DGIdb - OPRM1 Gene Record

OPRM1 4988 Druggable Genome

Alternate Names:

4988
OPIOID RECEPTOR MU 1
OPRM1
LMOR
M-OR-1
MOP
MOR
MOR1
OPRM
600018
8156
ENSG00000112038
OTTHUMG00000015870
P35372
OPRM_HUMAN
MU-TYPE OPIOID RECEPTOR
Mu opiate receptor
Mu opioid receptor
hMOP
MOR-1
319
NP_000905
NM_000914
μ receptor
MU-TYPE OPIOID RECEPTOR (MOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35372]
BE0000770
PA31945

Gene Info:

Target Subclass	GPCR
Target Main Class	Receptors
Transmembrane Helix Count	7
Target Subclass	Rhodopsin
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Interpro Short Name	7TM_GPCR_Rhodpsn
Interpro Name	GPCR, rhodopsin-like, 7TM
Interpro Type	Family
Interpro Acc	IPR000276
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	DRUGGABLE GENOME
Target Class	Receptors
GuideToPharmacology Gene Category Name	Opioid receptors
GuideToPharmacology Gene Category ID	50
Gene Biotype	PROTEIN_CODING

(10 More Sources)

Gene Categories: Category Details

KINASE
G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Ulens et al., 1999, Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents., Cardiovasc. Res.
Tyers, 1980, A classification of opiate receptors that mediate antinociception in animals., Br. J. Pharmacol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Walker et al., 1999, Naltrexone and beta-funaltrexamine antagonism of the antinociceptive and response rate-decreasing effects of morphine, dezocine, and d-propoxyphene., Psychopharmacology (Berl.)
Bannwarth et al., 2009, The dextropropoxyphene controversy., Joint Bone Spine
Picker, 1997, Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists., J. Pharmacol. Exp. Ther.
Codd et al., 1995, Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception., J. Pharmacol. Exp. Ther.
Melone et al., 2000, Etorphine increases the number of mu-opioid receptor-positive cells in the cerebral cortex., Neuroscience
Stafford et al., mu-Opioid receptor downregulation contributes to opioid tolerance in vivo., Pharmacol. Biochem. Behav.
Patel et al., 2002, Opioid agonists differentially regulate mu-opioid receptors and trafficking proteins in vivo., Mol. Pharmacol.
Duttaroy et al., 2000, In vivo regulation of mu-opioid receptor density and gene expression in CXBK and outbred Swiss Webster mice., Synapse
Gomes et al., 2002, Mu-opioid receptor down-regulation and tolerance are not equally dependent upon G-protein signaling., Pharmacol. Biochem. Behav.
Weerts et al., 2008, Differences in delta- and mu-opioid receptor blockade measured by positron emission tomography in naltrexone-treated recently abstinent alcohol-dependent subjects., Neuropsychopharmacology
Helm et al., Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification., Pain Physician
Hendershot CS et al., 2020, OPRM1 Moderates Daily Associations of Naltrexone Adherence With Alcohol Consumption: Preliminary Evidence From a Mobile Health Trial., Alcohol Clin Exp Res
Hartwell EE et al., 2020, Systematic review and meta-analysis of the moderating effect of rs1799971 in OPRM1, the mu-opioid receptor gene, on response to naltrexone treatment of alcohol use disorder., Addiction
Foulds JA et al., 2015, OPRM1 genotype and naltrexone response in depressed alcohol-dependent patients., Pharmacogenet Genomics
Chamorro AJ et al., 2012, Association of µ-opioid receptor (OPRM1) gene polymorphism with response to naltrexone in alcohol dependence: a systematic review and meta-analysis., Addict Biol
Oslin DW et al., 2015, Naltrexone vs Placebo for the Treatment of Alcohol Dependence: A Randomized Clinical Trial., JAMA Psychiatry
Jonas DE et al., 2014, Genetic polymorphisms and response to medications for alcohol use disorders: a systematic review and meta-analysis., Pharmacogenomics
Roche DJO et al., 2019, Lack of Association between Opioid-Receptor Genotypes and Smoking Cessation Outcomes in a Randomized, Controlled Naltrexone Trial., Alcohol Alcohol
Coller JK et al., 2011, OPRM1 A118G genotype fails to predict the effectiveness of naltrexone treatment for alcohol dependence., Pharmacogenet Genomics
Barrios de Tomasi et al., [Opioid antagonists and alcohol consumption]., Rev Neurol
Goodman et al., 2007, Mu opioid receptor antagonists: recent developments., ChemMedChem
Herz, 1998, Opioid reward mechanisms: a key role in drug abuse?, Can. J. Physiol. Pharmacol.
Ray R et al., 2006, Association of OPRM1 A118G variant with the relative reinforcing value of nicotine., Psychopharmacology (Berl)
Kato, 2008, [Pharmacological effects of a mu-opioid receptor antagonist naltrexone on alcohol dependence]., Nihon Arukoru Yakubutsu Igakkai Zasshi
McWhinney-Glass S et al., 2013, Cumulative genetic risk predicts platinum/taxane-induced neurotoxicity., Clin Cancer Res
Grond et al., 2004, Clinical pharmacology of tramadol., Clin Pharmacokinet
Raffa et al., 1992, Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an 'atypical' opioid analgesic., J. Pharmacol. Exp. Ther.
Potschka et al., 2000, Anticonvulsant and proconvulsant effects of tramadol, its enantiomers and its M1 metabolite in the rat kindling model of epilepsy., Br. J. Pharmacol.
Gillen et al., 2000, Affinity, potency and efficacy of tramadol and its metabolites at the cloned human mu-opioid receptor., Naunyn Schmiedebergs Arch. Pharmacol.
Liu YC et al., 2012, Human mu-opioid receptor gene A118G polymorphism predicts the efficacy of tramadol/acetaminophen combination tablets (ultracet) in oxaliplatin-induced painful neuropathy., Cancer
Ide et al., 2006, Mu opioid receptor-dependent and independent components in effects of tramadol., Neuropharmacology
Frink et al., 1996, Influence of tramadol on neurotransmitter systems of the rat brain., Arzneimittelforschung
