Kappa opioid receptor
opioid receptor, kappa 1
|Locus||Chr. 8 q11.2|
The κ-Opioid receptors are a class of opioid receptors with dynorphins as the primary endogenous ligands, and ketazocine as a potent selective exogenous ligand. There are three variants: κ1, κ2, and κ3.
It has long been believed that kappa-opioid receptor agonists are dysphoric. This misconception traces back to early articles in the 1980s about human tests with κ-opioid receptor agonists. It was stated that:
It is now widely accepted that κ-opioid receptor (partial) agonists have hallucinogenic ("psychotomimetic") effects, as exemplified by salvinorin A. These effects are generally undesirable in medicinal drugs and could have had frightening or disturbing effects in the tested humans, but they are not per se dysphoric. It is thought that the hallucinogenic effects of drugs such as butorphanol, nalbuphine, and pentazocine serve to limit their opiate abuse potential. In the case of salvinorin A, a structurally novel neoclerodane diterpene κ-opioid receptor agonist, thes hallucinogenic effects are sought after. While salvinorin A is considered a hallucinogen, its effects are qualitatively different than those produced by the classical psychedelic hallucinogens such as LSD or mescaline. 
These receptors are involved with analgesia.
κ receptors are located in the periphery by pain neurons, in the spinal cord and in the brain.
- ↑ Human psychopharmacology of ketocyclazocine as compared with cyclazocine, morphine and placebo J. Pharmacol. Exp. Ther. 238(3): 960-968 (1986) PMID 3018228
- ↑ Roth B, Baner K, Westkaemper R, Siebert D, Rice K, Steinberg S, Ernsberger P, Rothman R (2002). "Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist". Proc Natl Acad Sci U S A 99 (18): 11934-9. PMID 12192085. link
|Hypothalamic hormone receptors||CRH - FSH - LHRH - TRH - Somatostatin|
|Pituitary hormone receptors||Vasopressin (1A, 1B, 2) - Oxytocin - LHCG - Type I cytokine receptor (GH, Prolactin) - TSH|
|Other hormone receptors||Atrial natriuretic factor - Calcitonin - Cholecystokinin (A, B) - VIP|
|Opioid receptors||Delta - Kappa - Mu - Sigma (1, 2) - Nociceptin|
|Other neuropeptide receptors||Angiotensin - Bradykinin (B1, B2) / Tachykinin (TACR1) - Calcitonin gene-related peptide - Galanin - GPCR neuropeptide (B/W, FF, S, Y) - Neurotensin|
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