Kappa-type opioid receptor
Also known as: OPRK, OPRK1
Function
G protein-coupled opioid receptor that functions as a receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as a 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.
Classification
- Family (Pfam)
- PF00001 7tm_1
- InterPro
- GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Kappa_opi_rcpt, Opioid_rcpt
- Functional cluster
- Membrane Transporters & GPCRs
Experimental structures · PDB · 28
- 4DJH X-ray 2.90A
- 6B73 X-ray 3.10A
- 6VI4 X-ray 3.30A
- 7T10 EM 2.50A
- 7T11 EM 2.70A
- 7UL2 EM 2.40A
- 7UL3 EM 3.00A
- 7UL5 EM 3.10A
- 7Y1F EM 3.30A
- 7YIT X-ray 3.30A
- 7YMJ EM 3.35A
- 8DZP EM 2.71A
- … and 16 more
A predicted model is available from AlphaFold.
Gene Ontology · 46
- GO:0043679 axon terminus
- GO:0030425 dendrite
- GO:0016020 membrane
- GO:0005739 mitochondrion
- GO:0043005 neuron projection
- GO:0043204 perikaryon
- GO:0005886 plasma membrane
- GO:0045211 postsynaptic membrane
- GO:0042734 presynaptic membrane
- GO:0016529 sarcoplasmic reticulum
- GO:0030672 synaptic vesicle membrane
- GO:0030315 T-tubule
- GO:0038048 dynorphin receptor activity
- GO:0004985 G protein-coupled opioid receptor activity
- GO:0042923 neuropeptide binding
- GO:0033612 receptor serine/threonine kinase binding
- GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
- GO:0031635 adenylate cyclase-inhibiting opioid receptor signaling pathway
- GO:0048148 behavioral response to cocaine
- GO:0071333 cellular response to glucose stimulus
- GO:0071222 cellular response to lipopolysaccharide
- GO:0007268 chemical synaptic transmission
- GO:1990708 conditioned place preference
- GO:0051607 defense response to virus
- GO:0042755 eating behavior
- GO:0044849 estrous cycle
- GO:0038003 G protein-coupled opioid receptor signaling pathway
- GO:0006955 immune response
- GO:0007626 locomotory behavior
- GO:0042711 maternal behavior
- GO:0033685 negative regulation of luteinizing hormone secretion
- GO:0007218 neuropeptide signaling pathway
- GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway
- GO:0033603 positive regulation of dopamine secretion
- GO:1904000 positive regulation of eating behavior
- GO:1900745 positive regulation of p38MAPK cascade
- GO:1901381 positive regulation of potassium ion transmembrane transport
- GO:0046877 regulation of saliva secretion
- GO:1903937 response to acrylamide
- GO:0043627 response to estrogen
- GO:0045471 response to ethanol
- GO:0032868 response to insulin
- GO:0035094 response to nicotine
- GO:0007600 sensory perception
- GO:0019233 sensory perception of pain
- GO:0050951 sensory perception of temperature stimulus
Drugs targeting this protein · 30
- ASIMADOLINE agonist
- ANILERIDINE PHOSPHATE agonist
- OXYMORPHONE HYDROCHLORIDE agonist
- ANILERIDINE HYDROCHLORIDE agonist
- NALBUPHINE HYDROCHLORIDE agonist
- NALTREXONE HYDROCHLORIDE antagonist
- DEZOCINE antagonist
- NALOXONE HYDROCHLORIDE antagonist
- NALTREXONE antagonist
- ATICAPRANT antagonist
- LEVALLORPHAN TARTRATE partial agonist
- ONDELOPRAN antagonist
- SAMIDORPHAN L-MALATE partial agonist
- CEBRANOPADOL agonist
- BUPRENORPHINE HYDROCHLORIDE agonist
- BUTORPHANOL TARTRATE partial agonist
- BENZHYDROCODONE HYDROCHLORIDE agonist
- DEXTROMORAMIDE agonist
- HYDROCODONE BITARTRATE agonist
- AXOMADOL agonist
- DIFELIKEFALIN agonist
- CODEINE SULFATE agonist
- NAVACAPRANT antagonist
- ORP-101 antagonist
- NALFURAFINE HYDROCHLORIDE agonist
- BUPRENORPHINE agonist
- NALMEFENE HYDROCHLORIDE DIHYDRATE partial agonist
- NALOXONE HYDROCHLORIDE DIHYDRATE antagonist
- DIFELIKEFALIN ACETATE agonist
- CODEINE PHOSPHATE agonist
Related proteins · sequence + function similarity
- Kappa-type opioid receptor 0.99
- Kappa-type opioid receptor 0.99
- Kappa-type opioid receptor 0.99
- Kappa-type opioid receptor 0.99
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.96
- Mu-type opioid receptor 0.95
Co-cited proteins · studied together in the literature
- Na(+)/H(+) exchange regulatory cofactor NHE-RF1 1 shared papers
- Gamma-aminobutyric acid receptor-associated protein-like 1 1 shared papers
Literature · 13 cited papers
- Structure of the human kappa-opioid receptor in complex with JDTic. Nature · 2012
- The role of kappa-opioid receptor activation in mediating antinociception and addiction. Acta Pharmacol. Sin. · 2010
- Kinase cascades and ligand-directed signaling at the kappa opioid receptor. Psychopharmacology · 2010
- N-glycosylation of the human kappa opioid receptor enhances its stability but slows its trafficking along the biosynthesis pathway. Biochemistry · 2007
- GEC1 interacts with the kappa opioid receptor and enhances expression of the receptor. J. Biol. Chem. · 2006
- DNA sequence and analysis of human chromosome 8. Nature · 2006
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
- 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
- Isolation of a human kappa opioid receptor cDNA from placenta. Biochem. Biophys. Res. Commun. · 1994
- Human kappa opiate receptor second extracellular loop elevates dynorphin's affinity for human mu/kappa chimeras. J. Biol. Chem. · 1994
- Cloning of a human kappa opioid receptor from the brain. Life Sci. · 1995
- … and 1 more in the literature graph