Muriel J et al., 2019, Pharmacogenetics and prediction of adverse events in prescription opioid use disorder patients., Basic Clin Pharmacol Toxicol
Minami et al., 2007, Pharmacological aspects of the effects of tramadol on G-protein coupled receptors., J. Pharmacol. Sci.
Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
di Bosco et al., 2008, Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors., Chem Biol Drug Des
Tan-No et al., 2003, Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice., Eur J Pharm Sci
Giagnoni et al., 1983, Loperamide: evidence of interaction with mu and delta opioid receptors., Life Sci.
DeHaven-Hudkins et al., 1999, Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity., J. Pharmacol. Exp. Ther.
Roge et al., 1993, The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide., Scand. J. Gastroenterol.
Hoke et al., 1997, Comparative pharmacokinetics and pharmacodynamics of remifentanil, its principle metabolite (GR90291) and alfentanil in dogs., J. Pharmacol. Exp. Ther.
Warner et al., 1996, Intracranial pressure and hemodynamic effects of remifentanil versus alfentanil in patients undergoing supratentorial craniotomy., Anesth. Analg.
Scott et al., 2005, Spotlight on remifentanil for general anaesthesia., CNS Drugs
Guy et al., 1997, Comparison of remifentanil and fentanyl in patients undergoing craniotomy for supratentorial space-occupying lesions., Anesthesiology
Patel et al., 1996, Remifentanil., Drugs
Scott et al., 2005, Remifentanil: a review of its use during the induction and maintenance of general anaesthesia., Drugs
Barrett et al., 2001, Importance of sex and relative efficacy at the mu opioid receptor in the development of tolerance and cross-tolerance to the antinociceptive effects of opioids., Psychopharmacology (Berl.)
Gharagozlou et al., 2003, Activity of opioid ligands in cells expressing cloned mu opioid receptors., BMC Pharmacol.
Cook et al., 2000, Sex-related differences in the antinociceptive effects of opioids: importance of rat genotype, nociceptive stimulus intensity, and efficacy at the mu opioid receptor., Psychopharmacology (Berl.)
Morgan et al., 1999, An examination of the interactions between the antinociceptive effects of morphine and various mu-opioids: the role of intrinsic efficacy and stimulus intensity., Anesth. Analg.
Jacobs et al., 1992, Opioid receptor affinity for agonist-antagonist analgesics., J Am Podiatr Med Assoc
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.
Zernig et al., 1997, Clocinnamox inhibits the intravenous self-administration of opioid agonists in rhesus monkeys: comparison with effects on opioid agonist-mediated antinociception., Psychopharmacology (Berl.)
McNicol et al., 2008, Mu-opioid antagonists for opioid-induced bowel dysfunction., Cochrane Database Syst Rev
Meerpohl et al., 2008, [News from the cochrane library: mu opioid antagonists for opioid-induced bowel dysfunction]., Z Gastroenterol
Kishioka et al., 2000, Diltiazem enhances the analgesic but not the respiratory depressant effects of morphine in rhesus monkeys., Eur. J. Pharmacol.
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.
Tao et al., 2006, Nalbuphine is effective in decreasing the rewarding effect induced by morphine in rats., Drug Alcohol Depend
Mello et al., 2005, Effects of the mixed mu/kappa opioid nalbuphine on cocaine-induced changes in subjective and cardiovascular responses in men., Neuropsychopharmacology
Hoehe et al., 1993, Opiates increase plasma catecholamines in humans., Psychoneuroendocrinology
Vandormael B et al., 2011, Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixed μ/δ opioid receptor agonistic properties., J Med Chem
Cajanus K et al., 2014, How much oxycodone is needed for adequate analgesia after breast cancer surgery: effect of the OPRM1 118A>G polymorphism., J Pain
Dietis et al., 2009, Simultaneous targeting of multiple opioid receptors: a strategy to improve side-effect profile., Br J Anaesth
Pu J et al., 2019, Correlation between gene polymorphism and opioid efficacy in patients with gastric or intestinal cancer., Eur Rev Med Pharmacol Sci
Riley et al., 2008, Oxycodone: a review of its use in the management of pain., Curr Med Res Opin
Ordóñez Gallego et al., 2007, Oxycodone: a pharmacological and clinical review., Clin Transl Oncol
Naito T et al., 2011, CYP3A5*3 affects plasma disposition of noroxycodone and dose escalation in cancer patients receiving oxycodone., J Clin Pharmacol
Zhang S et al., 2009, A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors., Bioorg Med Chem Lett
Commiskey et al., 2005, Butorphanol: effects of a prototypical agonist-antagonist analgesic on kappa-opioid receptors., J. Pharmacol. Sci.
Fan et al., 2002, Butorphanol dependence and withdrawal decrease hippocampal kappa 2-opioid receptor binding., Brain Res.
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.
Fan et al., 2002, Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain., Brain Res. Bull.
Narita et al., 1994, Repeated administration of opioids alters characteristics of membrane-bound phorbol ester binding in rat brain., Eur. J. Pharmacol.
Walsh et al., 2008, Evaluation of the mu and kappa opioid actions of butorphanol in humans through differential naltrexone blockade., Psychopharmacology (Berl.)
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.
Vivian et al., 1999, kappa-Opioid receptor effects of butorphanol in rhesus monkeys., J. Pharmacol. Exp. Ther.
You et al., 2005, The novel analgesic and high-efficacy 5-HT1A receptor agonist F 13640 inhibits nociceptive responses, wind-up, and after-discharges in spinal neurons and withdrawal reflexes., Exp. Neurol.
