Kappa Opioid receptor



Template:DISPLAYTITLE:kappa Opioid receptor

Opioid receptor, kappa 1
Identifiers
Symbol(s) OPRK1; KOR; OPRK
External IDs OMIM: 165196 MGI: 97439 Homologene: 20253
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 receptors are a class of dynorphins as the primary endogenous ligands, and ketazocine as a potent selective exogenous ligand. There are three variants: κ1, κ2, and κ3.

Effects

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 cyclazocine (fig. 2C). Morphine failed to increase scores significantly on this scale which measures dysphoria."[1]

It is now widely accepted that κ-opioid receptor (partial) agonists have mescaline.[2]

Activation of the κ-opioid receptor appears to antagonize many of the effects of the μ opioid receptor.[3]

Kappa ligands are also known for their characteristic antidiuretic hormone (ADH).[4]

Kappa agonism is neuroprotective against hypoxia/ischemia; as such, kappa receptors may represent a novel therapeutic target.[5]

Location

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

Reversal

Non-specific opioid receptor antagonists (e.g., buprenorphine can be used to reverse the effects of kappa agonists.

References

  1. ^ 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.
  2. ^ Roth BL, Baner K, Westkaemper R, Siebert D, Rice KC, Steinberg S, Ernsberger P, Rothman RB (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.
  3. ^ Pan ZZ (1998). "mu-Opposing actions of the kappa-opioid receptor". Trends Pharmacol. Sci. 19 (3): 94–8. doi:10.1016/S0165-6147(98)01169-9. PMID 9584625.
  4. ^ 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.
  5. ^ 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.

Further reading

  • Hatzoglou A, Bakogeorgou E, Kampa M, et al. (2000). "Somatostatin and opioid receptors in mammary tissue. Role in cancer cell growth.". Adv. Exp. Med. Biol. 480: 55-63. PMID 10959409.
  • Narita M, Funada M, Suzuki T (2001). "Regulations of opioid dependence by opioid receptor types.". Pharmacol. Ther. 89 (1): 1-15. PMID 11316510.
  • Simonin F, Gavériaux-Ruff C, Befort K, et al. (1995). "kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system.". Proc. Natl. Acad. Sci. U.S.A. 92 (15): 7006-10. PMID 7624359.
  • Zhu J, Chen C, Xue JC, et al. (1995). "Cloning of a human kappa opioid receptor from the brain.". Life Sci. 56 (9): PL201-7. PMID 7869844.
  • Wang JB, Johnson PS, Wu JM, et al. (1994). "Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras.". J. Biol. Chem. 269 (42): 25966-9. PMID 7929306.
  • Mansson E, Bare L, Yang D (1994). "Isolation of a human kappa opioid receptor cDNA from placenta.". Biochem. Biophys. Res. Commun. 202 (3): 1431-7. PMID 8060324.
  • Yasuda K, Espinosa R, Takeda J, et al. (1994). "Localization of the kappa opioid receptor gene to human chromosome band 8q11.2.". Genomics 19 (3): 596-7. doi:10.1006/geno.1994.1117. PMID 8188308.
  • Chao CC, Gekker G, Hu S, et al. (1996). "kappa opioid receptors in human microglia downregulate human immunodeficiency virus 1 expression.". Proc. Natl. Acad. Sci. U.S.A. 93 (15): 8051-6. PMID 8755601.
  • Lee JW, Joshi S, Chan JS, Wong YH (1998). "Differential coupling of mu-, delta-, and kappa-opioid receptors to G alpha16-mediated stimulation of phospholipase C.". J. Neurochem. 70 (5): 2203-11. PMID 9572309.
  • Chatzaki E, Margioris AN, Makrigiannakis A, et al. (2000). "Kappa opioids and TGFbeta1 interact in human endometrial cells.". Mol. Hum. Reprod. 6 (7): 602-9. PMID 10871647.
  • Gomes I, Jordan BA, Gupta A, et al. (2001). "Heterodimerization of mu and delta opioid receptors: A role in opiate synergy.". J. Neurosci. 20 (22): RC110. PMID 11069979.
  • Mathieu-Kia AM, Fan LQ, Kreek MJ, et al. (2001). "Mu-, delta- and kappa-opioid receptor populations are differentially altered in distinct areas of postmortem brains of Alzheimer's disease patients.". Brain Res. 893 (1-2): 121-34. PMID 11223000.
  • Lokensgard JR, Gekker G, Peterson PK (2002). "Kappa-opioid receptor agonist inhibition of HIV-1 envelope glycoprotein-mediated membrane fusion and CXCR4 expression on CD4(+) lymphocytes.". Biochem. Pharmacol. 63 (6): 1037-41. PMID 11931835.
  • Li JG, Chen C, Liu-Chen LY (2002). "Ezrin-radixin-moesin-binding phosphoprotein-50/Na+/H+ exchanger regulatory factor (EBP50/NHERF) blocks U50,488H-induced down-regulation of the human kappa opioid receptor by enhancing its recycling rate.". J. Biol. Chem. 277 (30): 27545-52. doi:10.1074/jbc.M200058200. PMID 12004055.
  • Suzuki S, Chuang LF, Yau P, et al. (2002). "Interactions of opioid and chemokine receptors: oligomerization of mu, kappa, and delta with CCR5 on immune cells.". Exp. Cell Res. 280 (2): 192-200. PMID 12413885.
  • Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899-903. doi:10.1073/pnas.242603899. PMID 12477932.
  • McLaughlin JP, Xu M, Mackie K, Chavkin C (2003). "Phosphorylation of a carboxyl-terminal serine within the kappa-opioid receptor produces desensitization and internalization.". J. Biol. Chem. 278 (36): 34631-40. doi:10.1074/jbc.M304022200. PMID 12815037.
  • Ota T, Suzuki Y, Nishikawa T, et al. (2004). "Complete sequencing and characterization of 21,243 full-length human cDNAs.". Nat. Genet. 36 (1): 40-5. doi:10.1038/ng1285. PMID 14702039.
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This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Kappa_Opioid_receptor". A list of authors is available in Wikipedia.