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κ receptor

Family: Opioid receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Selected 3D Structures
Agonists
Antagonists
Allosteric Regulators
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 380 8q11.2 OPRK1 opioid receptor, kappa 1 50,81,102
Mouse 7 380 1 A2-A3 Oprk1 opioid receptor, kappa 1 6,37,46,60,98
Rat 7 380 5q11 Oprk1 opioid receptor, kappa 1 12,45,52-53,59
Previous and Unofficial Names
KOR
KOR-1
OP2
Kappa opioid receptor
KOP
K-OR-1
kappa-type opioid receptor
opioid receptor, kappa 1
Oprk2
R21
KOP-r
Database Links
ChEMBL Target 137 (Hs), 10008 (Mm), 10527 (Rn)
DrugBank Target 696 (Hs)
Ensembl ENSG00000082556 (Hs), ENSMUSG00000025905 (Mm), ENSRNOG00000007647 (Rn)
Entrez Gene 4986 (Hs), 18387 (Mm), 29335 (Rn)
GeneCards OPRK1 (Hs)
GenitoUrinary Development Molecular Anatomy Project Oprk1 (Mm)
HomoloGene 20253 (Hs)
Human Protein Reference Database 01309 (Hs)
InterPro P41145 (Hs), P33534 (Mm), P34975 (Rn)
KEGG Gene hsa:4986 (Hs), mmu:18387 (Mm), rno:29335 (Rn)
OMIM 165196 (Hs)
PhosphoSitePlus P41145 (Hs), P33534 (Mm), P34975 (Rn)
Protein Ontology (PRO) PRO:000001590 (Hs)
RefSeq Nucleotide NM_000912 (Hs), NM_011011 (Mm), NM_017167 (Rn)
RefSeq Protein NP_000903 (Hs), NP_035141 (Mm), NP_058863 (Rn)
TreeFam ENSG00000082556 (Hs), ENSMUSG00000025905 (Mm), ENSRNOG00000007647 (Rn)
UniGene Hs. 89455 (Hs)
UniProt P41145 (Hs), P33534 (Mm), P34975 (Rn)
Wikipedia κ receptor
Opioid receptors
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the human kappa opioid receptor in complex with JDTic
PDB Id:  4DJH
Resolution:  2.9Å
Species:  Human
References:  97
Search for other structures on the PDB
Search by keyword: Opioid receptors κ receptor Search by accession number: P34975, P41145, P33534
Natural/Endogenous Ligand(s)
α-neoendorphin {Sp: Human, Mouse, Rat}
β-endorphin {Sp: Rat} , β-endorphin {Sp: Human} , β-endorphin {Sp: Mouse}
β-neoendorphin {Sp: Human, Mouse, Rat}
big dynorphin {Sp: Human, Mouse, Rat}
dynorphin A {Sp: Human, Mouse, Rat}
dynorphin A-(1-13) {Sp: Human, Mouse, Rat}
dynorphin A-(1-8) {Sp: Human, Mouse, Rat}
dynorphin B {Sp: Human, Mouse, Rat}
[Leu]enkephalin {Sp: Human, Mouse, Rat}
[Met]enkephalin {Sp: Human, Mouse, Rat}
Comments: dynorphin A and big dynorphin are the highest potency endogenous ligands
Rank order of potency (Human)
big dynorphin > dynorphin A >> β-endorphin > [Leu]enkephalin > [Met]enkephalin
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
TRK820 Hs Full agonist 10.1 pKd 96
EKC Hs Full agonist 9.4 pKd 103
enadoline Hs Full agonist 8.6 – 9.2 pKd 26
[3H]U69593 Hs Full agonist 8.7 – 8.8 pKd 40,64,81
(-)-bremazocine Hs Partial agonist 10.5 pKi 91
dynorphin A {Sp: Human, Mouse, Rat} Rn Full agonist 10.0 – 10.3 pKi 45,52
(-)-cyclazocine Hs Partial agonist 10.0 pKi 91
dynorphin A-(1-13) {Sp: Human, Mouse, Rat} Hs Full agonist 9.3 – 10.7 pKi 64,91
(-)-EKC Hs Full agonist 10.0 pKi 91
dynorphin A-(1-13) {Sp: Human, Mouse, Rat} Rn Full agonist 9.9 pKi 52
dynorphin-(1-11) Hs Full agonist 9.7 pKi 91