Hajiha et al., 2009, Opioid receptor mechanisms at the hypoglossal motor pool and effects on tongue muscle activity in vivo., J. Physiol. (Lond.)
Dosen-Micovic et al., 2006, Steric interactions and the activity of fentanyl analogs at the mu-opioid receptor., Bioorg. Med. Chem.
Dardonville et al., 2006, Synthesis and pharmacological studies of new hybrid derivatives of fentanyl active at the mu-opioid receptor and I2-imidazoline binding sites., Bioorg. Med. Chem.
Smith et al., 1980, The interaction of ketamine with the opiate receptor., Life Sci.
Hustveit et al., 1995, Interaction of the chiral forms of ketamine with opioid, phencyclidine, sigma and muscarinic receptors., Pharmacol. Toxicol.
Emmerson et al., 1996, Characterization of opioid agonist efficacy in a C6 glioma cell line expressing the mu opioid receptor., J. Pharmacol. Exp. Ther.
Traynor et al., 1995, Modulation by mu-opioid agonists of guanosine-5'-O-(3-[35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells., Mol. Pharmacol.
Selley et al., 1997, mu-Opioid receptor-stimulated guanosine-5'-O-(gamma-thio)-triphosphate binding in rat thalamus and cultured cell lines: signal transduction mechanisms underlying agonist efficacy., Mol. Pharmacol.
Morgan et al., 1998, The mu opioid irreversible antagonist beta-funaltrexamine differentiates the discriminative stimulus effects of opioids with high and low efficacy at the mu opioid receptor., Psychopharmacology (Berl.)
Saha et al., 1990, Effects of morphine, buprenorphine, pentazocine and nalorphine on acquisition and extinction of active avoidance responses in rats., Indian J. Physiol. Pharmacol.
Kamei et al., 1994, Effects of diabetes on the antinociceptive effect of (+/-)pentazocine in mice., Res. Commun. Chem. Pathol. Pharmacol.
Martin et al., 1984, Stereoisomers of [3H]-N-allylnormetazocine bind to different sites in mouse brain., J. Pharmacol. Exp. Ther.
Levine et al., 1988, Synergism between the analgesic actions of morphine and pentazocine., Pain
Kakko et al., 2008, Mood and neuroendocrine response to a chemical stressor, metyrapone, in buprenorphine-maintained heroin dependence., Biol. Psychiatry
Eap CB et al., 2002, Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence., Clin Pharmacokinet
Kvam et al., 2004, Genetic analysis of the murine mu opioid receptor: increased complexity of Oprm gene splicing., J. Mol. Med.
Sotgiu et al., 2009, Cooperative N-methyl-D-aspartate (NMDA) receptor antagonism and mu-opioid receptor agonism mediate the methadone inhibition of the spinal neuron pain-related hyperactivity in a rat model of neuropathic pain., Pharmacol. Res.
Shi et al., 2002, Sequence variations in the mu-opioid receptor gene (OPRM1) associated with human addiction to heroin., Hum. Mutat.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Rennison D et al., 2006, Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring., J Med Chem
GREEN, 1959, Comparative effects of analgesics on pain threshold, respiratory frequency and gastrointestinal propulsion., Br J Pharmacol Chemother
Mizoguchi et al., 2002, Antagonistic property of buprenorphine for putative epsilon-opioid receptor-mediated G-protein activation by beta-endorphin in pons/medulla of the mu-opioid receptor knockout mouse., Neuroscience
Ide et al., 2004, Buprenorphine antinociception is abolished, but naloxone-sensitive reward is retained, in mu-opioid receptor knockout mice., Neuropsychopharmacology
Kishioka et al., 2000, Buprenorphine and methoclocinnamox: agonist and antagonist effects on respiratory function in rhesus monkeys., Eur. J. Pharmacol.
Sánchez-Blázquez et al., 2001, Agonists determine the pattern of G-protein activation in mu-opioid receptor-mediated supraspinal analgesia., Brain Res. Bull.
Zubieta et al., 2000, Buprenorphine-induced changes in mu-opioid receptor availability in male heroin-dependent volunteers: a preliminary study., Neuropsychopharmacology
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Wand GS et al., 2002, The mu-opioid receptor gene polymorphism (A118G) alters HPA axis activation induced by opioid receptor blockade., Neuropsychopharmacology
Nikolaev VO et al., 2007, Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors., J Biol Chem
Hernandez-Avila CA et al., 2003, Association between the cortisol response to opioid blockade and the Asn40Asp polymorphism at the mu-opioid receptor locus (OPRM1)., Am J Med Genet B Neuropsychiatr Genet
Neal et al., 2003, Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors., J. Chem. Neuroanat.
Narita et al., 2003, Up-regulation of mu-opioid receptor-mediated G-protein activation in protein kinase Cgamma knockout mice following repeated naloxone treatment., Neurosci. Lett.
Marek, 2003, Behavioral evidence for mu-opioid and 5-HT2A receptor interactions., Eur. J. Pharmacol.
Spetea et al., 2003, Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist., Eur. J. Neurosci.
van Dorp et al., 2007, Naloxone treatment in opioid addiction: the risks and benefits., Expert Opin Drug Saf
Hernandez-Avila CA et al., 2007, Population-specific effects of the Asn40Asp polymorphism at the mu-opioid receptor gene (OPRM1) on HPA-axis activation., Pharmacogenet Genomics
Freye et al., 1998, [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]., Schmerz
Chong RY et al., 2006, The mu-opioid receptor polymorphism A118G predicts cortisol responses to naloxone and stress., Neuropsychopharmacology
Allen et al., 2003, The competitive N-methyl-D-aspartate receptor antagonist (-)-6-phosphonomethyl-deca-hydroisoquinoline-3-carboxylic acid (LY235959) potentiates the antinociceptive effects of opioids that vary in efficacy at the mu-opioid receptor., J. Pharmacol. Exp. Ther.
