50 results about "Neurotensin" patented technology

A complex is provided for the treatment of neurogenic conditions having the formula: where R1 is M is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium (II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium (II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium (II):transporter ligand.

Disclosed are a method and a corresponding pharmaceutical composition for treating damaged cartilage and subchondral bone. Neurogenic compounds in general and neuropeptides in particular have been found to be highly effective in stimulated repair of cartilage and bone damaged due to traumatic injury, ligament disease, and disuse. Preferred active ingredients for use in the method and corresponding pharmaceutical composition include calcitonin gene-related peptide (CGRP), cholecystokinin (CCK), dynorphin, enkephalin, galanin, neuropeptide Y (NPY), neurotensin, somatostatin, substance P (SP), thyrotropin-releasing hormone (TRH), vasoactive intestinal peptide (VIP).

A compound is provided that has the formula NH2CH2CH2CH2C(O)N—R   (I) where R is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidetransferrin, glucosylamnine, amino saccharin, lactylamine, leucine, tryptophan, glutamate and amino cholines.

The present invention provides methods of treating cerebral ischemia in mammals comprising inducing hypothermia in a mammal before, during, or following cerebral ischemia in the mammal. The hypothermia is induced by administering to the mammal an effective dose of a neurotensin analog that is capable of crossing the blood-brain barrier and that comprises neo-tryptophan.

A compound is provided that has the formula NH2CH2CH2CHR1C(O)N—R  (I) where R1 is p-chlorophenyl, R is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptide transferrin, glucosylamine, amino saccharin, lactylamine, leucine, tryptophan, glutamate and amino cholines.

A complex is provided for the treatment of neurogenic conditions having the formula:where R1 isM is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium(II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium(II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium(II):transporter ligand.

A compound is provided that has the formulaNH2CH2CH2CH2C(O)N—R  (I)where R is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidetransferrin, glucosylamnine, amino saccharin, lactylamine, leucine, tryptophan, glutamate and amino cholines.

A compound is provided that has the formulaNH2CH2CH2CHR1C(O)N—R   (I)where R1 is p-chlorophenyl, R is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptide transferrin, glucosylamine, amino saccharin, lactylamine, leucine, tryptophan, glutamate and amino cholines.

The present invention pertains to the field of genomics and nanotechnology, specifically to the in vivo gene expression technologies and their application in gene therapy. It consists of the performance of the NTS-polyplex nanocomplex, which can carry nucleic acids to the neurons, involving neurotrophic therapy to treat neurodegenerative diseases. In particular, the present invention addresses the treatment of Parkinson's disease by the regulated expression of the BDNF neurotrophin.

Disclosed are a method and a corresponding pharmaceutical composition for treating damaged ligaments. Neurogenic compounds in general and neuropeptides in particular have been found to be highly effective in stimulated repair of ligaments damaged due to traumatic injury, ligament disease, and disuse. Preferred active ingredients for use in the method and corresponding pharmaceutical composition include calcitonin gene-related peptide (CGRP), cholecystokinin (CCK), dynorphin, enkephalin, galanin, neuropeptide Y (NPY), neurotensin, somatostatin, substance P (SP), thyrotropin-releasing hormone (TRH), vasoactive intestinal peptide (VIP).

A compound of the formulawhere R1 is H, C1–C4 alkyl and OH; R2 in is H, C1–C4 alkyl and OH; R3 is H and C1–C4 alkyl; R4 is H and C1–C4 alkyl; n is an integer between 0 and 2 inclusive; R5 is a nullity, NHR7C(O)—, C6H4—, C6H4—O—; R7 is C2–C6 alkyl; and R6 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, transferrin, glucosylamine, amino saccharin, saccharin ester, lactylamine, leucine, tryptophan, amino glutamate and amino cholines.

