DGIdb - OPRK1 Gene Record

OPRK1 4986 Druggable Genome

Alternate Names:

4986
OPIOID RECEPTOR KAPPA 1
OPRK1
K-OR-1
KOR
KOR-1
OPRK
165196
8154
ENSG00000082556
OTTHUMG00000164276
P41145
KAPPA-TYPE OPIOID RECEPTOR
OPRK_HUMAN
OPIOID RECEPTOR KAPPA
KAPPA-TYPE OPIOID RECEPTOR (KOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P41145]
PA31943
T60693
KOP
KOR1

Gene Info:

Uniprot Evidence	1: Evidence at protein level
Interpro Type	Family
Interpro Short Name	7TM_GPCR_Rhodpsn
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR000276
Uniprot Status	Swiss-Prot
Interpro Name	GPCR, rhodopsin-like, 7TM
Transmembrane Helix Count	7
Target Main Class	Receptors
Target Subclass	Rhodopsin
Target Subclass	GPCR
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(8 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Kreek MJ et al., 1999, Dynorphin A1-13 causes elevation of serum levels of prolactin through an opioid receptor mechanism in humans: gender differences and implications for modulation of dopaminergic tone in the treatment of addictions., J Pharmacol Exp Ther
Béguin C et al., 2012, Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues., Bioorg Med Chem Lett
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Ikeda T et al., 1997, The effect of opioids on thermoregulatory responses in humans and the special antishivering action of meperidine., Ann N Y Acad Sci
Cruz Pardos P et al., 2000, [Usefulness of meperidine in anesthesiology]., Rev Esp Anestesiol Reanim
Yasaei R et al., 2020, Meperidine,
Kurz M et al., 1993, Naloxone, meperidine, and shivering., Anesthesiology
Gharagozlou et al., 2006, Pharmacological profiles of opioid ligands at kappa opioid receptors., BMC Pharmacol.
Chien et al., 1995, (-)-Pentazocine analgesia in mice: interactions with a sigma receptor system., Eur. J. Pharmacol.
Mignat et al., 1995, Affinity profiles of morphine, codeine, dihydrocodeine and their glucuronides at opioid receptor subtypes., Life Sci.
Takahama et al., 2007, Central and peripheral mechanisms of narcotic antitussives: codeine-sensitive and -resistant coughs., Cough
Schmidt H et al., 2002, Affinities of dihydrocodeine and its metabolites to opioid receptors., Pharmacol Toxicol
Chen et al., 2005, Dextromethorphan differentially affects opioid antinociception in rats., Br. J. Pharmacol.
Hoehe et al., 1993, Opiates increase plasma catecholamines in humans., Psychoneuroendocrinology
Tao et al., 2006, Nalbuphine is effective in decreasing the rewarding effect induced by morphine in rats., Drug Alcohol Depend
Gear et al., 1999, The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain., Pain
Peng et al., 2007, Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors., J. Med. Chem.
Smith et al., 2009, The effects of repeated opioid administration on locomotor activity: I. Opposing actions of mu and kappa receptors., J. Pharmacol. Exp. Ther.
Mello et al., 2005, Effects of the mixed mu/kappa opioid nalbuphine on cocaine-induced changes in subjective and cardiovascular responses in men., Neuropsychopharmacology
Sun et al., 2003, Tramadol reduces the 5-HTP-induced head-twitch response in mice via the activation of mu and kappa opioid receptors., Life Sci.
Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
Zhang S et al., 2009, A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors., Bioorg Med Chem Lett
Teodorov et al., 2006, Preliminary study of the effects of morphine treatment on opioid receptor gene expression in brain structures of the female rat., Neuroscience
Leventhal et al., 1998, Morphine-6beta-glucuronide-induced hyperphagia: characterization of opioid action by selective antagonists and antisense mapping in rats., J. Pharmacol. Exp. Ther.
Kozak et al., 1994, Murine chromosomal location of the mu and kappa opioid receptor genes., Genomics
Chatti I et al., 2017, Genetic Analysis of Mu and Kappa Opioid Receptor and COMT Enzyme in Cancer Pain Tunisian Patients Under Opioid Treatment., Iran J Public Health
Zhu et al., 1996, The region in the mu opioid receptor conferring selectivity for sufentanil over the delta receptor is different from that over the kappa receptor., FEBS Lett.
