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Κ-opioid receptor

Index Κ-opioid receptor

The κ-opioid receptor (KOR) is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene. [1]

95 relations: Adrenorphin, Agonist-antagonist, Akuammicine, Analgesic, Animal psychopathology, AP-237, Asimadoline, Atomoxetine, Big dynorphin, Bremazocine, BRL-52537, Buprenorphine/samidorphan, CERC-501, Coronaridine, Cyclazocine, Cyprodime, Dezocine, Dihydromorphine, Dopamine agonist, Dopamine receptor D2, Dynorphin A, Enadoline, Eptazocine, Erinacine, Etorphine, G protein-coupled inwardly-rectifying potassium channel, Gamma-Hydroxybutyric acid, Gi alpha subunit, GR-89696, Hallucination, Hallucinogen, Hemorphin-4, Herkinorin, Heroin, Hydrocodone/paracetamol, Hypericum perforatum, HZ-2, ICI-199,441, ICI-204,448, Incarvillateine, Index of biochemistry articles, Δ-opioid receptor, Μ-opioid receptor, JDTic, Jon Levine (neuroscientist), Ketamine, Legal status of Salvia divinorum, Legal status of Salvia divinorum in the United States, Leu-enkephalin, LPK-26, ..., MCOPPB, Menthol, Met-enkephalin, Metazocine, Metkefamide, N-2′-Indolylnaltrexamine, Naltriben, Neurotransmitter, Nociceptin receptor, Norbinaltorphimine, Norbuprenorphine, Opioid, Opioid modulator, Oxilorphan, Penicillium parvum, Pentazocine, PF-4455242, Phenazocine, Physical dependence, Picenadol, Proxorphan, Psychedelic drug, Psychotomimetic, Rhodopsin-like receptors, Salvia divinorum, Salvinorin A, Salvinorin B methoxymethyl ether, SC-17599, Sigma receptor, Sigma-1 receptor, Sodium-hydrogen antiporter 3 regulator 1, Spiradoline, Tifluadom, Trevena Inc, U-50488, U-69,593, U-77891, Ubiquitin C, 18,19-Dehydrobuprenorphine, 18-Methoxycoronaridine, 2-Methoxyethyl-18-methoxycoronaridinate, 25I-NBOMe, 5'-Guanidinonaltrindole, 5-MeO-DALT, 8-Carboxamidocyclazocine. Expand index (45 more) »

Adrenorphin

Adrenorphin, also sometimes referred to as metorphamide, is an endogenous, C-terminally amidated, opioid octapeptide (Tyr-Gly-Gly-Phe-Met-Arg-Arg-Val-NH2) that is produced from proteolytic cleavage of proenkephalin A and is widely distributed throughout the mammalian brain.

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Agonist-antagonist

In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the activity of other agonists).

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Akuammicine

Akuammicine is an alkaloid found in Vinca minor and Aspidosperma.

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Analgesic

An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain.

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Animal psychopathology

Animal psychopathology is the study of mental or behavioral disorders in animals.

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AP-237

AP-237 (1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer patients as of 1986.

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Asimadoline

Asimadoline (EMD-61753) is a drug which acts as a peripherally selective κ-opioid receptor (KOR) agonist.

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Atomoxetine

Atomoxetine, sold under the brand name Strattera among others, is a norepinephrine (noradrenaline) reuptake inhibitor which is approved for the treatment of attention deficit hyperactivity disorder (ADHD).

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Big dynorphin

Big dynorphin is an endogenous opioid peptide of the dynorphin family that is composed of both dynorphin A and dynorphin B. Big dynorphin has the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln-Lys-Arg-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Gln-Phe-Lys-Val-Val-Thr.

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Bremazocine

Bremazocine is a κ-opioid receptor agonist related to pentazocine.

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BRL-52537

BRL-52537 is a drug which acts as a potent and highly selective κ-opioid agonist.

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Buprenorphine/samidorphan

Buprenorphine/samidorphan (developmental code name ALKS-5461) is a combination drug formulation of buprenorphine and samidorphan acting as a κ-opioid receptor (KOR) antagonist which is under development by Alkermes as an adjunct to antidepressant therapy in treatment-resistant depression (TRD).