Prommer, 2007, Levorphanol: the forgotten opioid., Support Care Cancer
Thompson et al., 2004, Activation of G-proteins by morphine and codeine congeners: insights to the relevance of O- and N-demethylated metabolites at mu- and delta-opioid receptors., J. Pharmacol. Exp. Ther.
Boswell MV et al., 2013, The role of hydromorphone and OPRM1 in postoperative pain relief with hydrocodone., Pain Physician
Olson KM et al., 2019, Comprehensive molecular pharmacology screening reveals potential new receptor interactions for clinically relevant opioids., PLoS One
Kotzer et al., 2000, The antitussive activity of delta-opioid receptor stimulation in guinea pigs., J. Pharmacol. Exp. Ther.
Peckham et al., 2006, Comparison of the antinociceptive response to morphine and morphine-like compounds in male and female Sprague-Dawley rats., J. Pharmacol. Exp. Ther.
Stoops et al., 2010, Intravenous oxycodone, hydrocodone, and morphine in recreational opioid users: abuse potential and relative potencies., Psychopharmacology (Berl.)
Hennies et al., 1988, Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids., Arzneimittelforschung
Walsh et al., 2008, The relative abuse liability of oral oxycodone, hydrocodone and hydromorphone assessed in prescription opioid abusers., Drug Alcohol Depend
Oertel et al., 2006, The mu-opioid receptor gene polymorphism 118A>G depletes alfentanil-induced analgesia and protects against respiratory depression in homozygous carriers., Pharmacogenet. Genomics
Leung et al., 2001, Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain., Pain
Lötsch et al., 2005, Are mu-opioid receptor polymorphisms important for clinical opioid therapy?, Trends Mol Med
Ginosar Y et al., 2009, Mu-opioid receptor (A118G) single-nucleotide polymorphism affects alfentanil requirements for extracorporeal shock wave lithotripsy: a pharmacokinetic-pharmacodynamic study., Br J Anaesth
Garrido et al., 2000, Pharmacokinetic-pharmacodynamic analysis of the EEG effect of alfentanil in rats following beta-funaltrexamine-induced mu-opioid receptor "knockdown" in vivo., Pharm. Res.
Gardell et al., 2006, Opioid receptor-mediated hyperalgesia and antinociceptive tolerance induced by sustained opiate delivery., Neurosci. Lett.
Chamberlin et al., 2007, Oral oxymorphone for pain management., Ann Pharmacother
Lemberg et al., 2006, Antinociception by spinal and systemic oxycodone: why does the route make a difference? In vitro and in vivo studies in rats., Anesthesiology
Halimi et al., 2000, Modulation of adenosine concentration by opioid receptor agonists in rat striatum., Eur. J. Pharmacol.
Spetea et al., 1998, Affinity profiles of novel delta-receptor selective benzofuran derivatives of non-peptide opioids., Neurochem. Res.
Takahama et al., 2007, Central and peripheral mechanisms of narcotic antitussives: codeine-sensitive and -resistant coughs., Cough
Baber M et al., 2015, The pharmacogenetics of codeine pain relief in the postpartum period., Pharmacogenomics J
Freissmuth et al., 1993, Binding and structure-activity-relation of benzo[f]isoquinoline- and norcodeinone-derivatives at mu-opioid receptors in the rat cerebral cortex., Br. J. Pharmacol.
Kraft, 2007, Emerging pharmacologic options for treating postoperative ileus., Am J Health Syst Pharm
Saufl et al., 2006, Nurses are everywhere: a practical perspective on the surgical team in managing postoperative ileus., J. Perianesth. Nurs.
Schmidt, 2001, Alvimopan* (ADL 8-2698) is a novel peripheral opioid antagonist., Am. J. Surg.
Büchler et al., 2008, Clinical trial: alvimopan for the management of post-operative ileus after abdominal surgery: results of an international randomized, double-blind, multicentre, placebo-controlled clinical study., Aliment. Pharmacol. Ther.
Neary et al., 2005, Alvimopan., Expert Opin Investig Drugs
Yuan, 2007, Methylnaltrexone mechanisms of action and effects on opioid bowel dysfunction and other opioid adverse effects., Ann Pharmacother
Bencherif et al., 2004, Mu-opioid receptor binding measured by [11C]carfentanil positron emission tomography is related to craving and mood in alcohol dependence., Biol. Psychiatry
Bartenstein et al., 1994, Quantification of opiate receptors in two patients with mesiobasal temporal lobe epilepsy, before and after selective amygdalohippocampectomy, using positron emission tomography., Epilepsy Res.
Mayberg et al., 1991, Quantification of mu and non-mu opiate receptors in temporal lobe epilepsy using positron emission tomography., Ann. Neurol.
Jewett et al., 2004, In vivo evaluation of new carfentanil-based radioligands for the mu opiate receptor., Nucl. Med. Biol.
Bencherif et al., 2004, Application of MRI-based partial-volume correction to the analysis of PET images of mu-opioid receptors using statistical parametric mapping., J. Nucl. Med.
Choi et al., 2006, The opioid ligand binding of human mu-opioid receptor is modulated by novel splice variants of the receptor., Biochem. Biophys. Res. Commun.
Johnson et al., 2006, Agonist-selective mechanisms of mu-opioid receptor desensitization in human embryonic kidney 293 cells., Mol. Pharmacol.
Yamada et al., 2006, Morphine can produce analgesia via spinal kappa opioid receptors in the absence of mu opioid receptors., Brain Res.
Castro et al., 2006, A quantitative approach to measure joint pain in experimental osteoarthritis--evidence of a role for nitric oxide., Osteoarthr. Cartil.
Poulain et al., 2001, From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands., J. Med. Chem.
Zamponi GW et al., 2009, Scaffold-based design and synthesis of potent N-type calcium channel blockers., Bioorg Med Chem Lett
