9 results about "OPIOID TOLERANCE" patented technology

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 application discloses application of a peripheral nervous system Mas-related G protein-coupled receptor D as a target point in preparation of a medicine for screening for relieving opioid tolerance. Jun The application further provides a medicine composition for regulating opioid tolerance, containing a Mas-related G protein-coupled receptor D siRNA sequence shown in SEQ ID NO. 1 or a siRNA sequence shown in SEQ ID NO. 2. The application further provides an in-situ hybridization kit for detecting expression of a Mas-related G protein-coupled receptor D gene in a dorsal root ganglion tissue of a peripheral nervous system. The application expands a new path for opioid companion diagnosis and intervention.

The invention discloses application of a peripheral nervous system Mas related G protein coupled receptor D as a target spot in preparing and screening a medicine for relieving opioid medicine tolerance. The invention also provides a pharmaceutical composition for regulating and controlling the tolerance of the opioid drugs. The pharmaceutical composition contains a Mas related G protein coupled receptor D siRNA sequence as shown in SEQ ID NO. 1 or a Jun siRNA sequence as shown in SEQ ID NO. 2. The invention also provides an in-situ hybridization kit for detecting the expression of the Mas related G protein coupled receptor D gene in the dorsal root ganglion tissue of the peripheral nervous system. According to the invention, a new path for accompanying diagnosis and intervention of opioid drugs is expanded.

The present invention provides methods for treating and / or managing pain. The invention further provides methods for reducing or inhibiting opioid tolerance, reducing risk of opioid addiction or dependence, restoring opioid efficacy, and enhancing the therapeutic effect of an opioid. The invention further provides compositions for use in the methods of the invention.

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).

This invention relates to compositions and methods for treating opioid tolerance in subjects, and to methods for selecting pain relief treatment regimens for subjects suffering from and / or at risk of developing opioid tolerance. Embodiments of the treatment methods of this invention include administering a gelling agent to produce a therapeutic effect against opioid tolerance in the subject.

The object of the present invention is to provide a novel method for preventing and / or treating opioid tolerance or opioid dependence. Specifically, the object of the present invention is to develop a peptide-based blocker for preventing MOR-DOR and KOR-DOR heterodimerization. Furthermore, the object of the present invention is to develop a homodimer blocker for MOR, DOR, and KOR that modulates downstream signaling without affecting internalization. 【Means for Solving the Problem】 The present invention is a prophylactic agent and / or therapeutic agent for preventing and / or treating opioid tolerance or opioid dependence, comprising a peptide that inhibits dimer formation of an opioid receptor, wherein the opioid receptor dimer is a heterodimer or homodimer formed from one or two opioid receptors selected from the group consisting of a μ type (MOR), a κ type (KOR), and a δ type (DOR).

According to the invention, peptide ligands of a neuropeptide FF receptor are designed, namely, endogenous peptide agonists neuropeptide FF (Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2) and neuropeptide VF (Val-Pro-Asn-Leu-Pro-Gln-Arg-Phe-NH2) of the neuropeptide FF receptor are used as chemical template molecules, and a series of analogues are derived by virtue of scanning of propargyl glycine (Pra) and scanning of azido alanine [Ala (N3)]. Further, Pra side chain alkynyl and Ala( N3) side chain azide of the analogue are chemically derived from small molecule compounds containing azide and alkynyl structures respectively through click chemistry reaction, and a peptide ligand of a neuropeptide FF receptor with a brand new structure is obtained by combining a substitution modification strategy of a single-site amino acid. In-vitro calcium mobilization experiments show that 44 agonists and 12 antagonists exist in the neuropeptide FF receptor peptide ligands, and the neuropeptide FF receptor peptide ligands with novel structures can be potentially used for relieving or treating side effects of tolerance, constipation, addiction, respiratory depression and the like of opioid drugs.

The present invention relates to compositions and methods for treating opioid tolerance in subjects and methods for selecting a pain-reduction therapeutic regimen for a subject who has an opioid tolerance and / or a subject who is at risk of having an opioid tolerance. Embodiments of treatment methods of the invention include administering a gelsolin agent to produce a therapeutic effect against opioid tolerance in a subject.