The invention provides a preparation method for jelly fish neurotensin, which comprises the following steps of: carrying out metallic ion removal treatment on jelly fish; sequentially carrying out steps of homogenating, enzymolysis, enzyme deactivating, concentration, ultrafiltration, freeze drying and the like; and finally obtaining purified jelly fish neurotensin powder. The method combines the modern enzyme engineering technology, provides a novel efficient production path for the jelly fish neurotensin, improves the utilization efficiency of jelly fish resources and has the characteristics that the operation is simple, the extraction rate is high, and the product activity preservation is good. The production cost of the jelly fish neurotensin is reduced. The rich protein resources of the jelly fish are sufficiently utilized, and various metallic ions in jelly fish bodies are basically and clearly removed through the metallic ion removal treatment, so the subsequent enzymolysis and application are safer. Results of jelly fish neurotensin antihypertensive activity experiments adopting spontaneously hypertensive rat (SHR) models show that the group of the preparation method obviously differs from the blank control group. The jelly fish neurotensin prepared by the preparation method has the antihypertensive activity similar to positive control captopril.

A compound of the formula where R1 is H, C1-C4 alkyl and OH; R2 in is H, C1-C4 alkyl and OH; R3 is H and C1-C4 alkyl; R4 is H and C1-C4 alkyl; n is an integer between 0 and 2 inclusive; R5 is a nullity, NHR7C(O)—, C6H4—, C6H4—O—; R7 is C2-C6 alkyl; and R6 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, transferrin, glucosylamine, amino saccharin, saccharin ester, lactylamine, leucine, tryptophan, amino glutamate and amino cholines.

The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

This invention relates to non-natural desamino alkyl amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino, alpha methyl N,N dimethyl homolysine residue.

The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

Subject matter of the present invention is a method for predicting the risk of getting cancer in a female subject that does not suffer from cancer or alternatively diagnosing cancer in a female subject comprising determining the level of pro-neurotensin or fragments thereof of at least 5 amino acids in a bodily fluid obtained from said female subject; and correlating said level of pro-neurotensin or fragments thereof with the a risk for getting cancer, wherein an elevated level is predictive for an enhanced risk of getting cancer or alternatively diagnosing cancer wherein an elevated level is correlated with the diagnosis of cancer and, wherein said cancer is selected from the group comprising breast cancer, lung cancer, pancreatic cancer and colon cancer.

Disclosed are a method and a corresponding pharmaceutical composition for treating damaged ligaments. Neurogenic compounds in general and neuropeptides in particular have been found to be highly effective in stimulated repair of ligaments damaged due to traumatic injury, ligament disease, and disuse. Preferred active ingredients for use in the method and corresponding pharmaceutical composition include calcitonin gene-related peptide (CGRP), cholecystokinin (CCK), dynorphin, enkephalin, galanin, neuropeptide Y (NPY), neurotensin, somatostatin, substance P (SP), thyrotropin-releasing hormone (TRH), vasoactive intestinal peptide (VIP).

This invention relates to non-natural desamino amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino N,N dimethyl homolysine residue.

The invention a chimeric peptide based on endomorphin-1 and neurotensin (8-13) and a synthesis method and application thereof. The chimeric peptide solves the problem that the existing endomorphin-1 has short lasting time of easing pain, low pain-easing activity based on peripheral administration and analgesic tolerance and gastrointestinal side effects. The chimeric peptide has an amino acid sequence of Tyr-Pro-Trp-Phe-Gly-Gly-Arg-Arg-Pro-Tyr-Ile-Leu. The synthesis method comprises 1, Fmoc-protective Wang resin pretreatment, 2, removal of a Fmoc-protective gene, 3, amino acid condensation reaction, 4, peptide chain extension, 5, cutting of the peptide chain from resin, and 6, crude peptide desalting and purification. The chimeric peptide has long duration of easing pain and has the advantages of no pain easing tolerance and low side effects on the gastrointestinal tract. The chimeric peptide is used for preparation of polypeptide pain easing drugs.

The invention discloses a prostatic cancer diagnosis developer, which has a structural formula shown in the description. The close relevancy of neurotensin and prostatic cancer is utilized; the neurotensin is marked by A1-18F; the prostatic cancer diagnosis developer is obtained. The diagnosis developer has excellent pharmacokinetic properties; the intake quantity on the prostate tumor is high; high sensitivity and specificity are realized on the prostatic cancer diagnosis; false positive cannot easily occur. In addition, a marking method is simple; after 6h from the marking, the radiochemicalpurity is still as high as 99 percent.