Chang et al., 1989, Sufentanil, morphine, met-enkephalin, and kappa-agonist (U-50,488H) inhibit substance P release from primary sensory neurons: a model for presynaptic spinal opioid actions., Anesthesiology
Barry et al., 2005, Opioids: old drugs for potential new applications., Curr. Pharm. Des.
Mayberg et al., 1991, Quantification of mu and non-mu opiate receptors in temporal lobe epilepsy using positron emission tomography., Ann. Neurol.
Oosten AW et al., 2016, Opioid treatment failure in cancer patients: the role of clinical and genetic factors., Pharmacogenomics
Nielsen et al., 2007, Oxycodone and morphine have distinctly different pharmacological profiles: radioligand binding and behavioural studies in two rat models of neuropathic pain., Pain
Ordóñez Gallego et al., 2007, Oxycodone: a pharmacological and clinical review., Clin Transl Oncol
Riley et al., 2008, Oxycodone: a review of its use in the management of pain., Curr Med Res Opin
Fan et al., 2002, Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain., Brain Res. Bull.
Vivian et al., 1999, kappa-Opioid receptor effects of butorphanol in rhesus monkeys., J. Pharmacol. Exp. Ther.
Fan et al., 2002, Butorphanol dependence and withdrawal decrease hippocampal kappa 2-opioid receptor binding., Brain Res.
Picker et al., 1996, Discriminative stimulus effects of butorphanol: influence of training dose on the substitution patterns produced by Mu, Kappa and Delta opioid agonists., J. Pharmacol. Exp. Ther.
Walsh et al., 2008, Evaluation of the mu and kappa opioid actions of butorphanol in humans through differential naltrexone blockade., Psychopharmacology (Berl.)
Ohta et al., 1989, [Kappa-type opioid receptor in human placental membrane]., Masui
Narita et al., 1994, Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain., Eur. J. Pharmacol.
Commiskey et al., 2005, Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors., J. Pharmacol. Sci.
Wakabayashi et al., 1995, Simultaneous measurement of biogenic amines and their metabolites in rat brain regions after acute administration of and abrupt withdrawal from butorphanol or morphine., Neurochem. Res.
Park et al., 2000, kappa-opioid agonist stimulated regional distribution of [(35)S]GTPgammas binding in butorphanol continuously infused rat., Brain Res. Bull.
Bruchas MR et al., 2007, Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase., J Biol Chem
Zhang Q et al., 2020, κ Opioid Receptor 1 Single Nucleotide Polymorphisms were Associated with the Methadone Dosage., Genet Test Mol Biomarkers
Boothby et al., 2007, Buprenorphine for the treatment of opioid dependence., Am J Health Syst Pharm
Robinson, 2006, Buprenorphine-containing treatments: place in the management of opioid addiction., CNS Drugs
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Wee et al., 2009, Inhibition of kappa opioid receptors attenuated increased cocaine intake in rats with extended access to cocaine., Psychopharmacology (Berl.)
Herz, 1997, Endogenous opioid systems and alcohol addiction., Psychopharmacology (Berl.)
Barrios de Tomasi et al., [Opioid antagonists and alcohol consumption]., Rev Neurol
Helm et al., Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification., Pain Physician
van Dorp et al., 2007, Naloxone treatment in opioid addiction: the risks and benefits., Expert Opin Drug Saf
Peng et al., 2007, Kappa receptor bivalent ligands., Curr Top Med Chem
Neil, 1984, Affinities of some common opioid analgesics towards four binding sites in mouse brain., Naunyn Schmiedebergs Arch. Pharmacol.
Cai J et al., 2014, Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity., Bioorg Med Chem
Klein et al., 2008, Acute and chronic heroin dependence in mice: contribution of opioid and excitatory amino acid receptors., Eur. J. Pharmacol.
Wee et al., 2010, The role of the dynorphin-kappa opioid system in the reinforcing effects of drugs of abuse., Psychopharmacology (Berl.)
Gerra G et al., 2007, Human kappa opioid receptor gene (OPRK1) polymorphism is associated with opiate addiction., Am J Med Genet B Neuropsychiatr Genet

DEZOCINE OPRK1

Interaction Score: 3.64

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor antagonist

Direct Interaction yes

Trial Name -

PMIDs:
16433932 17016423 17139284 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
NALBUPHINE OPRK1

