Found in numerous species of mint, including peppermintspearmintand watermintthe naturally-occurring compound menthol is a weak KOR agonist  owing to its antinociceptiveor pain blocking, effects in rats. It has also been reported that the KOR system is critical for stress-induced drug-seeking. The key compound in Salvia divinorumsalvinorin Ais known as a powerful, short-acting KOR agonist. An Introduction to Medicinal Chemistry. Biochemical and Biophysical Research Communications.
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The involvement of the KOR in stressas well as in consequences of chronic stress such as depressionanxietyanhedoniaand increased drug-seeking behaviorhas been made clear. Delta Kappa Mu Nociceptin. Journal of Cerebral Blood Flow and Metabolism. Though cocaine abuse is a frequently used model of addiction, KOR agonists have very marked effects on all types of addiction including alcohol, cocaine and opiate abuse.
Annals of the New York Academy of Sciences.
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Benzomorphans Alazocine — partial agonist Bremazocine — highly selective 8-Carboxamidocyclazocine Cyclazocine — partial agonist Ketazocine Metazocine — partial agonist Pentazocine — partial agonist Phenazocine — partial agonist Morphinans 6'-Guanidinonaltrindole 6'-GNTI — biased ligand: These receptors modulate the release of other neurochemicals such as serotonin in the case of MOR agonists and acetylcholine in the case of D 2.
GPR 1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 A B B
|Although seemingly paradoxical, it is well known that drug taking results in a change from homeostasis to allostasis.
Centrally active KOR agonists have hallucinogenic or dissociative effects, as exemplified by salvinorin A the active constituent in Salvia divinorum. Tinder is popular among college-age people.
Agonists abridged; see here for a full list: The claustrum is the region of the brain in which the KOR is most densely expressed.