The invention discloses application of neurotensin in diagnosis on castration resistant prostate cancer neuroendocrine subtype and prognosis judgment. The neurotensin level in serum of a subject is detected, correlation analysis is performed on the neurotensin level and clinical data of the subject, and meanwhile a basic biological experimental verification is utilized to prove that the neurotensin and the castration resistant prostate cancer neuroendocrine subtype have large correlation. By means of the application, a novel method is provided for clinic diagnosis on the castration resistant prostate cancer neuroendocrine subtype and the prognosis judgment.

The present invention relates to methods for the treatment, the prognostic assessment and the detection of breast cancer.

The invention provides a multi-site modified enkephalin and neurotensin (8-13) coupled cycled hybrid peptide, a compounding method and an application thereof and relates to a cycled hybrid peptide, the compounding method and the application thereof. The invention aims to solve the problems of inferior anti-enzymolysis capacity and non-ideal anti-neuropathic pain effect of present opioids. The hybrid peptide is a hybrid peptide 1, a hybrid peptide 2, a hybrid peptide 3 or a hybrid peptide 4. The preparation method comprises the following steps: 1) pre-treating 'Fmoc' protected Wang resin; 2) removing 'Fmoc' protecting groups; 3) triggering condensation reaction of amino acid; 4) prolonging peptide chain; 5) forming a disulfide bond; 6) cutting peptide chain from the resin; 7) desalting andpurifying crude peptide. According to the invention, the biological stability of hybrid peptide can be enhanced and an anti-neuropathic pain effect can be endowed, through multi-site unnatural amino acid substitution and cyclizing modification. The hybrid peptide provided by the invention can be used for preparing drugs for relieving neuropathic pain.

Disclosed is a technetium-99m-labeled glycine oligomer associated with imaging probes for biomolecules of interest. The glycine oligomer can be readily synthesized in a single process using an automated peptide synthesizer. The technetium-99m tricarbonyl-labeled glycine oligomers can be useful as a radiotracer for gamma or SPECT imaging apparatus. The technetium-99m tricarbonyl-labeled glycine oligomers can be applied to various peptidyl biomolecules such as RGD peptide, somatostatin, neurotensin, etc., and exhibit rapid renal clearance without being excessively retained within the body.

Subject matter of the present invention is a method for predicting the risk of a subject for contracting diabetes mellitus and / or metabolic syndrome or for diagnosing metabolic syndrome in a subject wherein said subject is non-diabetic, comprising the following steps determining the level of pro-neurotensin or fragments thereof of at least 5 amino acids in a bodily fluid obtained from said subject; and correlating said level of pro-neurotensin or fragments thereof with the risk of said subject for contracting diabetes mellitus and / or metabolic syndrome, wherein an elevated level is predictive for an enhanced risk of getting diabetes mellitus and / or metabolic syndrome, or wherein an elevated level correlates to the diagnosis of metabolic syndrome in a subject wherein said subject is non-diabetic.

A compound is provided that has the formula (II):where R1 in each occurrence is independently H, or C1-C4 alkyl; R2 is a nullity or CH—CH3, R3 is a nullity or C(O)—R6—NH; R6 is C2-C6 alkyl, (CH2CH2—O)n, or (CH(OH)CH2)n; n is an integer of between 1 and 4; R4 is a nullity or NH—R6—C(O); and R5 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, endocannabinoids 1 & 2, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptide transferrin, glucosyl ester, lactic acid, leucine, tryptophan, glutamic acid.

The invention relates to a layered double hydroxide material system, a preparation method thereof and application of the layered double hydroxide material system, in particular to an NT-LDH / EDTA layered double hydroxide material and an NT-LDH layered double hydroxide material; the NT-LDH / EDTA layered double hydroxide material comprises the following components: ethylenediamine tetraacetic acid (EDTA)-loaded zinc-aluminum layered double hydroxide, and a neurotensin (NT) antibody modified on the surface of the zinc-aluminum layered double hydroxide.