Interaction Score: 2.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name REN-213

Novel drug target Established target

Trial Name nalbuphine hydrochloride, PW-4142

PMIDs:
22204910 15655510 8388112 16517095 10534607 17407276 19403853 15602503 17016423 17139284

Sources:
DTC TdgClinicalTrial TEND TTD
U-69593 OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24613457

Sources:
DTC
CHEMBL1941031 OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22204910

Sources:
DTC
12-EPI-SALVINORIN A OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22204910

Sources:
DTC
DIFELIKEFALIN OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name CR845

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
ASIMADOLINE OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name asimadoline

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
MEPERIDINE OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 9100971 10846914 29261967 8267194

Sources:
TdgClinicalTrial TEND
SALVINORIN A OPRK1

Interaction Score: 1.82

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22204910

Sources:
DTC
BUTORPHANOL OPRK1

Interaction Score: 1.56

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
12127012 10381785 12470863 8968334 17909753 2555580 7705457 15942128 8746803 10779697

Sources:
TdgClinicalTrial TEND
CARFENTANIL OPRK1

Interaction Score: 1.36

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
15853689 1656846

Sources:
TTD
APADOLINE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL433508 OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL255067 OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
NIRAVOLINE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
NALFURAFINE HYDROCHLORIDE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROPOXYPHENE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 6151117

Sources:
TdgClinicalTrial TEND
NALTREXONE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist

Direct Interaction yes

Trial Name ALO-01, morphine sulfate and naltrexone hydrochloride,Embeda, Kadian NT

PMIDs:
19484223 9040115 17661275 18354714 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND
NORBINALTORPHIMINE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17702750

Sources:
DTC
ATICAPRANT OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
ENADOLINE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
CHEMBL570176 OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19892550

Sources:
DTC
PENTAZOCINE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8788445

Sources:
TdgClinicalTrial TEND
HYDROMORPHONE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name NMED-1077,Exalgo, Jurnista, Dilaudid

PMIDs:
16433932 17016423 17139284

Sources:
TdgClinicalTrial TEND
NALMEFENE OPRK1

Interaction Score: 0.91

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name nalmefene, CPH-101

Novel drug target Established target

PMIDs:
9862779

Sources:
DTC TdgClinicalTrial
CODEINE OPRK1

Interaction Score: 0.8

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7885194 17620111 17016423 17139284 12420793

Sources:
TdgClinicalTrial TEND
OXYCODONE OPRK1

Interaction Score: 0.71

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name transdermal oxycodone

Trial Name PTI-801,Oxytrex

Trial Name oxycodone, PTI-821,Remoxy

PMIDs:
27472837 17467904 17525040 18039433

Sources:
TdgClinicalTrial TEND PharmGKB
NALTREXONE HYDROCHLORIDE OPRK1

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
NALOXONE HYDROCHLORIDE OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
BUTORPHANOL TARTRATE OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor partial agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ANILERIDINE PHOSPHATE OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL300662 OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BUPRENORPHINE OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

Trial Name ALKS 5461

PMIDs:
17244875 16953647

Sources:
TdgClinicalTrial ChemblInteractions TEND
ANILERIDINE HYDROCHLORIDE OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Kappa opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
LEVALLORPHAN TARTRATE OPRK1

Interaction Score: 0.45

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor partial agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SUFENTANIL OPRK1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name sufentanil transdermal patch,Transdur-sufentanil

Novel drug target Established target

Trial Name sufentanil,Chronogesic

PMIDs:
8612823 2467589

Sources:
TdgClinicalTrial
NALOXONE OPRK1

Interaction Score: 0.33

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name buprenorphine + naloxone capsule,NanoBUP

Novel drug target Established target

Trial Name buprenorphine + naloxone,Suboxone

PMIDs:
17367258 18354714 17305578

Sources:
TdgClinicalTrial
NALBUPHINE HYDROCHLORIDE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CODEINE SULFATE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HYDROCODONE BITARTRATE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYMORPHONE HYDROCHLORIDE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BENZHYDROCODONE HYDROCHLORIDE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name KP201 (prodrug of hydrocodone)