etorphine Hs Full agonist 9.7 pKi 91
GR 89696 Hs Full agonist 9.7 pKi 69
U63640 Rn Full agonist 9.7 pKi 52
enadoline Hs Full agonist 9.6 pKi 31,58
dynorphin A {Sp: Human, Mouse, Rat} Hs Full agonist 8.3 – 10.8 pKi 64,81,91,102-103
dynorphin B {Sp: Human, Mouse, Rat} Rn Full agonist 9.5 pKi 52
naloxone benzoylhydrazone Hs Partial agonist 9.5 pKi 91
U69593 Hs Full agonist 9.5 pKi 40,91
α-neoendorphin {Sp: Human, Mouse, Rat} Rn Full agonist 8.9 – 10.0 pKi 45,52
α-neoendorphin {Sp: Human, Mouse, Rat} Hs Full agonist 8.3 – 10.2 pKi 81,102
β-neoendorphin {Sp: Human, Mouse, Rat} Rn Full agonist 9.1 pKi 52
E2078 Hs Full agonist 9.1 pKi 70
dynorphin B {Sp: Human, Mouse, Rat} Hs Partial agonist 8.1 – 9.9 pKi 64,81,91
U62066 Rn Full agonist 9.0 pKi 12
dynorphin A-(1-8) {Sp: Human, Mouse, Rat} Hs Full agonist 8.0 – 9.9 pKi 64,81,91,99
E2078 Rn Full agonist 8.8 pKi 52
EKC Rn Full agonist 8.8 pKi 52
ICI 204448 Rn Full agonist 8.8 pKi 12
tifluadom Hs Full agonist 8.8 pKi 103
U50488 Hs Partial agonist 7.8 – 9.7 pKi 11,64,81,91,102-103
(-)-pentazocine Hs Partial agonist 8.6 pKi 91
nalorphine Hs Partial agonist 7.9 – 9.1 pKi 91,103
U50488 Rn Partial agonist 8.2 – 8.7 pKi 12,45,52
U69593 Rn Full agonist 8.0 – 8.7 pKi 12,52
salvinorin A Hs Full agonist 7.8 – 8.7 pKi 9,73
β-neoendorphin {Sp: Human, Mouse, Rat} Hs Full agonist 7.9 pKi 81
(-)-pentazocine Hs Partial agonist 7.8 – 7.9 pKi 103
normorphine Hs Full agonist 7.8 pKi 91
nalbuphine Hs Full agonist 7.4 – 7.5 pKi 103
morphine Hs Partial agonist 7.3 pKi 91
β-endorphin {Sp: Human} Hs Partial agonist 6.3 – 7.9 pKi 81,91
dihydromorphine Hs Partial agonist 7.1 pKi 91
fentanyl Hs Partial agonist 7.1 pKi 91
etonitazene Hs Partial agonist 6.9 pKi 91
morphine Rn Partial agonist 6.7 – 7.0 pKi 12,52
β-endorphin {Sp: Human} Rn Full agonist 6.8 pKi 52
DAMGO Hs Partial agonist 6.5 pKi 91
(-)-methadone Hs Partial agonist 6.5 pKi 91
[Leu]enkephalin {Sp: Human, Mouse, Rat} Rn Full agonist 6.0 pKi 52
[Met]enkephalin {Sp: Human, Mouse, Rat} Rn Full agonist 6.0 pKi 52
DAMGO Rn Partial agonist 5.9 pKi 52
α-neoendorphin {Sp: Human, Mouse, Rat} Mm Full agonist 10.0 pIC50 98
dynorphin B {Sp: Human, Mouse, Rat} Mm Full agonist 10.0 pIC50 98
[D-Ala2,F5,Phe4]dynorphin-(1-17)-NH2 Mm Full agonist 9.7 pIC50 98
dynorphin-(1-17)-NH2 Mm Full agonist 9.7 pIC50 98
dynorphin A-(1-8) {Sp: Human, Mouse, Rat} Mm Full agonist 9.7 pIC50 98
(-)-bremazocine Mm Full agonist 9.5 pIC50 98
dynorphin A {Sp: Human, Mouse, Rat} Mm Full agonist 9.4 pIC50 98
[Met5]dynorphin-(1-17) Mm Full agonist 9.2 pIC50 98
EKC Mm Full agonist 9.0 pIC50 98
U50488 Mm Partial agonist 9.0 pIC50 98
U62066 Mm Full agonist 9.0 pIC50 98
U69593 Mm Full agonist 8.6 pIC50 98
ICI 204448 Mm Full agonist 8.2 pIC50 98
[D-Ala2,F5,Phe4]dynorphin-(1-13)-NH2 Mm Full agonist 7.7 pIC50 98
β-endorphin {Sp: Human} Mm Partial agonist 7.4 pIC50 98
nalbuphine Mm Full agonist 7.4 pIC50 98
View species-specific agonist tables
Agonist Comments
Ki values were determined in the absence of Na+ and GDP, except TRK820.

