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14-September-2008 18:02:43 - kappa Opioid receptor Notepad To comply with 's quality standards, this article may need to be rewritten. The discussion page may contain suggestions. Opioid receptor, kappa 1 Identifiers Symbols OPRK1; KOR; OPRK External IDs OMIM: 165196 MGI: 97439 HomoloGene: 20253 Gene ontology Molecular function: rhodopsin-like receptor activity receptor activity kappa-opioid receptor activity Cellular component: integral to plasma membrane membrane integral to membrane Biological process: immune response signal transduction G-protein coupled receptor protein signaling pathway G-protein signaling, adenylate cyclase inhibiting pathway synaptic transmission sensory perception behavior viral genome replication RNA expression pattern More reference expression data Orthologs Human Mouse Entrez 4986 18387 Ensembl ENSG00000082556 ENSMUSG00000025905 Uniprot P41145 Q14AL5 Refseq NM_000912 mRNA NP_000903 protein NM_011011 mRNA NP_035141 protein Location Chr 8: 54.3 - 54.33 Mb Chr 1: 5.58 - 5.59 Mb Pubmed search 1 2 The κ-Opioid receptor is a type of opioid receptor which binds the peptide opioid dynorphin as the primary endogenous ligand.1 κ receptors are widely distributed in the brain, spinal cord, and in pain neurons.2 Contents 1 Receptor subtypes 2 Signal transduction 3 Ligands 4 Function 5 References 6 External links Receptor subtypes Based on receptor binding studies, three variants of the κ-opioid receptor designated κ1, κ2, and κ3 have been characterized.34 However only one cDNA clone has been identified,5 hence these receptor subtypes likely arise from interaction of one κ-opioid receptor protein with other membrane associated proteins.6 Signal transduction κ-Opioid receptor activation by agonists is coupled to the G protein Gi/G0, which subsequently increases phosphodiesterase activity. Phosphodiesterases break down cAMP, producing an inhibitory effect in neurons.789 κ-Opioid receptors also couple to inward-rectifier potassium10 and to N-type calcium ion channels.11 Ligands The synthetic alkaloid ketazocine12 and terpenoid natural product salvinorin A13 are potent and selective κ-opioid receptor agonists. The κ-opioid receptor also mediates the action of the hallucinogenic side effects of opioids such as pentazocine.14 Function 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: Both doses of ketocyclazocine substantially elevated scores on the LSD subscale of the ARCI as did the high dose of cyclazocine fig. 2C. Morphine failed to increase scores significantly on this scale which measures dysphoria.15 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. 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, these 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.13 The involvement of the kappa-opioid receptor in stress response has been elucidated.16 Activation of the κ-opioid receptor appears to antagonize many of the effects of the μ opioid receptor.17 Kappa ligands are also known for their characteristic diuretic effects, due to their negative regulation of antidiuretic hormone ADH.18 Kappa agonism is neuroprotective against hypoxia/ischemia; as such, kappa receptors may represent a novel therapeutic target.19 References ^ James IF, Chavkin C, Goldstein A 1982. Selectivity of dynorphin for kappa opioid receptors. Life Sci. 31 12-13: 1331-4. PMID 6128656. ^ Mansour A, Fox CA, Akil H, Watson SJ January 1995. Opioid-receptor mRNA expression in the rat CNS: anatomical and functional implications. Trends Neurosci. 