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CERC-501

CERC-501 (originally known as LY-2456302) is a selective antagonist of the κ-opioid receptor (KOR) which was originally developed by Eli Lilly and is now under development by Janssen Pharmaceuticals for the treatment of major depressive disorder and substance use disorders including alcoholism, nicotine addiction, and illicit drug dependence.

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Coronaridine

Coronaridine, also known as 18-carbomethoxyibogamine, is an alkaloid found in Tabernanthe iboga and related species, including Tabernaemontana divaricata for which (under the now obsolete synonym Ervatamia coronaria) it was named.

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Cyclazocine

Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine.

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Cyprodime

Cyprodime is an opioid antagonist from the morphinan family of drugs.

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Dezocine

Dezocine (INN, USAN) (brand name Dalgan) is a marketed opioid analgesic of the benzomorphan group.

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Dihydromorphine

Dihydromorphine (Paramorfan, Paramorphan) is a semi-synthetic opioid structurally related to and derived from morphine.

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Dopamine agonist

A dopamine receptor agonist is a compound that activates dopamine receptors.

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Dopamine receptor D2

Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the DRD2 gene.

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Dynorphin A

Dynorphin A is a form of dynorphin and an endogenous opioid peptide with the amino acid sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys.

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Enadoline

Enadoline is a drug which acts as a highly selective κ-opioid agonist.

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Eptazocine

Eptazocine (Sedapain) is an opioid analgesic which was introduced in Japan by Morishita in 1987.

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Erinacine

Erinacines are natural substances isolated from Hericium erinaceum.

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Etorphine

Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine.

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G protein-coupled inwardly-rectifying potassium channel

The G protein-coupled inwardly-rectifying potassium channels (GIRKs) are a family of inward-rectifier potassium ion channels which are activated (opened) via a signal transduction cascade starting with ligand-stimulated G protein-coupled receptors (GPCRs).

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Gamma-Hydroxybutyric acid

γ-Hydroxybutyric acid (GHB), also known as 4-hydroxybutanoic acid, is a naturally occurring neurotransmitter and a psychoactive drug.

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Gi alpha subunit

Gi alpha subunit (Gαi, or Gi/G0 or Gi protein) is a heterotrimeric G protein subunit that inhibits the production of cAMP from ATP.

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GR-89696

GR-89696 is a drug which acts as a highly selective κ-opioid agonist.

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Hallucination

A hallucination is a perception in the absence of external stimulus that has qualities of real perception.

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Hallucinogen

A hallucinogen is a psychoactive agent which can cause hallucinations, perceptual anomalies, and other substantial subjective changes in thoughts, emotion, and consciousness.

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Hemorphin-4

Hemorphin-4 is an endogenous opioid peptide of the hemorphin family which possesses antinociceptive properties and is derived from the β-chain of hemoglobin in the bloodstream.

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Herkinorin

Herkinorin is an opioid analgesic that is an analogue of the natural product Salvinorin A. It was discovered in 2005 during structure-activity relationship studies into neoclerodane diterpenes, the family of chemical compounds of which Salvinorin A is a member.

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Heroin

Heroin, also known as diamorphine among other names, is an opioid most commonly used as a recreational drug for its euphoric effects.

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Hydrocodone/paracetamol

Hydrocodone/paracetamol, also known as hydrocodone/acetaminophen or hydrocodone/APAP and marketed under the trade name Vicodin and Norco among others, is the combination of an opioid pain medication, hydrocodone, with paracetamol (acetaminophen).

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Hypericum perforatum

Hypericum perforatum, known as perforate St John's-wort, common Saint John's wort and St John's wort, is a flowering plant in the family Hypericaceae.

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HZ-2

HZ-2 is a drug which acts as a highly selective κ-opioid agonist.

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ICI-199,441

ICI-199,441 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects.

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ICI-204,448

ICI-204,448 is a drug which acts as a potent and peripherally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching effects.