Inturrisi, Clinical pharmacology of opioids for pain., Clin J Pain
Sarhill et al., 2001, Hydromorphone: pharmacology and clinical applications in cancer patients., Support Care Cancer
Quigley, 2002, Hydromorphone for acute and chronic pain., Cochrane Database Syst Rev
Kumar et al., 2008, Hydromorphone efficacy and treatment protocol impact on tolerance and mu-opioid receptor regulation., Eur. J. Pharmacol.
Crooks et al., 2006, Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners., Bioorg. Med. Chem. Lett.
Gilbert et al., 2004, Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine., Eur. J. Pharmacol.
Cargnin S et al., 2014, Combined effect of common gene variants on response to drug withdrawal therapy in medication overuse headache., Eur J Clin Pharmacol
Schinka JA et al., 2002, A functional polymorphism within the mu-opioid receptor gene and risk for abuse of alcohol and other substances., Mol Psychiatry
Arias A et al., 2006, Association of an Asn40Asp (A118G) polymorphism in the mu-opioid receptor gene with substance dependence: a meta-analysis., Drug Alcohol Depend
Türkan H et al., 2019, The association between the OPRM1 A118G polymorphism and addiction in a Turkish population., Arh Hig Rada Toksikol
Tan EC et al., 2003, Mu opioid receptor gene polymorphisms and heroin dependence in Asian populations., Neuroreport
Greenwald et al., 2003, Effects of buprenorphine maintenance dose on mu-opioid receptor availability, plasma concentrations, and antagonist blockade in heroin-dependent volunteers., Neuropsychopharmacology
Deb I et al., 2010, Single-nucleotide polymorphism (A118G) in exon 1 of OPRM1 gene causes alteration in downstream signaling by mu-opioid receptor and may contribute to the genetic risk for addiction., J Neurochem
Yao et al., 2005, Activator of G protein signaling 3 regulates opiate activation of protein kinase A signaling and relapse of heroin-seeking behavior., Proc. Natl. Acad. Sci. U.S.A.
Franke P et al., 2001, Nonreplication of association between mu-opioid-receptor gene (OPRM1) A118G polymorphism and substance dependence., Am J Med Genet
Tolami HF et al., 2020, Haplotype-Based Association and In Silico Studies of OPRM1 Gene Variants with Susceptibility to Opioid Dependence Among Addicted Iranians Undergoing Methadone Treatment., J Mol Neurosci
Gao X et al., 2017, Contribution of Genetic Polymorphisms and Haplotypes in DRD2, BDNF, and Opioid Receptors to Heroin Dependence and Endophenotypes Among the Han Chinese., OMICS
Antonilli et al., 2005, Effect of repeated administrations of heroin, naltrexone, methadone, and alcohol on morphine glucuronidation in the rat., Psychopharmacology (Berl.)
Szeto CY et al., 2001, Association between mu opioid receptor gene polymorphisms and Chinese heroin addicts., Neuroreport
Becker et al., 2004, MOR1 receptor mRNA expression in human brains of drug-related fatalities-a real-time PCR quantification., Forensic Sci. Int.
Haerian BS et al., 2013, OPRM1 rs1799971 polymorphism and opioid dependence: evidence from a meta-analysis., Pharmacogenomics
Leysen et al., 1982, In vitro binding properties of 3H-sufentanil, a superior ligand for the mu-opiate receptor., Arch Int Pharmacodyn Ther
Colpaert et al., 1986, Epidural and intravenous sufentanil in the rat: analgesia, opiate receptor binding, and drug concentrations in plasma and brain., Anesthesiology
Camorcia M et al., 2012, Effect of μ-opioid receptor A118G polymorphism on the ED50 of epidural sufentanil for labor analgesia., Int J Obstet Anesth
Hurlé, 2001, Changes in the expression of G protein-coupled receptor kinases and beta-arrestin 2 in rat brain during opioid tolerance and supersensitivity., J. Neurochem.
Ilien et al., 1988, A mu-opioid receptor-filter assay. Rapid estimation of binding affinity of ligands and reversibility of long-lasting ligand-receptor complexes., Biochem. Pharmacol.
Levron, 1991, [Pharmacokinetics and pharmacodynamics of morphinomimetics in the central nervous system]., Agressologie
Leonard et al., 2015, Naloxegol: treatment for opioid-induced constipation in chronic non-cancer pain., Ann Pharmacother
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
Tidgewell K et al., 2008, Herkinorin analogues with differential beta-arrestin-2 interactions., J Med Chem
Harikumar KG et al., 2010, Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization., J Med Chem
Vilardaga JP et al., 2008, Conformational cross-talk between alpha2A-adrenergic and mu-opioid receptors controls cell signaling., Nat Chem Biol
Leung
Wahlström et al., 1994, Tricyclic antidepressants inhibit opioid receptor binding in human brain and hepatic morphine glucuronidation., Pharmacol. Toxicol.
Hamon et al., 1987, Opioid receptors and neuropeptides in the CNS in rats treated chronically with amoxapine or amitriptyline., Neuropharmacology
van Wijngaarden et al., 1990, The concept of selectivity in 5-HT receptor research., Eur. J. Pharmacol.
Kleinjan M et al., 2013, Dual growth of adolescent smoking and drinking: evidence for an interaction between the mu-opioid receptor (OPRM1) A118G polymorphism and sex., Addict Biol
Lerman C et al., 2004, The functional mu opioid receptor (OPRM1) Asn40Asp variant predicts short-term response to nicotine replacement therapy in a clinical trial., Pharmacogenomics J
Munafò MR et al., 2007, Association of the mu-opioid receptor gene with smoking cessation., Pharmacogenomics J
Chen YT et al., 2013, OPRM1 genetic polymorphisms are associated with the plasma nicotine metabolite cotinine concentration in methadone maintenance patients: a cross sectional study., J Hum Genet
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ALFENTANIL OPRM1