Discrimination of full or partial agonism is very dependent on the level of receptor expression and on the assay used to monitor agonist effects. Many agents may behave as full agonists or potent partial agonists in cell lines expressing cloned receptors in high concentration, but in other environments they may show only weak agonist activity. The identification of agonist activity in the table is largely based on the ability to stimulate GTPγS binding in cell lines expressing cloned human kappa receptors. Agents giving 85% or greater stimulation than that given by U69593 have been characterized as Full Agonists [91].

κ opioid receptors have been divided into several different subtypes, mainly on the basis of [3H]agonist binding assays. Generally 2 subtypes are recognised: κ1 and κ2. The benzeneacetamides and peptides are considered κ1 agonists and the benzomorphans bind to κ1 and κ2. However, there is only one gene product and the subtypes are considered putative.

Selective κ agonists are of several structural types. All have high affinity for the κ receptor and are full agonists.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]diprenorphine Hs Antagonist 9.1 pKd 81
nor-binaltorphimine Rn Antagonist 9.6 – 10.7 pKi 12,45,52
nor-binaltorphimine Hs Antagonist 8.9 – 11.0 pKi 64,68,81,91,102-103
GNTI Hs Antagonist 9.74 – 9.9 pKi 32,64,86
β-FNA Hs Antagonist 9.7 pKi 91
(-)-quadazocine Hs Antagonist 9.7 pKi 91
buprenorphine Hs Antagonist 9.1 – 10.2 pKi 91,103
diprenorphine Hs Antagonist 9.6 – 9.7 pKi 64,91,102-103
nalmefene Hs Antagonist 9.5 pKi 91
naltrexone Hs Antagonist 8.4 – 9.4 pKi 64,81,91
BNTX Hs Antagonist 8.4 pKi 91
naltriben Hs Antagonist 8.4 pKi 91
naloxone Hs Antagonist 7.6 – 8.6 pKi 64,81,91,102-103
naloxone Rn Antagonist 8.0 pKi 45,52
naltrindole Hs Antagonist 8.0 pKi 91
naltrindole Rn Antagonist 7.9 pKi 45
naloxone Rn Antagonist 7.7 pKi 12
(+)-naloxone Rn Antagonist 4.7 pKi 52
naltrexone Mm Antagonist 9.2 pIC50 98
nor-binaltorphimine Mm Antagonist 8.9 pIC50 98
naloxone Mm Antagonist 8.3 pIC50 98
naltrindole Mm Antagonist 7.4 pIC50 98
View species-specific antagonist tables
Allosteric Regulator Comments
Although no small molecules are considered direct allosteric regulators of κ opioid receptors, a number of proteins such as G protein-coupled receptor kinases, β-arrestins and G proteins clearly regulate receptor affinities and function. Furthermore, sodium and guanine nucleotides can modify the functional κ receptor complex and G protein interaction. Also, other G protein-coupled receptors appear to be able to form heterodimers with κ receptors, potentially modifying κ opioid receptor activity.