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Incarvillateine

Incarvillateine is a complex monoterpene alkaloid that is a derivative of α-truxillic acid.

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Index of biochemistry articles

Biochemistry is the study of the chemical processes in living organisms.

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Δ-opioid receptor

The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands.

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Μ-opioid receptor

The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins.

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JDTic

JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR).

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Jon Levine (neuroscientist)

Jon David Levine is an American neuroscientist known for his research on pain and analgesia.

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Ketamine

Ketamine, sold under the brand name Ketalar among others, is a medication mainly used for starting and maintaining anesthesia.

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Legal status of Salvia divinorum

Salvia divinorum, a psychoactive plant, is legal in most countries.

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Legal status of Salvia divinorum in the United States

The legal status of Salvia divinorum in the United States varies, with 29 states (and the territory of Guam) having completely banned it and others considering proposals for banning its use.

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Leu-enkephalin

Leu-enkephalin is an endogenous opioid peptide neurotransmitter with the amino acid sequence Tyr-Gly-Gly-Phe-Leu that is found naturally in the brains of many animals, including humans.

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LPK-26

LPK-26 is a potent and selective κ-opioid agonist, and has analgesic effects.

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MCOPPB

MCOPPB is a drug which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07 and much weaker activity at other opioid receptors.

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Menthol

Menthol is an organic compound made synthetically or obtained from corn mint, peppermint, or other mint oils.

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Met-enkephalin

Met-enkephalin, also known as metenkefalin (INN), sometimes referred to as opioid growth factor (OGF), is a naturally occurring, endogenous opioid peptide that has opioid effects of a relatively short duration.

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Metazocine

Metazocine is an opioid analgesic related to pentazocine.

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Metkefamide

Metkefamide (INN; LY-127,623), or metkephamid acetate (USAN), but most frequently referred to simply as metkephamid, is a synthetic opioid pentapeptide and derivative of Metenkephalin with the amino acid sequence Tyr-D-Ala-Gly-Phe-(N-Me)-Met-NH2.

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N-2′-Indolylnaltrexamine

N-2′-Indolylnaltrexamine (INTA) is an opioid and derivative of β-naltrexamine.

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Naltriben

Naltriben is a potent and selective antagonist for the delta opioid receptor, which is used in scientific research.

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Neurotransmitter

Neurotransmitters are endogenous chemicals that enable neurotransmission.

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Nociceptin receptor

The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the OPRL1 (opioid receptor-like 1) gene.

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Norbinaltorphimine

Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research.

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Norbuprenorphine

Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine.

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Opioid

Opioids are substances that act on opioid receptors to produce morphine-like effects.

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Opioid modulator

An opioid modulator (or opioid receptor modulator) is a drug which has mixed agonist and antagonist actions at different opioid receptors and thus cannot clearly be described as either an opioid agonist or antagonist.

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Oxilorphan

Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed.

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Penicillium parvum

Penicillium parvum is an anamorph species of the genus of Penicillium which was isolated from soil in Papua New Guinea.

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Pentazocine

Pentazocine, sold under the brand name Talwin among others, is a painkiller used to treat moderate to severe pain.

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PF-4455242

PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor.

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Phenazocine

Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects.

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Physical dependence

Physical dependence is a physical condition caused by chronic use of a tolerance forming drug, in which abrupt or gradual drug withdrawal causes unpleasant physical symptoms.

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Picenadol

Picenadol (LY-97435) is a 4-phenylpiperidine derivative that is an opioid analgesic drug developed by Eli Lilly in the 1970s.

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Proxorphan

Proxorphan (INN), also known as proxorphan tartate (USAN) (developmental code name BL-5572M), is an opioid analgesic and antitussive drug of the morphinan family that was never marketed.

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Psychedelic drug

Psychedelics are a class of drug whose primary action is to trigger psychedelic experiences via serotonin receptor agonism, causing thought and visual/auditory changes, and altered state of consciousness.

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Psychotomimetic

A drug with psychotomimetic (also known as psychotogenic) actions mimics the symptoms of psychosis, including delusions and/or delirium, as opposed to just hallucinations.

