-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 379);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 381 );Ac-dArg-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 382);Ac-Nle-c[Asp-His-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 383);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 384);Ac-dArg-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 385);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 386);Docket No. 183B-412975-WOAc-Nle-c[Asp-Phe-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 387);Ac-Nle-c[Asp-Bip-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 388);Ac-Nle-c[Asp-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 389);Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 390);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 391 );Ac-Nle-c[Asp-Bip-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 392);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dOys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 395);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 396);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 397);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 398);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 399);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 400);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 401 );Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Ala-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 404);Ac-Nle-c[dPen-Leu-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 405);Ac-Nle-c[dPen-Gly-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 406);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Docket No. 183B-412975-WOAc-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2’)-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 414);Ac-Nle-c[Asp-Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 415);Ac-Nle-c[Asp-His-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 416);Ac-dGln-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 417);Ac-dAsn-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 418);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 419);Ac-Ala-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 420);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 421 );Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 422);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 423);Ac-dAla-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 424);Ac-Nle-c[Asp-His-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 425);Ac-Glu-c[Asp-His-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 426);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 427);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 428);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 429);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 430);Ac-dGln-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 431 );Ac-dAsn-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 432);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 433);Ac-Nle-c[dAsp-dNal(2')-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 434);Docket No. 183B-412975-WOAc-Nle-c[Cys-dNal(2’)-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 435);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 436);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 437);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-dGln-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 449);Ac-dGln-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 450);Ac-dGln-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 451 );Ac-dGln-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 452);Ac-dAsn-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 453);Ac-dAsn-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 454);Ac-dAsn-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 455);Ac-dAsn-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 456);Ac-dArg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 457);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dArg-dPro-NH2 (SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.

108. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -107, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(i)) :X1-X2- R1- R2- R3-dNal(2’)- R5-R6- R7-Y1- Y2-Y3-Y4-Y5-Y6-Y7(I A(i)) wherein:X1is absent or norlecuine (Nle);X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, Ala, Gly, Leu, lie, Vai, loc, Tic, Glu, Glu-His, Ala-His, Trp, and Hyp;Docket No. 183B-412975-WOR5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and provided that: when R2is Glu, then either R1is Nle or Arg, wherein when R1is Nle, then R3is Pro, R4is dNal(2’), R5is Arg, R6is Trp, and R7is Orn or dOrn, when R3is Pro, then either (i) R1is Nle, R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus isDocket No. 183B-412975-WO amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, (ii) R1is Tyr, Gly, or dAla, X1is absent, and the N-terminus is acetylated,(iii) R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla and either R2is dPen or R6is Trp-Gly,(iv) R1is dNIe or dPhe and R2is Asp, or (v) R1is selected from Arg, dArg, dMet, d He, dLeu, Vai, Ala, Tie, dTle, Nva, dCys, dTyr, dGIn, dAsn, Dmt, and dPro, and when R3is not Pro, then R1is Nle, Arg, or dArg, and (i) R3is His, R2is Glu, and R5is and His, (ii) R3is absent, R2is Asp and R7is Lys, (iii) R3is selected from Ala, Gly, and Leu, and R2is Asp, (iii) R3is Glu-His, and R6is Trp-Gly, or (v) R3is selected from Hyp, Pro-His, Phe-Phe, dAla-His, Ala-His, Oic, loc, Tic, Glu, Glu-His, Ala, Gly, Leu, He, Vai, and Trp.

109. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -108, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(i)), wherein:X1is absent or norlecuine (Nle);X2is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, Glu, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R3is absent or selected from the group consisting of Pro, Oic, Pro-His, dAla-His, Ala, Gly, Leu, He, Vai, loc, Tic, Glu, Glu-His, Ala-His, Trp, and Hyp;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Docket No. 183B-412975-WOY3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal;Y5is absent or dVal;Y6is absent or dVal;Y7is absent or dPro; and the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent; and provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-Pro-dNal(2’)-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-Nle-c[Glu-His-dNal(2')-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 7);Ac-dGln-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dGln-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 10);Ac-dAsn-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-dAsn-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 14);Ac-Nle-c[Glu-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 16);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Ac-Ala-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 20);Ac-Nle-c[Glu-Oic-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 22);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Docket No. 183B-412975-WOAc-dAla-c[Glu-Pro-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Ac-dAla-c[Glu-His-dNal(2')-Arg-Trp-Orn]-d\Zal-dPro-NH2(SEQ ID NO: 28);Ac-Nle-c[Glu-Pro-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-His-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 32);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 37);Ac-Nle-c[Glu-His-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 38);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Glu-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 42);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 395);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 396);Ac-Nle-c[Pen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 397);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 398);Ac-Nle-c[dPen-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 399);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 400);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 401 );Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Ala-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 404);Ac-Nle-c[dPen-Leu-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 405);Ac-Nle-c[dPen-Gly-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 406);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Docket No. 183B-412975-WOAc-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 414);Ac-Nle-c[Asp-Glu-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 415);Ac-Nle-c[Asp-His-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 416);Ac-dGln-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 417);Ac-dAsn-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 418);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 419);Ac-Ala-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 420);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 421 );Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 422);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 423);Ac-dAla-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 424);Ac-Nle-c[Asp-His-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 425);Ac-Glu-c[Asp-His-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 426);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Om]-dVal-dPro-NH2(SEQ ID NO: 427);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 428);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 429);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 430);Ac-dGln-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 431 );Docket No. 183B-412975-WOAc-dAsn-c[Asp-Gln-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 432);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 433);Ac-Nle-c[dAsp-dNal(2')-Arg-Trp-dl_ys]-dVal-dPro-NH2(SEQ ID NO: 434);Ac-Nle-c[Cys-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 435);Ac-Nle-c[dCys-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 436);Ac-Nle-c[Asp-His-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 437);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-dGln-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 449);Ac-dGln-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 450);Ac-dGln-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 451 );Ac-dGln-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 452);Ac-dAsn-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 453);Ac-dAsn-c[Asp-Gly-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 454);Ac-dAsn-c[Asp-dHis-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 455);Ac-dAsn-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 456);Docket No. 183B-412975-WOAc-dArg-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 457);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Orn]-dArg-dPro-NH2(SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.1 10. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -109, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(ii)):X1-X2-R1-R2-Pro-dNal(2’)-R5-R6-R7-R8-Y1-Y2-Y3-Y4-Y5(IA(ii)) wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Glu, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, and dPro;Docket No. 183B-412975-WOR2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, Trp-Gly, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dVal; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen; a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y4are absent; and provided that: when R2is Glu, then R1is Nle, R5is Arg, R6is Trp, and R7is Orn or dOrn, when R1is Nle, then R7is not dPen, and Y1is present, wherein when R2is Cys, then R7is not dCys, and when R2is Asp, R5is Arg, and R6is Trp, then (a) R7is not dOrn or Lys when Y1is dVal, Y2is dPro, Y3-Y7are absent, and the C-terminus is amidated, (b) Y3-Y7are absent when Y1is dAla, Gly, Asp, or dAsp, and (c) R7is not Orn when Y1is dArg, when R1is Tyr, Gly, or dAla, then X1is absent, and the N-terminus is acetylated,Docket No. 183B-412975-WO when R1is Arg, Tyr, Glu, dHis, His, dLys, Lys, Gly, dAla then either R2is dPen or R6is Trp-Gly, and when R1is dNIe or dPhe, then R2is Asp.1 1 1. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -110, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IA(ii)), wherein:X1is absent or Nle;X2is absent or Nle;R1is selected from the group consisting of Nle, dArg, dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, dNIe, Nva, Gly, dCys, dPhe, Tyr, dTyr, dGIn, dAsn, Dmt, and dPro;R2is selected from the group consisting of dCys, Asp, dAsp, Pen, dPen, Glu, and Cys;R5is absent, or selected from the group consisting of Lys, Orn, His, Ala, and Arg;R6is selected from the group consisting Trp, dTrp, dNal(2’), Nal(1 ’), Phe, Tyr, dPhe, dTyr, and dNal(1 ’);R7is selected from the group consisting of Pro, Gly, Lys, dLys, Cys, dCys, Orn, dOrn, Pen, and dPen;Y1is selected from the group consisting of Vai, dVal, dPro, Hyp, dHyp, Pro, Ala, dAla, Gly, Asp, dAsp, Arg, dArg, Asn, dAsn, Lys, dLys, dTle, and Trp;Y2is absent or selected from the group consisting of dPro, dVal, Pro, Hyp, dHyp, Vai, Ala, dAla, Gly, Asp, Arg, Asn, dAsp, dArg, dAsn, and dTle;Y3is absent or selected from the group consisting of Vai, dVal, Pro, dPro, Lys, and dLys;Y4is absent or selected from the group consisting of dPro, Asp, dAsp, and dValand the non-naturally occurring melanocortin analog is optionally cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2is dPen, Cys, and R7is Pen or dPen; a disulfide bond between R2and R7, when R2is Cys or Pen and R7is Cys or Pen; a disulfide bond between R2and R7, when R2is dCys and R7is Cys, dCys, or Pen;Docket No. 183B-412975-WO a lactam bond between R2and R7, when R2is Asp or dAsp and R7is Lys, dLys, or Orn; and a lactam bond between R2and R7, when R2is Glu, R7is Orn or dOrn, Y1dVal, and Y3-Y7are absent, provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-Pro-dNal(2’)-Arg-dTrp-Orn]-dVal-dPro-NH2(SEQ ID NO: 5);Ac-dGln-c[Glu-Pro-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 8);Ac-dAsn-c[Glu-Pro-dNal(2’)-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 12);Ac-Ala-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 18);Dmt-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 24);Ac-dAla-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 26);Ac-Nle-c[Glu-Pro-dNal(2')-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 30);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 36);Ac-dPhe-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 41 );Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 393);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 394);Ac-dNle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 402);Ac-dPhe-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 