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Potassium channel
Calcium channel
References:  4,23,25,36,42,54,77,87
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
G12/G13 family 		Adenylate cyclase inhibition
Phospholipase C stimulation
Other - See Comments
Comments:  Activation of κ opioid receptors stimulates p42/p44 MAP kinase via βγ subunits of Gi/o proteins [8].
κ opioid receptors interact with NHERF-1/EBP50 to stimulate Na+/H+ exchange independent of Gi/o proteins [30].
References:  8,30,41,44,56,93
Tissue Distribution
CNS: olfactory bulb, nucleus accumbens, caudate nucleus, putamen, temporal cortex, parietal cortex, thalamic nuclei > amygdala, occipital cortex, frontal cortex, hypothalamus, ventral tegmental area, cerebellar cortex > hippocampus, corpus mamillare, locus coeruleus, pituitary, spinal cord > globus pallidus, substantia nigra, superior colliculus, inferior colliculus, olivary nucleus.
Species:  Human
Technique:  RT-PCR.
References:  81
Skin.
Species:  Human
Technique:  RT-PCR and Immunohistochemistry.
References:  75
Immune cells.
Species:  Human
Technique:  RT-PCR.
References:  19
CNS: amygdala, caudate nucleus, hypothalamus, subthalamic nucleus > hippocampus, thalamus > substantia nigra, corpus callosum.
Species:  Human
Technique:  Northern blotting.
References:  102
Intestine.
Species:  Mouse
Technique:  RT-PCR.
References:  67
CNS: claustrum, nucleus accumbens, endopiriform nucleus, ventral pallidum, preoptic area, fundus striati, hypothalamus, substantia nigra.
Species:  Mouse
Technique:  Radioligand binding.
References:  35
Pregnant uterus.
Species:  Mouse
Technique:  in situ hybridisation.
References:  105
CNS: olfactory tubercle, endopiriform nucleus, ventral pallidum, hypothalamus, deep cortical layers, claustrum.
Species:  Mouse
Technique:  Radioligand binding.
References:  35
CNS: nucleus accumbens, pyramidal and molecular layers of the hippocampus, granular cell layer of the dentate gyrus, midline nuclei of the thalamus, hindbrain regions > striatum.
Species:  Rat
Technique:  Radioligand binding.
References:  89
Ear: cochlea.
Species:  Rat
Technique:  RT-PCR and immunocytochemistry.
References:  33
CNS: amygdala, olfactory tubercle, nucleus accumbens, caudate putamen, medial preoptic area, hypothalamus, median eminence, periventricular thalamus, interpeduncular nucleus.
Species:  Rat
Technique:  Radioligand binding.
References:  49
CNS: hippocampus, dentate gyrus, hypothalamic and thalamic nuclei, cortex, caudate putamen, olfactory tubercle, nucleus accumbens
Species:  Rat
Technique:  in situ hybridisation.
References:  20
κ1: CNS: claustrum, endopiriform nucleus, caudate putamen, nucleus accumbens, midline nuclear group of the thalamus, superficial grey layer of the superior colliculus, central grey.
κ2: CNS: caudate putamen, nucleus accumbens, amygdala, thalamus, interpeduncular nuclei.
Species:  Rat
Technique:  Radioligand binding.
References:  94
CNS: ventral forebrain, hypothalamus, thalamus, posterior pituitary, and midbrain. Primarily postsynaptic membranes.
Species:  Rat
Technique:  Immunohistochemistry.
References:  3
CNS: κ receptors only represent a small percentage of opioid receptors in the superficial layers (I and II) of the dorsal horn of the spinal cord.
Species:  Rat
Technique:  Radioligand binding.
References:  7
CNS: telencephalon, diencephalon > mesencephalon, metencephalon.
Species:  Rat
Technique:  Radioligand binding.
References:  61
Tissue Distribution Comments
κ opioid receptors show a fairly widespread distribution although quantitatively they represent only a small percentage of the total opioid receptors in the brain. This contrasts with the guinea-pig brain, where κ opioid receptor expression is far more abundant. In all species, the early receptor autoradiography was carried out with low selectivity ligands such as [3H]ethylketocycazocine and [3H]bremazocine and their cross labelling of μ and δ receptors was supressed by the use of excess cold ligands to displace their binding to μ and δ opioid sites. Since the late 1980s highly selective κ opioid receptor ligands such as [3H]U69,593 and [3H]CI-977 have been used and the distribution is more restrictive when these ligands are employed.