Interaction Score: 3.89

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16906017 11240090 11752352 15694871 19605407 10955836

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank
ANILERIDINE OPRM1

Interaction Score: 2.33

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank
METHADYL ACETATE OPRM1

Interaction Score: 1.95

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
20163389 6268422 11752352 19153939

Sources:
DrugBank
DEZOCINE OPRM1

Interaction Score: 1.95

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor partial agonist

Trial Name -

PMIDs:
11702089 12513698 10958085 9399970 9972766 1361946

Sources:
TEND TdgClinicalTrial DrugBank ChemblInteractions
LEVALLORPHAN OPRM1

Interaction Score: 1.75

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Details of the Assay for Interaction Competition binding assay- the calculated K<sub>i</sub> varies depending on the radioligand used.

PMIDs:
8819494 7723747 9016350 8968334 9862398

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
DIPHENOXYLATE OPRM1

Interaction Score: 1.56

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8386327 18192961 8583364 11752352 10202212

Sources:
TEND TdgClinicalTrial DrugBank
ALVIMOPAN OPRM1

Interaction Score: 1.43

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction yes

PMIDs:
17909271 16597533 11755894 19086236 15882122 11752352

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
ETHYLMORPHINE OPRM1

Interaction Score: 1.17

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
16580639 16682505 16530171 11752352 16580848

Sources:
DrugBank
NALTREXONE OPRM1

Interaction Score: 1.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
17487229 18354714 32020635 31961981 25715171 22515274 25760804 25410894 31206155 21946895 11752352 17661275 17918759 9673788 16960700 19068776

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
CHEMBL2365680 OPRM1

Interaction Score: 1.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
15589524 16332149 16114980 19403616 11752352 16376082 16797997

Sources:
DrugBank
DAMGO OPRM1

Interaction Score: 0.97

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
24613457 18380425 20235611

Sources:
DTC GuideToPharmacology
HYDROCODONE OPRM1

Interaction Score: 0.91

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name ZX002, hydrocodone bitartrate

Novel drug target Established target

Trial Name PTI-701

PMIDs:
14600248 23703421 31170174 10640321 16291875 11752352 20665209 2849950 18606504

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
NALBUPHINE OPRM1

Interaction Score: 0.91

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17407276 9084061 18425947 18810678 10844102 19403853 16517095 15602503 9399970 8388112

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
OXYMORPHONE OPRM1

Interaction Score: 0.88

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name oxymorphone hydrochloride, EN3202,Opana, Opana ER

PMIDs:
16343768 17595308 17006080 11752352 10854833 9712193

Sources:
TEND TdgClinicalTrial DrugBank
LEVOMETHADYL ACETATE OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
11561100 2471291 9360954 11752352 10911931

Sources:
DrugBank
CHEMBL255300 OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17616524

Sources:
DTC
NALOXEGOL OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
25471070

Sources:
DrugBank
AXELOPRAN OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name TD-1211

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
CARFENTANIL OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
14744466 7957034 1656846 15028244 15001679

Sources:
DrugBank
ALFENTANIL HYDROCHLORIDE OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
DIMETHYLTHIAMBUTENE OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
17139284 17016423 13651575

Sources:
DrugBank
CLOCINNAMOX OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17004724

Sources:
DTC
PENTAZOCINE OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2286420 8042002 8968334 6094791 3419842

Sources:
TEND TdgClinicalTrial DrugBank
BEVENOPRAN OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Mu opioid receptor antagonist

Direct Interaction yes

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
PROPOXYPHENE OPRM1

Interaction Score: 0.78

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10690289 6249436 11752352 10379623 19604717 9399970 7562497

Sources:
TEND TdgClinicalTrial DrugBank
SUFENTANIL OPRM1

Interaction Score: 0.72

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
6131653 3014923 22153130 11299311 31773688 11752352 2847746 1688220

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
BUTORPHANOL OPRM1

Interaction Score: 0.72

Interaction Types & Directionality:

agonist (activating)

partial antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
15942128 12470863 8746803 12127012 7705457 17909753 8968334 9399970 10381785

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
ELUXADOLINE OPRM1

Interaction Score: 0.65

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

Specific Action of the Ligand Agonist

PMIDs:
25261794 23583433

Sources:
DrugBank GuideToPharmacology ChemblInteractions
HYDROMORPHONE OPRM1

Interaction Score: 0.62

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
12479250 11305075 11869661 18789923

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
DIACETYLMORPHINE HYDROCHLORIDE OPRM1

Interaction Score: 0.58

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
16580639 12902992 15937104 15986196 15013161

Sources:
DrugBank
ENDOMORPHIN-1 OPRM1

Interaction Score: 0.58

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? True

Direct Interaction? False

PMIDs:
22724433

Sources:
DTC GuideToPharmacology
LEVORPHANOL OPRM1

Interaction Score: 0.58

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
12975489 17039381

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
REMIFENTANIL OPRM1

Interaction Score: 0.56

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name remifentanil,Ultiva

Novel drug target Established target

PMIDs:
9103501 8694317 16332149 9066316 8875131 16114980 11752352

Sources:
TEND TdgClinicalTrial DrugBank

METHYLNALTREXONE OPRM1

Interaction Score: 0.52

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Displacement of [<sup>3</sup>H]DAMGO from human μ opioid receptors expressed in CHO cells

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
17504835

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology

NALOXONE OPRM1

Interaction Score: 0.52

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name REN-213

Trial Name buprenorphine + naloxone,Suboxone

Novel drug target Established target

PMIDs:
11751037 17616524 12627468 12842269 18354714 12566163 12909198 12887410 17367258 11752352 18004207 17918759 12799988 16123758

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
ETORPHINE OPRM1

Interaction Score: 0.52

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
11098106 11420091 12435815 11752352 10881033 11900797

Sources:
DrugBank GuideToPharmacology
CODEINE OPRM1

Interaction Score: 0.49

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Full agonist

PMIDs:
17620111 15509185 11752352 25752520 8306082

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
OXYCODONE OPRM1

Interaction Score: 0.48

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name COL-003, sustained release oxycodone

Novel drug target Established target

Trial Name PTI-801,Oxytrex

PMIDs:
25239082 19474215 31773688 18039433 17525040 21209234

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank ChemblInteractions
BUPRENORPHINE OPRM1

Interaction Score: 0.46

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
12435410 15100703 30549211 11752352 10729371 11275413 10942856

