140 results about "Opiate receptors" patented technology

The present invention provides kappa opioid receptor peptide agonists, methods for preparing these compounds, compositions comprising these kappa opioid receptor peptide agonists, and methods of using the kappa opioid receptor peptide agonists to treat pain or other conditions.

The invention relates to a drug-loaded bone filling material, a preparation method thereof and application of the drug-loaded bone filling material in inhibition of relapse of opioid drugs. The drug-loaded bone filling material is prepared from the following raw materials: powder and curing liquid, the powder comprises a mixture of an opioid receptor antagonist and inorganic calcium salt; in the powder, the mass ratio of the opioid receptor antagonist to the inorganic calcium salt is 4-20%. After a performance test, the drug-loaded bone filling material has the advantages of proper coagulation time, good compressive strength and better drug sustained release characteristic, on one hand, artificial bones capable of promoting osteoblast differentiation can be filled in a bone defect area, and on the other hand, side effects caused by opioid drugs can be relieved, and symptoms can be relieved; meanwhile, for relieving opioid addicts, long-time drug action can be maintained, relapse can be prevented or reduced, and the pharmaceutical composition has great application potential in promoting osteoblast differentiation or inhibiting relapse of opioid drugs.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

Disclosed herein is a solid Form A of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4-amine hydrochloride exhibiting at least X-ray lines (in degrees 2θ ± 0.2) at 4.30, 8.59, 12.88, 18.82 and 21.34 in a powder diffraction pattern when measured using Cu Kα radiation. The solid Form A is an antagonist of the kappa-opioid receptor (KOR) and is useful for treating conditions that benefit from the same. Compositions comprising the solid Form A, as well as related methods of use are also disclosed.

Disclosed are a peptide amide compound composition, a preparation method therefor and medical use thereof. Specifically, the composition contains a compound of formula (I) and pH regulators, and the pH of the solution thereof is 3-5.5. The composition is stable and requires few excipients, and is stable in clinical use. The composition is used for treating or preventing a disease or condition associated with kappa opioid receptors

The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

Methods and compositions are provided for treating individuals exhibiting opioid withdrawal symptoms with opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of opioid withdrawal symptoms, including respiratory depression, sedation, and hypotension. Methods and compositions are also provided for treating stimulant overdose with a benzodiazepine and beta-adrenergic blocking agent. Methods and compositions are also provided for treating concurrent stimulant and opioid overdose comprising administering to a patient in need thereof a benzodiazepine and an opioid antagonist. Methods and compositions are also provided for treating individuals exhibiting opioid withdrawal symptoms or prophy tactically treating individuals for opioid withdrawal symptoms from opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of withdrawal, including respiratory depression, sedation, and hypotension.

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

A series of non-peptide mu opioid receptor (MOR) selective modulators is provided. The compounds have the general formula (I) where R is (II) and where one of a, b, c, d, e or f is the point of attachment of indole ring R to the epoxymorphinan skeleton; at least one of the atoms at positions a, b, c, d, e and f is N; the remaining atoms at positions at a, b, c, d, e and f are CH; and * is a chiral carbon. The compounds are generally MOR antagonists and are used to treat disorders related to opioid receptor functions such as opioid addiction and opioid overdose, for the treatment of neurological diseases and for the treatment of pain, without causing constipation.

Provided herein are compositions and methods of using a Mu opioid receptor (MOR) antagonist (e.g. axelopran) alone or in combination with checkpoint inhibitor (such as e.g. an inhibitor of the PD-1 / PD-L1 pathway (e.g. an antibody such e.g. pem-brolizumab)) and / or an inhibitor of VEGF (e.g. bevacizumab) for reducing angiogenesis or treating cancer. Also provided herein are kits containing a MOR antagonist (e.g. axelopran) alone or in combination with checkpoint inhibitor and / or an inhibitor of VEGF for reducing angiogenesis or treating cancer.

