Kappa-type opioid receptor

Details

Name
Kappa-type opioid receptor
Synonyms
  • K-OR-1
  • OPRK
Gene Name
OPRK1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0001260|Kappa-type opioid receptor
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
Number of residues
380
Molecular Weight
42644.665
Theoretical pI
7.79
GO Classification
Functions
dynorphin receptor activity / neuropeptide binding / opioid receptor activity
Processes
adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway / adenylate cyclase-inhibiting opioid receptor signaling pathway / behavior / behavioral response to cocaine / cellular response to lipopolysaccharide / defense response to virus / eating behavior / estrous cycle / immune response / locomotory behavior / maternal behavior / negative regulation of luteinizing hormone secretion / neuropeptide signaling pathway / opioid receptor signaling pathway / phospholipase C-activating G-protein coupled receptor signaling pathway / positive regulation of dopamine secretion / positive regulation of locomotion / positive regulation of p38MAPK cascade / positive regulation of potassium ion transmembrane transport / regulation of aerobic respiration / regulation of energy homeostasis / regulation of saliva secretion / regulation of sensory perception of pain / response to acrylamide / response to estrogen / response to ethanol / response to insulin / response to morphine / response to radiation / sensory perception / sensory perception of pain / sensory perception of temperature stimulus / synaptic transmission
Components
axon terminus / dendrite / integral component of membrane / integral component of plasma membrane / neuron projection / perikaryon / plasma membrane / synapse
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions.
Pfam Domain Function
Transmembrane Regions
58-85 96-119 133-154 174-196 223-247 275-296 312-333
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0021645|Kappa-type opioid receptor (OPRK1)
ATGGACTCCCCGATCCAGATCTTCCGCGGGGAGCCGGGCCCTACCTGCGCCCCGAGCGCC
TGCCTGCCCCCCAACAGCAGCGCCTGGTTTCCCGGCTGGGCCGAGCCCGACAGCAACGGC
AGCGCCGGCTCGGAGGACGCGCAGCTGGAGCCCGCGCACATCTCCCCGGCCATCCCGGTC
ATCATCACGGCGGTCTACTCCGTAGTGTTCGTCGTGGGCTTGGTGGGCAACTCGCTGGTC
ATGTTCGTGATCATCCGATACACAAAGATGAAGACAGCAACCAACATTTACATATTTAAC
CTGGCTTTGGCAGATGCTTTAGTTACTACAACCATGCCCTTTCAGAGTACGGTCTACTTG
ATGAATTCCTGGCCTTTTGGGGATGTGCTGTGCAAGATAGTAATTTCCATTGATTACTAC
AACATGTTCACCAGCATCTTCACCTTGACCATGATGAGCGTGGACCGCTACATTGCCGTG
TGCCACCCCGTGAAGGCTTTGGACTTCCGCACACCCTTGAAGGCAAAGATCATCAATATC
TGCATCTGGCTGCTGTCGTCATCTGTTGGCATCTCTGCAATAGTCCTTGGAGGCACCAAA
GTCAGGGAAGACGTCGATGTCATTGAGTGCTCCTTGCAGTTCCCAGATGATGACTACTCC
TGGTGGGACCTCTTCATGAAGATCTGCGTCTTCATCTTTGCCTTCGTGATCCCTGTCCTC
ATCATCATCGTCTGCTACACCCTGATGATCCTGCGTCTCAAGAGCGTCCGGCTCCTTTCT
GGCTCCCGAGAGAAAGATCGCAACCTGCGTAGGATCACCAGACTGGTCCTGGTGGTGGTG
GCAGTCTTCGTCGTCTGCTGGACTCCCATTCACATATTCATCCTGGTGGAGGCTCTGGGG
AGCACCTCCCACAGCACAGCTGCTCTCTCCAGCTATTACTTCTGCATCGCCTTAGGCTAT
ACCAACAGTAGCCTGAATCCCATTCTCTACGCCTTTCTTGATGAAAACTTCAAGCGGTGT
TTCCGGGACTTCTGCTTTCCACTGAAGATGAGGATGGAGCGGCAGAGCACTAGCAGAGTC
CGAAATACAGTTCAGGATCCTGCTTACCTGAGGGACATCGATGGGATGAATAAACCAGTA