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
DIACETYLMORPHINE OPRM1

Interaction Score: 0.42

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
12657887 16580639 12902992 19891732 15937104 11424981 31853823 28692418 11933204 15986196 11338173 15013161 23651028

Sources:
PharmGKB
METENKEFALIN OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
24856378

Sources:
DrugBank
CHEMBL13786 OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17616524

Sources:
DTC
TIANEPTINE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
25026323 28303899

Sources:
PharmGKB DrugBank
DIFENOXIN HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DIHYDROCODEINE BITARTRATE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PZM21 OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Biased agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
FENTANYL CITRATE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PHENCYCLIDINE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEVOMETHADYL ACETATE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEPERIDINE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYCODONE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
TRAMADOL HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NALDEMEDINE TOSYLATE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Mu opioid receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHYLSAMIDORPHAN OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Mu opioid receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROPOXYPHENE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OLICERIDINE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHYLNALTREXONE BROMIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Mu opioid receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DIHYDROMORPHINE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
16777416 15178355 19474215

Sources:
DrugBank GuideToPharmacology
MORPHINE SULFATE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions

OXYCODEGOL OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name NKTR-181

Details of the Assay for Interaction Competitive membrane binding assay measuring displacement [3H]naloxone from human μ receptors expressed by CHO cells.

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology

NALTALIMIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor partial agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
REMIFENTANIL HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
METHADONE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GSK-1521498 OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology
FRAKEFAMIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NALMEFENE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
NALOXEGOL OXALATE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
FENTANYL HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
NALDEMEDINE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
DrugBank GuideToPharmacology ChemblInteractions
CHEMBL570176 OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19892550

Sources:
DTC
CHEMBL409225 OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21978284

Sources:
DTC
LEVORPHANOL TARTRATE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
HYDROMORPHONE HYDROCHLORIDE OPRM1

Interaction Score: 0.39

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
KETOBEMIDONE OPRM1

Interaction Score: 0.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
8153059 8878254

Sources:
DrugBank
DIPRENORPHINE OPRM1

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
20641600

Sources:
DrugBank GuideToPharmacology
Z160 OPRM1

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19815411

Sources:
DTC
LOPERAMIDE OPRM1

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Agonist

PMIDs:
18284554 14592702 11752352 6319884 10087042 8488368

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
SAMIDORPHAN OPRM1

Interaction Score: 0.26

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Mu opioid receptor antagonist

Direct Interaction yes

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
TRAMADOL OPRM1

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
15509185 1309873 10991912 10961373 21837673 16793069 8955860 30549211 17380034 11752352 31004280

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
TAPENTADOL OPRM1

Interaction Score: 0.22

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10592235

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
MARAVIROC OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ANILERIDINE HYDROCHLORIDE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
TAPENTADOL HYDROCHLORIDE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DADLE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BUTORPHANOL TARTRATE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor partial agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ANILERIDINE PHOSPHATE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CEBRANOPADOL OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Details of the Assay for Interaction Radioligand binding assay

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
LEVALLORPHAN TARTRATE OPRM1

Interaction Score: 0.19

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
FENTANYL OPRM1

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
15589524 16332149 16114980 19403616 11752352 16376082 16797997

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions
MORPHINE OPRM1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Novel drug target Established target

Trial Name intranasal morphine,Rylomine

PMIDs:
17616524 16580639 16682505 16530171 18193048 18380425 11752352 16580848

Sources:
TEND DTC TdgClinicalTrial DrugBank GuideToPharmacology
MORPHINE GLUCURONIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
PHOLCODINE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
OPIUM OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
CODEINE SULFATE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BUPRENORPHINE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYMORPHONE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AXOMADOL OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
QUADAZOCINE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NORMORPHINE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NALORPHINE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
GuideToPharmacology
BNTX OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NALBUPHINE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ETHYLKETOCYCLAZOCINE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CHEMBL442577 OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology
HYDROCODONE POLISTIREX OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FAXELADOL OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NALTREXONE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HYDROCODONE BITARTRATE OPRM1

Interaction Score: 0.13

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 PHOSPHATE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LOPERAMIDE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ATICAPRANT OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
BENZHYDROCODONE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name KP201 (prodrug of hydrocodone)

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
CODEINE POLISTIREX OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NALTRINDOLE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NALMEFENE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
ADL-5747 OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology
ZYKLOPHIN OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DIPHENOXYLATE HYDROCHLORIDE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ODELEPRAN OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
METHADONE OPRM1

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
17850768 12405865 14991152 19717013 11933204 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
CARBETAPENTANE OPRM1

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
8872359

Sources:
DrugBank
TRIMEBUTINE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
1963196

Sources:
DrugBank
NALOXONE HYDROCHLORIDE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
ETONITAZENE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
SUFENTANIL CITRATE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NALTRIBEN OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NORBINALTORPHIMINE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
COTININE OPRM1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23223006

Sources:
PharmGKB
MEPERIDINE OPRM1

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
11585443

Sources:
DrugBank GuideToPharmacology
NICOTINE OPRM1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22260295 15007373 17224915 23223006 11840318 16387451 31246565 16960700

Sources:
PharmGKB
ONDANSETRON OPRM1

Interaction Score: 0.06

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
2164935

Sources:
DrugBank
COCAINE OPRM1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11840318 16387451 31246565

Sources:
PharmGKB
KETAMINE OPRM1

Interaction Score: 0.06

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
6246318 8835358

Sources:
DrugBank
NABIXIMOLS OPRM1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11840318 31246565 26264914

Sources:
PharmGKB DrugBank
SUMATRIPTAN OPRM1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25096645

Sources:
PharmGKB
DEXTROMETHORPHAN OPRM1

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
7562497

Sources:
DrugBank
CHEMBL609728 OPRM1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
METHAMPHETAMINE OPRM1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16402083

Sources:
PharmGKB
AMITRIPTYLINE OPRM1

Interaction Score: 0.03

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
7971731 3037421

Sources:
DrugBank
ACETAMINOPHEN OPRM1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21837673