The present application relates to a deuterated dual NOP and opioid receptor agonist and uses thereof. Disclosed are compounds of formula (II) or pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof, and uses thereof in the manufacture of medicaments for the treatment / prevention of diseases mediated by NOP and opioid receptors, wherein each group in (II) is as defined in the specification. (II)

Problem The purpose of the present invention is to provide a novel method for prevention and / or treatment of opioid tolerance or opioid dependence. Specifically, the purpose of the present invention is to develop peptide-based blockers to block MOR-DOR and KOR-DOR heterodimerization. In addition, the purpose of the present invention is to develop homodimer blockers for MOR, DOR, and KOR which modulate their downstream signaling without affecting their internalization. Solution The present invention is a prophylactic and / or therapeutic agent for the prevention and / or treatment of opioid tolerance or opioid dependence comprising the peptide which inhibits the dimer formation of the opioid receptor, wherein the above opioid receptor dimer is a heterodimer or a homodimer formed from one or two opioid receptors selected from the group consisting of the μ type (MOR), the κ type (KOR), and the δ type (DOR).

The present invention provides an application of a kappa opioid receptor agonist in the preparation of a drug for preventing and / or treating temporal lobe epilepsy, wherein the kappa opioid receptor agonist is a non-nitrogen-containing diterpenoid substance, and the non-nitrogen-containing diterpenoid substance is carnosine A. The present invention uses carnosine A to inhibit the excitability mechanism in the brain through kappa opioid receptors to prevent and treat temporal lobe epilepsy; compared with other existing anti-epileptic drugs, carnosine A acts on a completely new target, can simultaneously regulate multiple ion channels located at different positions, has a stable anti-epileptic effect, and is not prone to drug resistance.

The present application discloses a compound of formula (I), compositions comprising said compound, and a method of using said compound as a cannabinoid receptor ligand in the treatment or prevention of diseases associated with a cannabinoid receptor, such as, CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR119, TRPV1, TPRV2, PPARγ or a μ-opioid receptor.

The invention provides novel ligands of Kappa (κ) opioid receptors, such as can be used to modulate a Kappa opioid receptor. Methods of synthesis and methods of use are also provided. Compounds of the invention can be used therapeutically in the treatment of dissociative disorders or pain, or to provide neuroprotection, or to induce diuresis, or to modulate the immune system, or for treatment of one or more of an affective disorders comprising depression or stress / anxiety; an addictive disorder; alcoholism, epilepsy; a cognition deficiency; schizophrenia; Alzheimer's disease; or pain.

The present disclosure relates to compositions that upregulate the production of one or more sequences of micro-interfering ribonucleic acid (miRNA). The sequences of miRNA may be complimentary to a sequence of target messenger RNA (mRNA) that encodes for translation of a target biomolecule, and the miRNA may cause the target mRNA to be degraded or inactivated, thereby causing a decrease in bioavailability of the target biomolecule because it is degraded or inactivated by the miRNA, thereby decreasing the bioavailability of the target biomolecule within a subject that is administered the one or more compositions. In some embodiments of the present disclosure, the target biomolecule is an opioid receptor. In some embodiments of the present disclosure, the target biomolecule is one or more of the mu opioid receptor, the delta opioid receptor, the kappa opioid receptor and the nociceptin opioid receptor.

Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, that are negative allosteric modulators of the p-opioid receptor (MOR). Also disclosed are methods of inhibiting MOR as well as treating opioid overdose.

The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.

The present disclosure is directed to kappa opioid receptor ligands and pharmaceutical compositions thereof and their utility as neurological modulators (e.g., anti-nociceptive agents, antidepressants, anxiolytics, antipruritics). Specifically, the disclosed kappa opioid ligands are G-protein biased kappa opioid agonists containing a core and three different arms as is shown in Formula (A) below.

The present invention provides a pharmaceutical composition for treating or preventing anhedonia, said composition comprising, as an active ingredient, a selective δ opioid receptor agonist, wherein preferably, the selective δ opioid receptor agonist further has a κ opioid receptor antagonist action and a μ opioid receptor antagonist action.

Provided is a composition comprising Chlamydomonas reinhardtii or an extract of Chlamydomonas reinhardtii, the Chlamydomonas reinhardtii or the extract of Chlamydomonas reinhardtii comprising an agonist of an opioid receptor.