TGA
Chromosome Location
8
Locus
8q11.2
External Identifiers
ResourceLink
UniProtKB IDP41145
UniProtKB Entry NameOPRK_HUMAN
GenBank Protein ID532060
GenBank Gene IDU11053
GenAtlas IDOPRK1
HGNC IDHGNC:8154
General References
  1. Mansson E, Bare L, Yang D: Isolation of a human kappa opioid receptor cDNA from placenta. Biochem Biophys Res Commun. 1994 Aug 15;202(3):1431-7. [Article]
  2. Simonin F, Gaveriaux-Ruff C, Befort K, Matthes H, Lannes B, Micheletti G, Mattei MG, Charron G, Bloch B, Kieffer B: 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. 1995 Jul 18;92(15):7006-10. [Article]
  3. Zhu J, Chen C, Xue JC, Kunapuli S, DeRiel JK, Liu-Chen LY: Cloning of a human kappa opioid receptor from the brain. Life Sci. 1995;56(9):PL201-7. [Article]
  4. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [Article]
  5. Nusbaum C, Mikkelsen TS, Zody MC, Asakawa S, Taudien S, Garber M, Kodira CD, Schueler MG, Shimizu A, Whittaker CA, Chang JL, Cuomo CA, Dewar K, FitzGerald MG, Yang X, Allen NR, Anderson S, Asakawa T, Blechschmidt K, Bloom T, Borowsky ML, Butler J, Cook A, Corum B, DeArellano K, DeCaprio D, Dooley KT, Dorris L 3rd, Engels R, Glockner G, Hafez N, Hagopian DS, Hall JL, Ishikawa SK, Jaffe DB, Kamat A, Kudoh J, Lehmann R, Lokitsang T, Macdonald P, Major JE, Matthews CD, Mauceli E, Menzel U, Mihalev AH, Minoshima S, Murayama Y, Naylor JW, Nicol R, Nguyen C, O'Leary SB, O'Neill K, Parker SC, Polley A, Raymond CK, Reichwald K, Rodriguez J, Sasaki T, Schilhabel M, Siddiqui R, Smith CL, Sneddon TP, Talamas JA, Tenzin P, Topham K, Venkataraman V, Wen G, Yamazaki S, Young SK, Zeng Q, Zimmer AR, Rosenthal A, Birren BW, Platzer M, Shimizu N, Lander ES: DNA sequence and analysis of human chromosome 8. Nature. 2006 Jan 19;439(7074):331-5. [Article]
  6. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  7. Wang JB, Johnson PS, Wu JM, Wang WF, Uhl GR: Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras. J Biol Chem. 1994 Oct 21;269(42):25966-9. [Article]
  8. Li JG, Chen C, Liu-Chen LY: 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. 2002 Jul 26;277(30):27545-52. Epub 2002 May 9. [Article]
  9. Chen C, Li JG, Chen Y, Huang P, Wang Y, Liu-Chen LY: GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor. J Biol Chem. 2006 Mar 24;281(12):7983-93. Epub 2006 Jan 23. [Article]
  10. Li JG, Chen C, Liu-Chen LY: N-Glycosylation of the human kappa opioid receptor enhances its stability but slows its trafficking along the biosynthesis pathway. Biochemistry. 2007 Sep 25;46(38):10960-70. Epub 2007 Aug 21. [Article]
  11. Wang YH, Sun JF, Tao YM, Chi ZQ, Liu JG: The role of kappa-opioid receptor activation in mediating antinociception and addiction. Acta Pharmacol Sin. 2010 Sep;31(9):1065-70. doi: 10.1038/aps.2010.138. Epub 2010 Aug 23. [Article]
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Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00454MeperidineapprovedyesDetails
DB00611Butorphanolapproved, illicit, vet_approvedyesagonistDetails
DB00844NalbuphineapprovedyesagonistDetails
DB00921Buprenorphineapproved, illicit, investigational, vet_approvedyesantagonistDetails