403);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dVal-dPro-NH2(SEQ ID NO: 407);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dVal-dPro-NH2(SEQ ID NO: 408);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dArg-dPro-NH2(SEQ ID NO: 409);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dLys-dPro-NH2(SEQ ID NO: 410);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dHyp-NH2(SEQ ID NO: 411 );Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dTle-dPro-NH2(SEQ ID NO: 412);Docket No. 183B-412975-WOAc-Nle-c[dPen-Pro-dNal(2’)-Arg-Trp-Gly-dPen]-dVal-dPro-NH2(SEQ ID NO: 413);Ac-Phe-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 438);Ac-Phe-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 439);Ac-Phe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 441 );Ac-Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 442);Ac-Glu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 443);Ac-Lys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 444);Ac-dLys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 445);Ac-Arg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 446);Ac-His-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 447);Ac-dHis-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 448);Ac-dArg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 457);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 458);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 459);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-NH2(SEQ ID NO: 460);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dArg-dPro-NH2(SEQ ID NO: 461 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dVal-dPro-NH2(SEQ ID NO: 462);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 463);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 464);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 465);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-dVal-dPro-NH2(SEQ ID NO: 466);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-Asp-dVal-dPro-NH2(SEQ ID NO: 467);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Gly-Asp-dVal-dPro-NH2(SEQ ID NO: 468);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAla-dAsp-dVal-dPro-NH2(SEQ ID NO: 469);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-dAsp-dVal-dPro-NH2(SEQ ID NO: 470); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAla-dAsp-dAsp-dVal-dPro-NH2(SEQ ID NO: 471 ), wherein c represents cyclization via a lactam or disulfide bond.1 12. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -107, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IB):X1-X2- R1- R2- R3- R4- R5- R6- R7- Y1-Y2- Y3-Y4(IB) wherein:X1is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, Ala, Lys, dLys, His, and dHis;R2is selected from the group consisting of Asp, Glu, and Cys;R3is absent or selected from the group consisting of Pro, His, dHis, His-Arg, Pro-Arg, Phe, Bip, Trp, Tyr, and Gin;R4is selected from the group consisting of p(l)dPhe, p(Br)dPhe, p(CF3)dPhe, and p(CI)dPhe;R5is His or Arg;R6is selected from the group consisting Trp, dNal(2’), Nal(2’), and Tic;R7is selected from the group consisting of Lys, Cys, and Orn;Y1is selected from the group consisting of dVal, dPro, and dTle;Y2is selected from the group consisting of dPro, dVal, and dTle;Y3is absent, dVal, or dPro;Y4is absent or dPro; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2and R7are both Cys; a lactam bond between R2and R7, when R2is Asp and R7is Lys; and a lactam bond between R2and R7, when R2is Glu, and R7is Orn,Docket No. 183B-412975-WO provided that: when R2is Glu, then R1is Nle and either (i) R3is Pro, R4is p(CI)dPhe, R5is Arg, R6is Trp, and R7is Orn, or (ii) R3is His and R4is p(Br)dPhe, when R4is p(CI)dPhe, then X1is absent, R1is Ala or Nle, R7is not dOrn Y1is dVal or dTle, Y2is dPro, and Y3-Y7are absent, wherein when R1is Ala, then R3is His, and when R1is Nle, then either (i) R3is selected from dHis, Phe, Bip, Trp, Tyr, Pro, and Gin, or (ii) R3is His, and R7is not Orn, and when R4is p(Br)dPhe, then R3is not Bip, wherein when R3is His and R1is His or dHis, then Y1is dVal.1 13. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -107 and 112, wherein the non-naturally occurring melanocortin analog comprises a sequence of Formula (IB), wherein:X1is absent or Nle;R1is selected from the group consisting of Nle, Arg, dArg, Ala, Lys, dLys, His, and dHis;R2is selected from the group consisting of Asp, Glu, and Cys;R3is selected from the group consisting of Pro, His, dHis, His-Arg, Pro-Arg, Phe, Bip, Trp, Tyr, and Gin;R4is selected from the group consisting of p(l)dPhe, p(Br)dPhe, p(CFs)dPhe, and p(CI)dPhe;R5is His or Arg;R6is selected from the group consisting Trp, dNal(2’), Nal(2’), and Tic;R7is selected from the group consisting of Lys, Cys, and Orn;Y1is selected from the group consisting of dVal, dPro, and dTle;Y2is selected from the group consisting of dPro, dVal, and dTle;Y3is absent, dVal, or dPro;Y4is absent or dPro; and the non-naturally occurring melanocortin analog is cyclized via a moiety selected from: a disulfide bond between R2and R7, when R2and R7are both Cys;Docket No. 183B-412975-WO a lactam bond between R2and R7, when R2is Asp and R7is Lys; and a lactam bond between R2and R7, when R2is Glu, and R7is Orn, provided that the non-naturally melanocortin antagonist does not comprise a sequence selected from the group consisting of:Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 3);Ac-Nle-c[Glu-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2 (SEQ ID NO: 17);Ac-Ala-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 19);Ac-Ala-c[Glu-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 21 );Ac-Nle-c[Glu-Pro-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 31 );Ac-Nle-c[Glu-His-p(CI)dPhe-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 33);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 34);Ac-Nle-c[Glu-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 35);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 247);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 248);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 249);Ac-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 250);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 251 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 252);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 253);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 254);Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 255);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 256);Ac-Arg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 257);Ac-Lys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 258);Ac-dLys-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 259);Docket No. 183B-412975-WOAc-His-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 260);Ac-dHis-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 261 );Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 262);Ac-Arg-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 267);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 274);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 275);Ac-Ala-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 276);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 281 );Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 282);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 286);Ac-dArg-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 289);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 290);Ac-Nle-c[Asp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 291 );Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 390);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 391 ); and Ac-Nle-c[Asp-Bip-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 392), wherein c represents cyclization via a lactam or disulfide bond.1 14. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, wherein the sequence of any one of Formulae (l)-(IB) is cyclized through a lactam bond between R2and R7.1 15. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, wherein R4is dNal(2’).Docket No. 183B-412975-WO1 16. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-dOrn]-dVal-dPro-NH2(SEQ ID NO: 509);Ac-Nle-c[Glu-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 510);Ac-Nle-c[dAsp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 511 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-OH (SEQ ID NO: 473);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-dLys]-dVal-dPro-NH2(SEQ ID NO: 560); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 561 ), wherein c represents cyclization through R2and R7via a lactam bond.1 17. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein the sequence of any one of Formulae (l)-(IB) is:Ac-Arg-c[Glu-His-dNal(2’)-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 483); orAc-Arg-c[Glu-Pro-His-dNal(2’)-His-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 484), wherein c represents cyclization through R2and R7via a lactam bond.1 18. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein at least one of X1and X2is present.1 19. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 118, wherein X1is Nle or Phe and X2is absent or Nle.

120. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, 118, and 119, wherein the sequence of any one of Formulae (I)- (IB) is selected from the group consisting of:Ac-Nle-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 476);Docket No. 183B-412975-WOAc-Nle-Nle-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 477); and Ac-Nle-Phe-Phe-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 478), wherein c represents cyclization through a lactam bond between R2and R7.

121. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 15, wherein R1is Arg, dArg, transPro(guan), cisPro(guan), dMet, dlle, dLeu, dVal, dAla, Ala, Tie, dTle, Nva, Gly, dCys, dPhe, dTyr, dGIn, dAsn, dTyr, Tyr, Dmt, dPro, dNIe, or Glu.

122. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 121 , wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Ala-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 479);Ac-cisPro(guan)-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 485);Ac-dAla-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 486);Ac-dArg-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 457);Ac-dAsn-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 489);Ac-dCys-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 490);Ac-dGln-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 491 );Ac-dlle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 492);Ac-dLeu-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 493);Ac-dMet-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 494);Ac-dNle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 495);Ac-dPhe-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 496);Ac-dPro-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 497);Ac-dTle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 498);Docket No. 183B-412975-WOAc-dTyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 499);Ac-dVal-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 500);Ac-Gly-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 502);Ac-Nva-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 503);Ac-Tle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 504);Ac-transPro(guan)-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 505);Dmt-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 506); dTyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 507); and Tyr-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 508), wherein c represents cyclization through a lactam bond between R2and R7.

123. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 15, wherein R3is absent, transPro(guan), cisPro(guan), Aba, Aia, Ata, Aic, Hyp, Pro-His, Ala, Gly, Leu, lie, Vai, Trp, Oic, loc, Tic, Glu, dAla, Ala, Hyp, and Phe.

124. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 123, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Aba-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 514);Ac-Nle-c[Asp-Aia-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 515);Ac-Nle-c[Asp-Aic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 516);Ac-Nle-c[Asp-Ala-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 517);Ac-Nle-c[Asp-Ata-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 519);Ac-Nle-c[Asp-cisPro(guan)-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 520);Ac-Nle-c[Asp-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 522);Ac-Nle-c[Asp-Glu-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 524);Docket No. 183B-412975-WOAc-Nle-c[Asp-Gly-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 526);Ac-Nle-c[Asp-Hyp-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 527);Ac-Nle-c[Asp-lle-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 529);Ac-Nle-c[Asp-loc-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 530);Ac-Nle-c[Asp-Leu-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 531 );Ac-Nle-c[Asp-Oic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 532);Ac-Nle-c[Asp-Tic-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 538);Ac-Nle-c[Asp-transPro(guan)-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 539);Ac-Nle-c[Asp-Trp-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 540); and Ac-Nle-c[Asp-Val-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 541 ), wherein c represents cyclization through a lactam bond between R2and R7.

125. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein R3is a dipeptide comprising His and / or Pro.

126. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 125, wherein R3is Phe-His, Pro-His, Ala-His, or dAla-His.

127. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, 125, and 126, wherein the sequence of any one of Formulae (I)- (IB) is selected from the group consisting of:Ac-Nle-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dlle-dPro-NH2(SEQ ID NO: 533);Ac-Nle-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dLeu-dPro-NH2(SEQ ID NO: 534);Ac-Nle-c[Asp-Phe-His-dNal(2')-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 535);Ac-Nle-c[Asp-Pro-His-dNal(2')-Arg-Trp-Lys]-dPro-dVal-NH2(SEQ ID NO: 536);Ac-Nle-c[Asp-Pro-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 537);Docket No. 183B-412975-WOAc-Nle-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 521 );Ac-Arg-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 481 );Ac-dArg-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 488);Ac-Nle-c[Asp-Ala-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 518);Ac-Arg-c[Asp-Ala-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 480);Ac-dArg-c[Asp-Ala-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 487); andAc-Arg-c[Asp-dAla-His-dNal(2')-Arg-Trp-Lys]-NH2(SEQ ID NO: 482), wherein c represents cyclization through a lactam bond between R2and R7.

128. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 15, wherein R5is absent, Ala, cisPro(guan), His, Lys, Orn, or transPro(guan).

129. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 128, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-His-dNal(2')-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 512);Ac-Nle-c[Asp-His-dNal(2')-transPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 513);Ac-Nle-c[Asp-Pro-dNal(2')-Ala-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 542);Ac-Nle-c[Asp-Pro-dNal(2')-cisPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 543);Ac-Nle-c[Asp-Pro-dNal(2')-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 544);Ac-Nle-c[Asp-Pro-dNal(2')-Lys-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 545);Ac-Nle-c[Asp-Pro-dNal(2')-Orn-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 546);Ac-Nle-c[Asp-Pro-dNal(2')-transPro(guan)-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 547); andAc-Nle-c[Asp-Pro-dNal(2')-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 548), wherein c represents cyclization through R2and R7via a lactam bond.Docket No. 183B-412975-WO130. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein R6is Aba, Aia, Ata, dNal(1 ’), dNal(2’), dPhe, dTrp, dTyr, Nal(1 ’), Phe, or Tyr.

131. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 130, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Aba-Lys]-dVal-dPro-NH2(SEQ ID NO: 549);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Aia-Lys]-dVal-dPro-NH2(SEQ ID NO: 550);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Ata-Lys]-dVal-dPro-NH2(SEQ ID NO: 551 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dNal(1 ')-Lys]-dVal-dPro-NH2(SEQ ID NO: 552);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 553);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dPhe-Lys]-dVal-dPro-NH2(SEQ ID NO: 554);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dTrp-Lys]-dVal-dPro-NH2(SEQ ID NO: 555);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-dTyr-Lys]-dVal-dPro-NH2(SEQ ID NO: 556);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Nal(1 ')-Lys]-dVal-dPro-NH2(SEQ ID NO: 557);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Phe-Lys]-dVal-dPro-NH2(SEQ ID NO: 558); andAc-Nle-c[Asp-Pro-dNal(2')-Arg-Tyr-Lys]-dVal-dPro-NH2(SEQ ID NO: 559), wherein c represents cyclization through R2and R7via a lactam bond.

132. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein R6is Trp-Gly or Trp-Pro.

133. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 132, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Hyp-dNal(2’)-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 528);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Pro-Lys]-dVal-dPro-NH2(SEQ ID NO: 563);Ac-Nle-c[Asp-Glu-dNal(2')-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 523);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 562);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-dl_ys-dAsp-NH2(SEQ ID NO: 564);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 565);Ac-Glu-c[Asp-Pro-dNal(2’)-Arg-Trp-Gly-Lys]-dPro-dPro-Lys-Asp-NH2(SEQ ID NO: 501 ); andAc-Nle-c[Asp-Glu-His-dNal(2’)-Arg-Trp-Gly-Lys]-dVal-dPro-NH2(SEQ ID NO: 525), wherein c represents cyclization through R2and R7via a lactam bond.

134. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115, wherein Y1is an amino acid other than dVal and / or Y2is an amino acid other than dPro.

135. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -115 and 134, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dVal-OH (SEQ ID NO: 474);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Ala-Ala-NH2(SEQ ID NO: 566);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Ala-NH2(SEQ ID NO: 567);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-dPro-dVal-NH2(SEQ ID NO: 568);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-dPro-NH2(SEQ ID NO: 569);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-NH2(SEQ ID NO: 570);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-Pro-Val-NH2(SEQ ID NO: 571 );Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Arg-Val-Pro-NH2(SEQ ID NO: 572);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Asn-dPro-NH2(SEQ ID NO: 573);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asn-NH2 (SEQ ID NO: 574);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-dPro-NH2(SEQ ID NO: 575);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Asp-NH2 (SEQ ID NO: 576);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-dAla-NH2(SEQ ID NO: 577);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dAla-NH2(SEQ ID NO: 578);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dArg-dPro-dVal-NH2(SEQ ID NO: 579);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dArg-dPro-NH2(SEQ ID NO: 580);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dArg-NH2(SEQ ID NO: 581 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsn-dPro-NH2(SEQ ID NO: 582);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsn-NH2(SEQ ID NO: 583);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-dPro-NH2(SEQ ID NO: 584);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dAsp-NH2(SEQ ID NO: 585);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dHyp-dVal-NH2(SEQ ID NO: 586);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dHyp-NH2(SEQ ID NO: 587);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dHyp-Val-NH2(SEQ ID NO: 588);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dLys-dPro-dVal-NH2(SEQ ID NO: 589);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dLys-dPro-NH2(SEQ ID NO: 590);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dPro-dLys-dAsp-NH2(SEQ ID NO: 591 );Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dPro-dPro-NH2(SEQ ID NO: 592);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dTle-NH2(SEQ ID NO: 593);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-NH2(SEQ ID NO: 594);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 595);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dTle-dPro-NH2(SEQ ID NO: 596);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 597);Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dTle-dTle-NH2(SEQ ID NO: 598);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dTle-dVal-NH2(SEQ ID NO: 599);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-Arg-NH2(SEQ ID NO: 600);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-Asn-NH2(SEQ ID NO: 601 );Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-Asp-NH2(SEQ ID NO: 602);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dArg-NH2(SEQ ID NO: 603);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dAsn-NH2(SEQ ID NO: 604);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dAsp-NH2(SEQ ID NO: 605);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dHyp-NH2(SEQ ID NO: 606);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dTle-NH2(SEQ ID NO: 607);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dVal-NH2(SEQ ID NO: 608);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-Hyp-NH2(SEQ ID NO: 609);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-NH2(SEQ ID NO: 610);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Gly-Gly-NH2(SEQ ID NO: 61 1 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Hyp-dVal-NH2(SEQ ID NO: 612);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Hyp-NH2(SEQ ID NO: 613);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Hyp-Val-NH2(SEQ ID NO: 614);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-dPro-dVal-NH2(SEQ ID NO: 615);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-dPro-NH2(SEQ ID NO: 616);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-Pro-Val-NH2(SEQ ID NO: 617);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-Val-Pro-NH2(SEQ ID NO: 618);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Pro-NH2(SEQ ID NO: 619);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Trp-NH2(SEQ ID NO: 620);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-Val-dHyp-NH2(SEQ ID NO: 621 );Docket No. 183B-412975-WOAc-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Val-Hyp-NH2(SEQ ID NO: 622); Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Val-NH2(SEQ ID NO: 623); Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Val-Pro-NH2(SEQ ID NO: 624) Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dPro-dVal-dPro-NH2(SEQ ID NO: 625);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dVal-dPro-NH2(SEQ ID NO: 626);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 627);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dVal-dVal-dVal-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 628);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Arg-dVal-dPro-NH2(SEQ ID NO: 629);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dArg-dVal-dPro-NH2(SEQ ID NO: 630);Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dLys-dVal-dPro-NH2(SEQ ID NO: 631 );Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 632);Ac-Nle-c[Asp-Pro-dNal(2’)-Arg-Trp-Lys]-dTle-dVal-dPro-NH2(SEQ ID NO: 633); and Ac-Nle-c[Asp-Pro-dNal(2')-Arg-Trp-Lys]-Lys-dVal-dPro-NH2(SEQ ID NO: 634), wherein c represents cyclization through R2and R7via a lactam bond.

136. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 14, wherein R4is selected from dPhe, p(F)dPhe, p(Br)dPhe, p(CI)dPhe, p(CF3)dPhe, and p(l)dPhe.

137. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114 and 136, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-Pro-p(l)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 676);Ac-Nle-c[Asp-His-p(l)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 658);Ac-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 672);Docket No. 183B-412975-WOAc-Nle-c[Asp-His-p(CF3)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 654);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 674);Ac-Nle-c[Glu-Pro-p(CI)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 677);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 656);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 651 );Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 652);Ac-Nle-c[Glu-His-p(Br)dPhe-Arg-Trp-Orn]-dVal-dPro-NH2(SEQ ID NO: 636);Ac-Nle-c[Asp-Pro-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 673); and Ac-Nle-c[Asp-Pro-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 668), wherein c represents cyclization through R2and R7via a lactam bond.

138. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114 and 136, wherein X1is present.

139. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, 136, and 138, wherein the sequence of any one of Formulae (I)- (IB) is:Ac-Nle-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 694); or Ac-Nle-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 695), wherein c represents cyclization through a lactam bond between R2and R7.

140. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114 and 136, wherein R1is Ala, Arg, dArg, Lys, dLys, His, or dHis.

141. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, 136, and 140, wherein Y1is dVal or dTle and Y2is dPro.Docket No. 183B-412975-WO142. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 14, 136, 140, and 141 , wherein the sequence of any one of Formulae (l)-(IB) selected from the group consisting of:Ac-Ala-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 641 );Ac-Ala-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 642);Ac-Arg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 643);Ac-dArg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 644);Ac-dHis-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 645);Ac-dLys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 646);Ac-His-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 647);Ac-Lys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 648);Ac-Ala-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 659);Ac-Ala-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 660);Ac-Arg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 661 );Ac-dArg-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 662);Ac-dLys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 663); andAc-Lys-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 664), wherein c represents cyclization through a lactam bond between R2and R7.

143. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114 and 136, wherein R3is dHis, Oic, Phe, Bip, Trp, Tyr, and Gin.

144. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, 136, and 143, wherein the sequence of any one of Formulae (I)- (IB) selected from the group consisting of:Ac-Nle-c[Asp-Oic-dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 472);Docket No. 183B-412975-WOAc-Nle-c[Asp-Bip-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 678);Ac-Nle-c[Asp-dHis-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 679);Ac-Nle-c[Asp-dHis-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 680);Ac-Nle-c[Asp-Gln-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 681 );Ac-Nle-c[Asp-Gln-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 682);Ac-Nle-c[Asp-Phe-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 683);Ac-Nle-c[Asp-Phe-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 684);Ac-Nle-c[Asp-Trp-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 686);Ac-Nle-c[Asp-Trp-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 687);Ac-Nle-c[Asp-Trp-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 688);Ac-Nle-c[Asp-Tyr-p(Br)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 689);Ac-Nle-c[Asp-Tyr-p(CI)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 690); and Ac-Nle-c[Asp-Tyr-p(F)dPhe-Arg-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 691 ), wherein c represents cyclization through a lactam bond between R2and R7.

145. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114 and 136, wherein R5is an amino acid other than Arg and / or R6is an amino acid other than Trp.

146. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, 136, and 145, wherein:(i) R5is His and R6is Trp; or(ii) R5is Arg and R6is selected from the group consisting of dNal(2’), Nal(2’), Aba, Aia, and Ata.Docket No. 183B-412975-WO147. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 14, 136, 145, and 146, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Nle-c[Asp-His-p(CI)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 657);Ac-Nle-c[Asp-His-p(Br)dPhe-His-Trp-Lys]-dVal-dPro-NH2(SEQ ID NO: 653);Ac-Nle-c[Asp-Pro-dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 635);Ac-Nle-c[Asp-Pro-p(F)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 675);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 655);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 637);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-dNal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 638);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Nal(2')-Lys]-dVal-dPro-NH2(SEQ ID NO: 650);Ac-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Aba-Lys]-dVal-dPro-NH2(SEQ ID NO: 669);Ac-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Ata-Lys]-dVal-dPro-NH2(SEQ ID NO: 670); andAc-Nle-c[Asp-Pro-p(CF3)dPhe-Arg-Aia-Lys]-dVal-dPro-NH2(SEQ ID NO: 671 ), wherein c represents cyclization through R2and R7via a lactam bond.

148. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, 136, and 145, wherein R5is Arg and R6is Tic.

149. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 14, 136, 145, and 148, wherein the sequence of any one of Formulae (l)-(IB) is:Ac-Nle-c[Asp-His-Arg-p(l)dPhe-Arg-Tic-Lys]-dVal-dPro-NH2(SEQ ID NO: 649); orAc-Nle-c[Asp-Pro-Arg-p(l)dPhe-Arg-Tic-Lys]-dVal-dPro-NH2(SEQ ID NO: 685), wherein c represents cyclization through R2and R7via a lactam bond.Docket No. 183B-412975-WO150. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114 and 136, wherein Y1is an amino acid other than dVal and / or Y2is an amino acid other than dPro.

151. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -114, 136, and 150, wherein the sequence of any one of Formulae (I)- (IB) is selected from the group consisting of:Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dTle-dVal-NH2(SEQ ID NO: 666);Ac-Nle-c[Asp-His-p(CI)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 667);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 639);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dVal-dVal-dVal-dPro-NH2(SEQ ID NO: 640);Ac-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 665);Ac-Nle-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dPro-dVal-dPro-NH2(SEQ ID NO: 692); andAc-Nle-Nle-c[Asp-His-p(Br)dPhe-Arg-Trp-Lys]-dTle-dPro-NH2(SEQ ID NO: 693), wherein c represents cyclization through R2and R7via a lactam bond.

152. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, wherein the sequence of any one of Formulae (l)-(IB) is cyclized through a lactam bond between R2and R9.

153. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113 and 152, wherein the sequence of any one of Formulae (l)-(IB) is: Ac-Nle-c[Asp-Phe-Phe-Pro-His-dNal(2')-Arg-Trp-Lys]-dVal-dPro-NH2, wherein c represents cyclization through a lactam bond between R2and R9.

154. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, wherein the sequence of any one of Formulae (l)-(IB) is cyclized through a disulfide bond between R2and R7.Docket No. 183B-412975-WO155. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113 and 154, wherein R4is dNal(2’).

156. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, 154, and 155, wherein the sequence of any one of Formulae (I)- (IB) is selected from the group consisting of:Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 708);Ac-Nle-c[Cys-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 709);Ac-Nle-c[dCys-Pro-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 710);Ac-Nle-c[dCys-Pro-dNal(2')-Arg-Trp-dCys]-dVal-dPro-NH2(SEQ ID NO: 711 );Ac-Nle-c[dCys-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 712);Ac-Nle-c[dPen-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 713);Ac-Nle-c[Pen-Pro-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 714); andAc-Nle-c[Pen-Pro-dNal(2')-Arg-Trp-Pen]-dVal-dPro-NH2(SEQ ID NO: 715), wherein c represents cyclization through a disulfide bond between R2and R7.

157. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 13, 154, and 155, wherein R1is selected from Arg, dArg, Ala, His, dHis, Lys, dLys, dLeu, and dTyr.

158. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 13, 154, 155, and 157, wherein the sequence of any one of Formulae (l)-(IB) is selected from the group consisting of:Ac-Ala-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 697);Ac-Arg-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 700);Ac-dArg-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 701 );Ac-dHis-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 702);Docket No. 183B-412975-WOAc-dLeu-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2 (SEQ ID NO: 703);Ac-dLys-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2 (SEQ ID NO: 704);Ac-dTyr-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 705);Ac-His-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2 (SEQ ID NO: 706); and Ac-Lys-c[dPen-Pro-dNal(2')-Arg-Trp-dPen]-dVal-dPro-NH2(SEQ ID NO: 707), wherein c represents cyclization through a disulfide bond between R2and R7.

159. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, 154, and 155, wherein R3is dAla-His.

160. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -1 13, 154, 155, and 159, wherein the sequence of any one of Formulae (l)-(IB) is:Ac-Arg-c[Cys-dAla-His-dNal(2')-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 698); or Ac-Arg-c[Cys-dAla-His-dNal(2')-Arg-Trp-Cys]-NH2(SEQ ID NO: 699), wherein c represents cyclization through a disulfide bond between R2and R7.

161. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113 and 154, wherein R4is selected from p(Br)dPhe, p(CI)dPhe, and p(F)dPhe.

162. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, 154, and 161 , wherein the sequence of any one of Formulae (I)- (IB) is selected from the group consisting of:Ac-Nle-c[Cys-His-p(Br)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 716);Ac-Nle-c[Cys-His-p(CI)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 717); and Ac-Nle-c[Cys-Pro-p(F)dPhe-Arg-Trp-Cys]-dVal-dPro-NH2(SEQ ID NO: 718),Docket No. 183B-412975-WO wherein c represents cyclization through a disulfide bond between R2and R7.

163. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113, wherein the sequence of any one of Formulae (l)-(IB) is linear.

164. The pharmaceutical composition, pharmaceutical formulation, or method of any one of claims 1 -113 and 163, wherein the sequence of any one of Formulae (l)-(l B) is:Ac-Nle-Asp-Pro-dNal(2')-Arg-Trp-dVal-dPro-NH2(SEQ ID NO: 719); orAc-Nle-Asp-Pro-dNal(2')-Arg-Trp-Lys-dVal-dPro-NH2(SEQ ID NO: 720).

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