For a review of κ opioid receptor expression in the rat see [48].
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of musculature contraction of sections of mouse vas deferens following stimulation of the intramural nerves.
Species:  Mouse
Tissue:  Vas deferens.
Response measured:  Inhibition of electrically-evoked contractions.
References:  13
Measurement of K+ conductance, using a 2 electrode voltage clamp, in Xenopus oocytes transfected with the rat κ receptor and Kir3 channel.
Species:  Rat
Tissue:  Xenopus oocytes.
Response measured:  Increase in K+ conductance.
References:  25
Measurement of Ca2+ conductance, using a whole cell voltage clamp, in PC-12 cells transfected with the mouse κ receptor.
Species:  Mouse
Tissue:  PC-12 cells.
Response measured:  Increase in K+ conductance and decrease in Ca2+ conductance.
References:  87
Measurement of cAMP levels in R1.1 murine thymoma cells endogenously expressing the κ receptor.
Species:  Mouse
Tissue:  R1.1 murine thymoma cells.
Response measured:  Inhibition of cAMP accumulation.
References:  42
Measurement of cAMP levels in CHO cells transfected with the rat κ receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP accumulation.
References:  5
Measurement of cAMP levels in PC-12 cells transfected with the mouse κ receptor.
Species:  Mouse
Tissue:  PC-12 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  87
Measurement of cAMP levels in COS-7 cells transfected with the rat κ receptor.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  12
Measurement of cAMP levels in CHO cells transfected with the human κ receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Inhibition of cAMP accumulation.
References:  104
Measurement of [35S]GTPγS binding in CHO cells transfected with the human κ receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  [35S]GTPγS binding.
References:  103
Physiological Functions
Sedative and sensorimotor effects in rats.
Species:  Rat
Tissue:  In vivo.
References:  92,95
Water diuresis, potentially by modulation of vasopressin.
Species:  Human
Tissue:  In vivo.
References:  62,66,71
Water diuresis, potentially by modulation of vasopressin.
Species:  Rat
Tissue:  In vivo.
References:  43,83,95
Water diuresis, potentially by modulation of vasopressin.
Species:  Mouse
Tissue:  In vivo.
References:  95
Neuroendocrine effects: stimulation of prolactin release, probably by modulation of the tuberoinfundibular dopamine system.
Species:  Human
Tissue:  In vivo.
References:  38,65
Neuroendocrine effects: stimulation of prolactin release, probably by modulation of the tuberoinfundibular dopamine system.
Species:  Rat
Tissue:  In vivo.
References:  17,39
Sedative and sensorimotor effects in mice.
Species:  Mouse
Tissue:  In vivo.
References:  92,95
Sedative and interoceptive effects in humans (such as psychotomimetic, dysphoric and potentially hallucinogenic).
Species:  Human
Tissue:  In vivo.
References:  72
Modulation of dopaminergic function.
Species:  Human
Tissue:  In vivo.
References:  100
Modulation of dopaminergic function. This may be related to the κ agonist effects on hedonic states (such as causing place aversion in rodents), as well as the blockade of the reinforcing, locomotor stimulant and neurobiological effects of psychostimulants such as cocaine.
Species:  Rat
Tissue:  In vivo.
References:  16,21,47,80,84
Modulation of dopaminergic function. This may be related to the κ agonist effects on hedonic states (such as causing place aversion in rodents), as well as the blockade of the reinforcing, locomotor stimulant and neurobiological effects of psychostimulants such as cocaine.
Species:  Mouse