DB00318Codeineapproved, illicityesagonistDetails
DB00327Hydromorphoneapproved, illicityesagonistDetails
DB00647Dextropropoxypheneapproved, illicit, investigational, withdrawnyesantagonistDetails
DB01209Dezocineapproved, investigationalyesantagonistDetails
DB00652Pentazocineapproved, vet_approvedyesagonistDetails
DB00295Morphineapproved, investigationalyesagonistDetails
DB00370MirtazapineapprovedunknownagonistDetails
DB00704Naltrexoneapproved, investigational, vet_approvedyesantagonistDetails
DB015713-MethylfentanylillicityesagonistDetails
DB01497Etorphineillicit, vet_approvedyesagonistDetails
DB05046V1003investigationalunknownDetails
DB05104AsimadolineinvestigationalunknownDetails
DB05155CR665investigationalunknownDetails
DB05443ADL 10-0101investigationalunknownDetails
DB00497Oxycodoneapproved, illicit, investigationalyesagonistDetails
DB00193Tramadolapproved, investigationalunknownagonistDetails
DB06204TapentadolapprovedunknownDetails
DB06409Morphine glucuronideinvestigationalunknownDetails
DB01452Diamorphineapproved, illicit, investigationalunknownagonistDetails
DB00708Sufentanilapproved, investigationalunknownDetails
DB01535Carfentanilillicit, investigational, vet_approvedunknownagonistDetails
DB00321AmitriptylineapprovedunknownagonistDetails
DB00854LevorphanolapprovedunknownagonistDetails
DB01565Dihydromorphineexperimental, illicitunknownagonistDetails
DB01183Naloxoneapproved, vet_approvedyesantagonistDetails
DB00813Fentanylapproved, illicit, investigational, vet_approvedunknownagonistDetails
DB00825LevomentholapprovedunknownagonistDetails
DB014393-Methylthiofentanylexperimental, illicityesagonistDetails
DB01548Diprenorphineillicit, vet_approvedunknownantagonistDetails
DB00836LoperamideapprovedunknownagonistDetails
DB06274Alvimopanapproved, investigationalunknownantagonistDetails
DB00899RemifentanilapprovedunknownagonistDetails
DB06800MethylnaltrexoneapprovednoantagonistDetails
DB06738KetobemidoneinvestigationalyesagonistDetails
DB00514DextromethorphanapprovedunknownagonistDetails
DB00396Progesteroneapproved, vet_approvedunknownactivatorpotentiatorDetails
DB01221Ketamineapproved, vet_approvedunknownagonistDetails
DB06148Mianserinapproved, investigationalunknownagonistDetails
DB09272Eluxadolineapproved, investigationalyesagonistDetails
DB06230Nalmefeneapproved, investigational, withdrawnyespartial agonistDetails
DB11691Naldemedineapproved, investigationalyesantagonistDetails
DB00555Lamotrigineapproved, investigationalunknowninhibitorDetails
DB09209Pholcodineapproved, illicityesantagonistDetails
DB11130Opiumapproved, illicityesagonistDetails
DB11186Pentoxyverineapproved, investigational, withdrawnunknownagonistDetails
DB14146LoxicodegolinvestigationalunknownagonistDetails
DB00289Atomoxetineapprovedunknownpartial agonistDetails
DB09173ButyrfentanylillicitunknownagonistDetails
DB01238Aripiprazoleapproved, investigationalunknownligandDetails
DB06288Amisulprideapproved, investigationalnoagonistDetails
DB12543Samidorphanapproved, investigationalunknownpartial agonistDetails
DB11938Difelikefalinapproved, investigationalyesagonistDetails