Kappa opioid receptor

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opioid receptor, kappa 1
Identifiers
Symbol	OPRK1
HUGO	8154
Entrez	4986
OMIM	165196
RefSeq	NM_000912
UniProt	P41145
Other data
Locus	Chr. 8 q11.2

κ-Opioid receptors are also involved with analgesia, but activation also produces marked nausea and dysphoria.

Kappa ligands are also known for their characteristic diuretic effects, due to their negative regulation of antidiuretic hormone (ADH).

Kappa agonism is neuroprotective against hypoxia\ischemia, as such, kappa receptors may represent a novel therapeutic target.

The endogenous ligands for the Kappa receptor are the dynorphins.

κ receptors are located in the periphery by pain neurons, in the spinal cord and in the brain.

Kappa agonists whether full or partial produce psychotomimetic effects. In the case of the mixed (partial) agonist/antagonist analgesic drugs e.g. butorphanol, nalbuphine and buprenorphine the psychotomimesis is undesirable and serves to limit abuse potential.

In the case of Salvinorin A, a structurally novel neoclerodane diterpene Kappa ligand, these effects are sought after. While Salvinorin A is considered a hallucinogen by those to whom it is known, its effects are qualitatively different than those produced by the classical indoleamine hallucinogens. ^[1]

[edit] References

^ 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