Tissue:  In vivo.
References:  101
Immune changes have been observed in immune cells in peripheral tissues.
Species:  Mouse
Tissue:  lymphoid cells.
References:  79,88
Immune changes have been observed in immune cells in central tissues.
Species:  Human
Tissue:  Microglial cells.
References:  10,51
Enhancement of food intake.
Species:  Rat
Tissue:  In vivo.
References:  55
Blockade of pruritus.
Species:  Mouse
Tissue:  In vivo.
References:  90
Blockade of pruritus.
Species:  Rat
Tissue:  In vivo.
References:  22
Body temperature regulation:
κ receptor activation induces hypothermia, blocked by selective κ receptor antagonists. The effect is centrally mediated, involving both oxidative metabolism and heat exchange.
Species:  Rat
Tissue:  In vivo.
References:  1,24
Antinociception: systemic administration.
Species:  Rat
Tissue:  In vivo.
References:  76,95
Antinociception: systemic administration.
Species:  Mouse
Tissue:  In vivo.
References:  57,95
Antinociception: systemic administration.
Species:  Human
Tissue:  In vivo.
References:  63
Peripheral antinociception.
Species:  Rat
Tissue:  In vivo.
References:  2,85
Attenuation of contractions induced by intestinal distension in the gastrointestinal tract.
Species:  Rat
Tissue:  In vivo.
References:  78
Stimulation of relief from abdominal pain and bloating.
Species:  Human
Tissue:  In vivo.
References:  14
Physiological Consequences of Altering Gene Expression
κ opiod receptor knockout mice exhibit enhanced sensitivity to chemical visceral pain, abolished hypolocomotor, analgesic and aversive actions of the prototypic κ receptor agonist U50488H and attenuation of morphine withdrawl.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  82
κ receptor knockout mice exhibit increased in humoral responses to antigen challenge.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  18
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Oprk1tm1Jep Oprk1tm1Jep/Oprk1tm1Jep
involves: C57BL/6		 MGI:97439  MP:0001462 abnormal avoidance learning behavior PMID: 19864633 
Oprk1tm1Kff Oprk1tm1Kff/Oprk1tm1Kff
involves: 129S2/SvPas * C57BL/6		 MGI:97439  MP:0001392 abnormal locomotor activity PMID: 9463367 
Oprk1tm1Kff Oprk1tm1Kff/Oprk1tm1Kff
involves: 129S2/SvPas * C57BL/6		 MGI:97439  MP:0001970 abnormal pain threshold PMID: 9463367 
Oprk1tm1Jep Oprk1tm1Jep/Oprk1tm1Jep
involves: 129S/SvEv * 129S6/SvEvTac * C57BL/6		 MGI:97439  MP:0001982 decreased chemically-elicited antinociception PMID: 16672569 
Oprk1tm1Kff Oprk1tm1Kff/Oprk1tm1Kff
involves: 129S2/SvPas * C57BL/6		 MGI:97439  MP:0000623 decreased salivation PMID: 9463367 
Oprk1tm1Jep Oprk1tm1Jep/Oprk1tm1Jep
Not Specified		 MGI:97439  MP:0009778 impaired behavioral response to anesthetic PMID: 11032994 
Oprk1tm1Kff Oprk1tm1Kff/Oprk1tm1Kff
involves: 129S2/SvPas * C57BL/6		 MGI:97439  MP:0009757 impaired behavioral response to morphine PMID: 9463367 
Oprk1tm1Kff Oprk1tm1Kff/Oprk1tm1Kff
involves: 129S2/SvPas * C57BL/6		 MGI:97439  MP:0001934 increased litter size PMID: 9463367 
Oprk1+|Oprk1tm1Kff Oprk1tm1Kff/Oprk1+
involves: 129S2/SvPas * C57BL/6		 MGI:97439  MP:0001934 increased litter size PMID: 9463367 
Biologically Significant Variant Comments
κ1 and κ2 receptor subtypes have been proposed based on in vivo pharmacology showing lack of cross-tolerance between U69,593 and bremazocine and differential antagonism by quadazocine and (-)UPHIT [27-29]. Receptor binding studies have led to suggestions of κ1, κ2 and κ3 subtypes [15,74]. However, only one κ receptor cDNA clone has been reported and no κ receptor variants have been characterised. Interaction between κ and δ receptors in transfected cells has been reported and suggested to result in κ2 subtype pharmacology [34]. Multiple active conformations of the κ receptor are likely to exist. κ receptor subtypes are likely due to interaction of receptor with other proteins or receptors at the level of neuronal circuitry, but not mRNA variants.