The present disclosure is directed to kappa opioid receptor ligands and pharmaceutical compositions thereof and their utility as anti-nociceptive agents. Specifically, the disclosed kappa opioid ligands are G-protein biased kappa opioid agonists containing a bis amide core.

Disclosed herein is a solid Form A of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4-amine hydrochloride exhibiting at least X-ray lines (in degrees 2θ±0.2) at 4.30, 8.59, 12.88, 18.82 and 21.34 in a powder diffraction pattern when measured using Cu Kα radiation. The solid Form A is an antagonist of the kappa-opioid receptor (KOR) and is useful for treating conditions that benefit from the same. Compositions comprising the solid Form A, as well as related methods of use are also disclosed.

A series of non-peptide opioid receptor modulators having the general formula: (I) is provided. In the formula: R = (II) * is a chiral carbon; M is a saturated or unsaturated, branched or unbranched, substituted or unsubstituted alkyl chain from 0-10 atoms in length; X1, X2, X3, X4, or X5 are independently, C, N, O, or S; and R is attached to M by any of X1, X2, X3, X4, or X5. The compounds are used to treat disorders related to opioid receptor functions such as opioid addiction, opioid overdose, pain and constipation caused by opioid use.

The present invention relates to a pharmaceutical composition for treating drug addiction comprising opioid receptor nanodiscs and to a method for preparing opioid receptor nanodiscs. Specifically, the opioid receptor nanodiscs, according to the present invention, inhibit the interaction between an opioid receptor and an opioid-based drug without exhibiting toxicity in the body, are delivered to the brain when administered into the body, and significantly restore the delay in a hot-plate response caused by opioid-based drug addiction, thereby being usefully applicable to treatment of opioid-based drug addiction.

The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyl), -(alkenyl), -(alkynyl), -(cycloalkyl), (haloalkyl), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.

This invention provides a novel κ-opioid receptor (KOR receptor) agonist compound that exhibits excellent efficacy and action. [Solution] In one embodiment, a compound represented by formula IB, its stereoisomer, or a pharmaceutically acceptable salt thereof is provided. Such novel amide bond-containing compounds not only have excellent KOR receptor agonist activity (high affinity for κ opioid receptors), but also have very good hydrophilicity, and therefore have a lower ability to cross the blood-brain barrier and enter the brain. JPEG2026086406000232.jpg3368

The aspects of the disclosed embodiments introduce a novel class of bioactive compounds, including short peptides and peptidosteroids, designed for the selective modulation of G-Protein Coupled Receptors (GPCRs), with a particular focus on the human mu-opioid receptor (MOR). These compounds feature specific amino acid sequences and modifications such as acylation and covalent steroid modifications, including 3beta-hydroxy-5-cholenoic acid or other fatty acid derivatives. These modifications enhance stability, membrane affinity, receptor selectivity, and allosteric modulation potential. The aspects of the disclosed embodiments provide a platform for receptor-targeted therapies, particularly for chronic pain conditions such as neuropathic pain, cancer-related pain, and postoperative pain. By biasing MOR signaling toward analgesic pathways and reducing adverse effects, these compounds address the limitations of traditional opioid therapies, offering improved safety, efficacy, and bioavailability. The described peptides and peptidosteroids also exhibit potential for broader GPCR-mediated therapeutic applications, establishing their utility in advancing precision pharmacology.

Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.

The application discloses a detection method for the affinity of an endogenous opioid peptide to a mu opioid receptor (MOR), a detection kit and application thereof, and is based on a NanoBiT (NanoLuc Binary Technology) luciferase fragment complementation chemiluminescence detection technology, a mu opioid receptor-LgBiT carrier is constructed, a corresponding ligand-HiBiT is synthesized, and the ligand-HiBiT is successfully applied to the determination of the affinity of a beta-endorphin peptide to the mu opioid receptor, so that the mu opioid receptor binding detection at the level of living cells is realized. The detection method and system constructed by the application can be applied to the in-vitro evaluation of the ligand-receptor binding characteristics and the determination of the corresponding endogenous ligand binding affinity, is consistent with the natural mu opioid receptor affinity data determined by a classical method, and is safer and more efficient.