18 1: 22-9. PMID 7535487. ^ de Costa BR, Rothman RB, Bykov V, Jacobson AE, Rice KC February 1989. Selective and enantiospecific acylation of kappa opioid receptors by 1S,2S-trans-2-isothiocyanato-N-methyl-N-2-1-pyrrolidinyl cyclohexy l benzeneacetamide. Demonstration of kappa receptor heterogeneity. J. Med. Chem. 32 2: 281-3. PMID 2536435. ^ Rothman RB, France CP, Bykov V, De Costa BR, Jacobson AE, Woods JH, Rice KC August 1989. Pharmacological activities of optically pure enantiomers of the kappa opioid agonist, U50,488, and its cis diastereomer: evidence for three kappa receptor subtypes. Eur. J. Pharmacol. 167 3: 345-53. PMID 2553442. ^ Mansson E, Bare L, Yang D August 1994. Isolation of a human kappa opioid receptor cDNA from placenta. Biochem. Biophys. Res. Commun. 202 3: 1431-7. doi:10.1006/bbrc.1994.2091. PMID 8060324. ^ Jordan BA, Devi LA June 1999. G-protein-coupled receptor heterodimerization modulates receptor function. Nature 399 6737: 697-700. doi:10.1038/21441. PMID 10385123. ^ Lawrence DM, Bidlack JM September 1993. The kappa opioid receptor expressed on the mouse R1.1 thymoma cell line is coupled to adenylyl cyclase through a pertussis toxin-sensitive guanine nucleotide-binding regulatory protein. J. Pharmacol. Exp. Ther. 266 3: 1678-83. PMID 8103800. ^ Konkoy CS, Childers SR January 1993. Relationship between kappa 1 opioid receptor binding and inhibition of adenylyl cyclase in guinea pig brain membranes. Biochem. Pharmacol. 45 1: 207-16. PMID 8381004. ^ Schoffelmeer AN, Rice KC, Jacobson AE, et al September 1988. Mu-, delta- and kappa-opioid receptor-mediated inhibition of neurotransmitter release and adenylate cyclase activity in rat brain slices: studies with fentanyl isothiocyanate. Eur. J. Pharmacol. 154 2: 169-78. PMID 2906610. ^ Henry DJ, Grandy DK, Lester HA, Davidson N, Chavkin C March 1995. Kappa-opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes. Mol. Pharmacol. 47 3: 551-7. PMID 7700253. ^ Tallent M, Dichter MA, Bell GI, Reisine T December 1994. The cloned kappa opioid receptor couples to an N-type calcium current in undifferentiated PC-12 cells. Neuroscience 63 4: 1033-40. PMID 7700508. ^ Pasternak GW June 1980. Multiple opiate receptors: 3Hethylketocyclazocine receptor binding and ketocyclazocine analgesia. Proc. Natl. Acad. Sci. U.S.A. 77 6: 3691-4. PMID 6251477. ^ a b Roth BL, Baner K, Westkaemper R, et al September 2002. Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. Proc. Natl. Acad. Sci. U.S.A. 99 18: 11934-9. doi:10.1073/pnas.182234399. PMID 12192085. ^ Holtzman SG February 1985. Drug discrimination studies. Drug Alcohol Depend 14 3-4: 263-82. PMID 2859972. ^ Kumor KM, Haertzen CA, Johnson RE, Kocher T, Jasinski D 1986. Human psychopharmacology of ketocyclazocine as compared with cyclazocine, morphine and placebo. J. Pharmacol. Exp. Ther. 238 3: 960-8. PMID 3018228. ^ Benjamin B. Land, Michael R. Bruchas, Julia C. Lemos, Mei Xu, Erica J. Melief, and Charles Chavkin 2008. The Dysphoric Component of Stress Is Encoded by Activation of the Dynorphin kappa-Opioid System. J. Neurosci. 28 2: 407-414. doi:10.1523. PMID 18184783. ^ Pan ZZ 1998. mu-Opposing actions of the kappa-opioid receptor. Trends Pharmacol. Sci. 19 3: 94-8. doi:10.1016/S0165-61479801169-9. PMID 9584625. ^ Yamada K, Imai M, Yoshida S 1989. Mechanism of diuretic action of U-62,066E, a kappa opioid receptor agonist. Eur. J. Pharmacol. 