REFERENCES

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1. Adler, M. W. and Geller, E. B. (1987) Hypothermia and poikilothermia induced by a kappa-agonist opioid and a neuroleptic. Eur J Pharmacol, 140: 233-237. [PMID:2889606]

2. Andreev, N., Urban, L. and Dray, A. (1994) Opioids suppress spontaneous activity of polymodal nociceptors in rat paw skin induced by ultraviolet irradiation. Neuroscience, 58: 793-798. [PMID:8190256]

3. Arvidsson, U., Riedl, M., Chakrabarti, S., Vulchanova, L., Lee, J. H., Nakano, A. H., Lin, X., Loh, H. H., Law, P. Y. and Wessendorf, M. W. (1995) The kappa-opioid receptor is primarily postsynaptic: combined immunohistochemical localization of the receptor and endogenous opioids. Proc Natl Acad Sci U S A, 92: 5062-5066. [PMID:7539141]

4. Attali, B. and Vogel, Z. (1986) Inhibition of adenylate cyclase and induction of heterologous desensitization by kappa agonists in rat spinal cord. NIDA Res Monogr, 75: 141-144. [PMID:2828959]

5. Avidor-Reiss, T., Zippel, R., Levy, R., Saya, D., Ezra, V., Barg, J., Matus-Leibovitch, N. and Vogel, Z. (1995) kappa-Opioid receptor-transfected cell lines: modulation of adenylyl cyclase activity following acute and chronic opioid treatments. FEBS Lett, 361: 70-74. [PMID:7890042]

6. Belkowski, S. M., Zhu, J., Liu-Chen, L. Y., Eisenstein, T. K., Adler, M. W. and Rogers, T. J. (1995) Sequence of kappa-opioid receptor cDNA in the R1.1 thymoma cell line. J Neuroimmunol, 62: 113-117. [PMID:7499487]

7. Besse, D., Lombard, M. C. and Besson, J. M. (1991) Autoradiographic distribution of mu, delta and kappa opioid binding sites in the superficial dorsal horn, over the rostrocaudal axis of the rat spinal cord. Brain Res, 548: 287-291. [PMID:1651143]

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To cite this database page, please use the following:

Anna Borsodi, Girolamo Caló, Charles Chavkin, MacDonald J. Christie, Olivier Civelli, Brian M. Cox, Lakshmi A. Devi, Christopher Evans, Graeme Henderson, Volker Höllt, Brigitte Kieffer, Ian Kitchen, Mary-Jeanne Kreek, Lee-Yuan Liu-Chen, Jean-Claude Meunier, Philip S. Portoghese, Toni S. Shippenberg, Eric J. Simon, Lawrence Toll, John R. Traynor, Hiroshi Ueda, Yung H. Wong.
Opioid receptors: κ receptor. Last modified on 15/02/2013. Accessed on 19/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=318.


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