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Rhodopsin-like receptors

Rhodopsin-like receptors are a family of proteins that comprise the largest group of G protein-coupled receptors.

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Salvia divinorum

Salvia divinorum (also known as sage of the diviners, ska maría pastora, seer's sage, yerba de la pastora or simply salvia) is a plant species with transient psychoactive properties when its leaves are consumed by chewing, smoking or as a tea.

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Salvinorin A

Salvinorin A is the main active psychotropic molecule in Salvia divinorum, a Mexican plant which has a long history of use as an entheogen by indigenous Mazatec shamans.

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Salvinorin B methoxymethyl ether

Salvinorin B methoxymethyl ether (2-O-methoxymethylsalvinorin B) is a semi-synthetic analogue of the natural product salvinorin A used in scientific research.

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SC-17599

SC-17599 is a steroid derivative drug discovered in 1968 which acts as a selective μ-opioid receptor agonist, with little or no affinity for the δ-opioid or κ-opioid receptors.

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Sigma receptor

Schematic σ receptor The sigma receptors σ1 and σ2 bind to ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine.

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Sigma-1 receptor

The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor.

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Sodium-hydrogen antiporter 3 regulator 1

Sodium-hydrogen antiporter 3 regulator 1 is a regulator of Sodium-hydrogen antiporter 3.

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Spiradoline

Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist.

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Tifluadom

Tifluadom is a benzodiazepine derivative with an unusual activity profile.

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Trevena Inc

Trevena Inc is a clinical stage biopharmaceutical company, headquartered in Chesterbrook, Pennsylvania, USA, and is involved in the discovery and development of G-protein coupled receptors (GPCR) biased ligands.

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U-50488

U-50488 is a drug which acts as a highly selective κ-opioid agonist, but without any μ-opioid antagonist effects.

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U-69,593

U-69,593 is a drug which acts as a potent and selective κ1-opioid receptor agonist.

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U-77891

U-77891 is an opioid analgesic drug that was first synthesized in 1983 by the Upjohn company.

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Ubiquitin C

Polyubiquitin-C is a protein encoded by the UBC gene in humans.

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18,19-Dehydrobuprenorphine

18,19-Dehydrobuprenorphine (HS-599) is a derivative of buprenorphine.

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18-Methoxycoronaridine

(–)-18-Methoxycoronaridine (18-MC) is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont.

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2-Methoxyethyl-18-methoxycoronaridinate

(–)-2-Methoxyethyl-18-methoxycoronaridinate (ME-18-MC) is a second generation synthetic derivative of ibogaine developed by the research team led by the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont.

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25I-NBOMe

25I-NBOMe (2C-I-NBOMe, Cimbi-5, also shortened to "25I") is a psychedelic hallucinogen that is used in biochemistry research for mapping the brains usage of the type 2A serotonin receptor and later also has been used for recreational purpose.

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5'-Guanidinonaltrindole

5'-Guanidinonaltrindole (5'-GNTI) is an opioid antagonist used in scientific research which is highly selective for the κ opioid receptor.

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5-MeO-DALT

5-MeO-DALT or N,N-di allyl-5-methoxy tryptamine is a psychedelic tryptamine first synthesized by Alexander Shulgin.

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8-Carboxamidocyclazocine

8-Carboxamidocyclazocine (8-CAC) is an opioid analgesic drug related to cyclazocine, invented by medicinal chemist Mark P. Wentland and co-workers in Cogswell Laboratory at Rensselaer Polytechnic Institute.

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K Opioid, K Opioid receptors, K-Opioid, K-Opioid receptor, K-Opioid receptors, K-opioid receptor, Kappa Opioid, Kappa Opioid Receptor Agonist, Kappa Opioid receptor, Kappa Opioid receptors, Kappa agonist, Kappa opioid receptor, Kappa receptor, Kappa receptor agonist, Kappa-Opioid, Kappa-Opioid receptor, Kappa-Opioid receptors, Kappa-opioid receptor, OPRK1, OPRK1 (gene), Κ-Opioid receptor.

References

[1] https://en.wikipedia.org/wiki/Κ-opioid_receptor

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