160 2: 229-37. PMID 2547626. ^ Zeynalov E, Nemoto M, Hurn PD, Koehler RC, Bhardwaj A 2006. Neuroprotective effect of selective kappa opioid receptor agonist is gender specific and linked to reduced neuronal nitric oxide. J. Cereb. Blood Flow Metab. 26 3: 414-20. doi:10.1038/sj.jcbfm.9600196. PMID 16049424. External links κ opioid receptor. IUPHAR Receptor Database. International Union of Pharmacology 2007-10-15. Retrieved on 2008-05-18. MeSH kappa+Opioid+Receptor v d e Transmembrane receptor: G protein-coupled receptors Class A: Rhodopsin like Adrenergic α1 A, B, D, α2 A, B, C, β1, β2, β3 Eicosanoid CysLT 1, 2, LTB4 1, 2, FPRL1, OXE, Prostaglandin DP, EP 1, 2, 3, 4, PGF, Prostacyclin, Thromboxane Neuropeptide B/W 1, 2, FF 1, 2, S, Y 1, 2, 4, 5 Orphan 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, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182 Purinergics Adenosine A1, A2a, A2b, A3, P2Y, 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14 Serotonin all but 5-HT3 5-HT1 A, B, D, E, F, 5-HT2 A, B, C, 5-HT 4, 5A, 6, 7 Other Acetylcholine M1, M2, M3, M4, M5 - Adrenomedullin - Anaphylatoxin C3a, C5a - Angiotensin 1, 2 - Apelin - Bile acid - Bombesin BRS3, GRPR, NMBR - Bradykinin B1, B2 - Cannabinoid CB1, CB2 - Chemokine - Cholecystokinin A, B - Dopamine D1, D2, D3, D4, D5 - EBI2 - Endothelin A, B - Estrogen - Formyl peptide 1, L1, L2 - Free fatty acid 1, 2, 3, 4 - FSH - Galanin 1, 2, 3 - Gonadotropin-releasing hormone 1, 2 - Ghrelin - Histamine H1, H2, H3, H4 - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid 1, 2, 3, 4, 5, 6, 7, 8 - MAS 1, 1L, D, E, F, G, X1, X2, X3, X4 - Melanocortin 1, 2, 3, 4, 5 - MCHR 1, 2 - Melatonin 1A, 1B- Motilin - neuromedin B, U 1, 2 - Neurotensin 1, 2 - Opioid Delta, Kappa, Mu, Nociceptin, but not Sigma - Olfactory - Opsin 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH - Orexin 1, 2 - Oxytocin - Oxoglutarate - PAF - Prokineticin 1, 2 - Prolactin-releasing peptide - Protease-activated 1, 2, 3, 4 - Relaxin 1, 2, 3, 4 - Somatostatin 1, 2, 3, 4, 5 - SREB - Succinate - TAAR 1, 2, 3, 5, 6, 8, 9 - Tachykinin 1, 2, 3 - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin 1A, 1B, 2 Class B: Secretin like Brain-specific angiogenesis inhibitor 1, 2, 3 - Cadherin 1, 2, 3 - Calcitonin - CD97 - Corticotropin-releasing hormone 1, 2 - EMR 1, 2, 3 - Glucagon GR, GIPR, GLP1R, GLP2R - Growth hormone releasing hormone - PACAPR1- GPR 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157 - Latrophilin 1, 2, 3, ELTD1 - Parathyroid hormone 1, 2 - Secretin - Vasoactive intestinal peptide 1, 2 Class C: Metabotropic glutamate / pheromone Calcium-sensing receptor - GABA B 1, 2 - Glutamate receptor Metabotropic glutamate 1, 2, 3, 4, 5, 6, 7, 8 - GPRC6A - GPR 156, 158, 179 - RAIG 1, 2, 3, 4 - Taste receptors TAS1R 1, 2, 3 TAS2R 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50 Frizzled / Smoothened Frizzled 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 - Smoothened v d e Neuropeptide receptors 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 Retrieved from http://en..org/wiki/Kappa_Opioid_receptor Categories: Genes on chromosome 8 | Human proteins | Cell signaling | Signal transduction | Opioid receptorHidden categories: articles needing rewrite | Protein pages needing a picture Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 8 July 2008, at 02:28
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