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ODELEPRAN OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NALMEFENE HYDROCHLORIDE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUPRENORPHINE HYDROCHLORIDE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AXOMADOL OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HYDROCODONE POLISTIREX OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

PMIDs:
None found

Sources:
ChemblInteractions
U-50488 METHANE SULFONATE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CODEINE PHOSPHATE OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

PMIDs:
None found

Sources:
ChemblInteractions
CODEINE POLISTIREX OPRK1

Interaction Score: 0.3

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

PMIDs:
None found

Sources:
ChemblInteractions
DIACETYLMORPHINE OPRK1

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
18343363 20352414 17373729

Sources:
PharmGKB
MORPHINE OPRK1

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name TPM-1/Morphine

Trial Name Statex

Trial Name MoxDuo

PMIDs:
16753266 9808678 17016423 17139284 7959748 29259946

Sources:
TdgClinicalTrial TEND PharmGKB
CEBRANOPADOL OPRK1

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRAMADOL OPRK1

Interaction Score: 0.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name PTI-601

Novel drug target Established target

Trial Name tramadol extended-release,Raliva ER

PMIDs:
12570923 31004280

Sources:
TdgClinicalTrial TEND
CHLOROXINE OPRK1

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC TTD
CHEMBL2094567 OPRK1

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
HYDROCODONE OPRK1

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TEND
CHEMBL1492017 OPRK1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1390716 OPRK1

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL546170 OPRK1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL586135 OPRK1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL428064 OPRK1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
COCAINE OPRK1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
CHEMBL528694 OPRK1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
METHADONE OPRK1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31940240

Sources:
PharmGKB
CLIOQUINOL OPRK1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SIROLIMUS OPRK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ALCOHOL OPRK1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

Ensembl: ENSG00000082556
- Version: 101_38
Alternate Names:

OPRK1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P41145
- Version: 11-September-2012
Alternate Names:

ENSG00000082556 Ensembl Gene Id

OPRK1 Uniprot Gene Name

P41145 Uniprot Accession

Gene Info:

Uniprot Evidence 1: Evidence at protein level

Interpro Type Family

Interpro Short Name 7TM_GPCR_Rhodpsn

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P41145
- Version: 01-August-2011
Alternate Names:

P41145 Uniprot Accession

OPRK_HUMAN Uniprot Id

ENSG00000082556 Ensembl Gene Id

Gene Info:

Transmembrane Helix Count 7

Target Main Class Receptors

Target Subclass Rhodopsin

Publications:
RussLampel: ENSG00000082556
- Version: 26-July-2011
Alternate Names:

KAPPA-TYPE OPIOID RECEPTOR (KOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P41145] Description

OPRK1 Display Id

ENSG00000082556 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P41145
- Version: January-2014
Alternate Names:

OPRK1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:

PharmGKB: OPRK1

Version: 18-August-2020

Alternate Names:

PA31943 PharmGKB ID

Gene Info:

Publications:

Oosten AW et al., 2016, Opioid treatment failure in cancer patients: the role of clinical and genetic factors., Pharmacogenomics

Zhang Q et al., 2020, κ Opioid Receptor 1 Single Nucleotide Polymorphisms were Associated with the Methadone Dosage., Genet Test Mol Biomarkers

Chatti I et al., 2017, Genetic Analysis of Mu and Kappa Opioid Receptor and COMT Enzyme in Cancer Pain Tunisian Patients Under Opioid Treatment., Iran J Public Health

TTD: Opioid receptor kappa

Version: 2020.06.01

Alternate Names:

OPRK1 TTD Gene Abbreviation

T60693 TTD Target ID

Gene Info:

Publications:

Aldrich JV et al., 2009, Peptide kappa opioid receptor ligands: potential for drug development., AAPS J

Al-Hasani R et al., 2011, Molecular mechanisms of opioid receptor-dependent signaling and behavior., Anesthesiology

DTC: OPRK1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Béguin C et al., 2012, Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues., Bioorg Med Chem Lett

Zhang S et al., 2009, A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors., Bioorg Med Chem Lett

Cai J et al., 2014, Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity., Bioorg Med Chem

HingoraniCasas: ENSG00000082556
- Version: 31-May-2017
Alternate Names:

ENSG00000082556 Gene Symbol

OPRK1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: OPRK
- Version: chembl_23
Alternate Names:

OPRK GENE_SYMBOL

OPRK1 GENE_SYMBOL

Kappa-type opioid receptor UNIPROT

Gene Info:

Publications:
GO: OPRK1
- Version: 01-February-2022
Alternate Names:

OPRK GO Gene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
dGene: OPRK1
- Version: 27-Jun-2013
Alternate Names:

4986 Gene ID

KOR dGene Synonym

OPRK dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Mechanism of Interaction	Kappa opioid receptor antagonist
Direct Interaction	yes
Trial Name	-

Trial Name	REN-213
Novel drug target	Established target
Trial Name	nalbuphine hydrochloride, PW-4142

Mechanism of Interaction	Kappa opioid receptor agonist
Direct Interaction	yes

Mechanism of Interaction	Opioid receptors; mu/kappa/delta antagonist
Direct Interaction	yes
Trial Name	ALO-01, morphine sulfate and naltrexone hydrochloride,Embeda, Kadian NT

Trial Name	nalmefene, CPH-101
Novel drug target	Established target

Trial Name	transdermal oxycodone
Trial Name	PTI-801,Oxytrex
Trial Name	oxycodone, PTI-821,Remoxy

Mechanism of Interaction	Kappa opioid receptor partial agonist
Direct Interaction	yes

Trial Name	sufentanil transdermal patch,Transdur-sufentanil
Novel drug target	Established target
Trial Name	sufentanil,Chronogesic

Trial Name	buprenorphine + naloxone capsule,NanoBUP
Novel drug target	Established target
Trial Name	buprenorphine + naloxone,Suboxone

Mechanism of Interaction	Opioid receptors; mu/kappa/delta agonist
Direct Interaction	yes

Trial Name	KP201 (prodrug of hydrocodone)
Novel drug target	Established target

Trial Name	PTI-601
Novel drug target	Established target
Trial Name	tramadol extended-release,Raliva ER

ENSG00000082556	Ensembl Gene Id
OPRK1	Uniprot Gene Name
P41145	Uniprot Accession

KAPPA-TYPE OPIOID RECEPTOR (KOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P41145]	Description
OPRK1	Display Id
ENSG00000082556	Ensembl Gene Id

OPRK	GENE_SYMBOL
OPRK1	GENE_SYMBOL
Kappa-type opioid receptor	UNIPROT

OPRK1 Gene Record

OPRK1 4986 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Kappa opioid receptor antagonist Direct Interaction yes Trial Name -

PMIDs: 16433932 17016423 17139284 11752352

Sources: TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name REN-213 Novel drug target Established target Trial Name nalbuphine hydrochloride, PW-4142

PMIDs: 22204910 15655510 8388112 16517095 10534607 17407276 19403853 15602503 17016423 17139284

Sources: DTC TdgClinicalTrial TEND TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24613457

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22204910

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22204910

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name CR845 Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name asimadoline

PMIDs: None found

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 9100971 10846914 29261967 8267194

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22204910

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 12127012 10381785 12470863 8968334 17909753 2555580 7705457 15942128 8746803 10779697

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 15853689 1656846

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Kappa opioid receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752352 6151117

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist Direct Interaction yes Trial Name ALO-01, morphine sulfate and naltrexone hydrochloride,Embeda, Kadian NT

PMIDs: 19484223 9040115 17661275 18354714 11752352

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor antagonist

Direct Interaction yes

Trial Name -

PMIDs:
16433932 17016423 17139284 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name REN-213

Novel drug target Established target

Trial Name nalbuphine hydrochloride, PW-4142

PMIDs:
22204910 15655510 8388112 16517095 10534607 17407276 19403853 15602503 17016423 17139284

Sources:
DTC TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
24613457

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22204910

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22204910

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name CR845

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name asimadoline

PMIDs:
None found

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 9100971 10846914 29261967 8267194

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
22204910

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
12127012 10381785 12470863 8968334 17909753 2555580 7705457 15942128 8746803 10779697

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

PMIDs:
15853689 1656846

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Kappa opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 6151117

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Opioid receptors; mu/kappa/delta antagonist

Direct Interaction yes

Trial Name ALO-01, morphine sulfate and naltrexone hydrochloride,Embeda, Kadian NT

PMIDs:
19484223 9040115 17661275 18354714 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
17702750

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
19892550

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8788445

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)