Sources:
PharmGKB
AMPHETAMINE OPRM1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
CANNABIDIOL OPRM1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26264914

Sources:
DrugBank
ARIPIPRAZOLE OPRM1

Interaction Score: 0.02

Interaction Types & Directionality:

ligand

Interaction Info:

PMIDs:
26346901

Sources:
DrugBank
CARBOPLATIN OPRM1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23963862

Sources:
PharmGKB
DOCETAXEL OPRM1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23963862

Sources:
PharmGKB
PACLITAXEL OPRM1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23963862

Sources:
PharmGKB

Ensembl: ENSG00000112038
- Version: 101_38
Alternate Names:

OPRM1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P35372
- Version: January-2014
Alternate Names:

OPRM1 Gene Symbol

MOR Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
HopkinsGroom: P35372
- Version: 11-September-2012
Alternate Names:

4988 Entrez Gene Id

MU-TYPE OPIOID RECEPTOR Uniprot Protein Name

ENSG00000112038 Ensembl Gene Id

Gene Info:

Interpro Short Name 7TM_GPCR_Rhodpsn

Interpro Name GPCR, rhodopsin-like, 7TM

Interpro Type Family

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P35372
- Version: 01-August-2011
Alternate Names:

P35372 Uniprot Accession

OPRM1 Gene Symbol

4988 Entrez Gene Id

Gene Info:

Target Subclass GPCR

Target Main Class Receptors

Transmembrane Helix Count 7

Publications:
RussLampel: ENSG00000112038
- Version: 26-July-2011
Alternate Names:

OPRM1 Display Id

ENSG00000112038 Ensembl Gene Id

MU-TYPE OPIOID RECEPTOR (MOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35372] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
GuideToPharmacology: 4988
- Version: 29-September-2020
Alternate Names:

8156 HUGO Gene ID

8156 HUGO Gene Symbol

opioid receptor mu 1 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Opioid receptors

GuideToPharmacology Gene Category ID 50

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

PharmGKB: OPRM1

Version: 18-August-2020

Alternate Names:

PA31945 PharmGKB ID

Gene Info:

Publications:

Oertel et al., 2006, The mu-opioid receptor gene polymorphism 118A>G depletes alfentanil-induced analgesia and protects against respiratory depression in homozygous carriers., Pharmacogenet. Genomics

Ginosar Y et al., 2009, Mu-opioid receptor (A118G) single-nucleotide polymorphism affects alfentanil requirements for extracorporeal shock wave lithotripsy: a pharmacokinetic-pharmacodynamic study., Br J Anaesth

Chen YT et al., 2013, OPRM1 genetic polymorphisms are associated with the plasma nicotine metabolite cotinine concentration in methadone maintenance patients: a cross sectional study., J Hum Genet

DrugBank: BE0000770

Version: 5.1.7

Alternate Names:

OPRM1 DrugBank Gene Name

P35372 UniProt Accession

4988 Entrez Gene Id

Gene Info:

Publications:

Grond et al., 2004, Clinical pharmacology of tramadol., Clin Pharmacokinet

Raffa et al., 1992, Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an 'atypical' opioid analgesic., J. Pharmacol. Exp. Ther.

Potschka et al., 2000, Anticonvulsant and proconvulsant effects of tramadol, its enantiomers and its M1 metabolite in the rat kindling model of epilepsy., Br. J. Pharmacol.

DTC: OPRM1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Vandormael B et al., 2011, Superpotent [Dmt¹] dermorphin tetrapeptides containing the 4-aminotetrahydro-2-benzazepin-3-one scaffold with mixed μ/δ opioid receptor agonistic properties., J Med Chem

Nikolaev VO et al., 2007, Live cell monitoring of mu-opioid receptor-mediated G-protein activation reveals strong biological activity of close morphine biosynthetic precursors., J Biol Chem

Wang Y et al., 2012, A new class of highly potent and selective endomorphin-1 analogues containing α-methylene-β-aminopropanoic acids (map)., J Med Chem

HingoraniCasas: ENSG00000112038
- Version: 31-May-2017
Alternate Names:

ENSG00000112038 Gene Symbol

OPRM1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: MOR1
- Version: chembl_23
Alternate Names:

MOR1 GENE_SYMBOL

OPRM1 GENE_SYMBOL

Mu-type opioid receptor UNIPROT

Gene Info:

Publications:
Pharos: OPRM1
- Version: 03-September-2020
Alternate Names:

Mu-type opioid receptor Gene Name

P35372 UniProt ID

Gene Info:

Gene Categories:

KINASE, G PROTEIN COUPLED RECEPTOR

Publications:
GO: OPRM1
- Version: 05-September-2020
Alternate Names:

MOR1 GO Gene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
dGene: OPRM1
- Version: 27-Jun-2013
Alternate Names:

4988 Gene ID

LMOR dGene Synonym

M-OR-1 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:

Direct Interaction	yes
Mechanism of Interaction	Mu opioid receptor partial agonist
Trial Name	-

Novel drug target	Established target
Trial Name	-
Details of the Assay for Interaction	Competition binding assay- the calculated K<sub>i</sub> varies depending on the radioligand used.

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Antagonist

Trial Name	ZX002, hydrocodone bitartrate
Novel drug target	Established target
Trial Name	PTI-701

Specific Action of the Ligand	Agonist
Endogenous Drug?	False
Direct Interaction?	True

Trial Name	TD-1211
Novel drug target	Established target
Direct Interaction	yes

Mechanism of Interaction	Mu opioid receptor agonist
Direct Interaction	yes

Mechanism of Interaction	Mu opioid receptor antagonist
Direct Interaction	yes
Novel drug target	Established target

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False
Direct Interaction?	True

Trial Name	remifentanil,Ultiva
Novel drug target	Established target

Details of the Assay for Interaction	Displacement of [<sup>3</sup>H]DAMGO from human μ opioid receptors expressed in CHO cells
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Trial Name	REN-213
Trial Name	buprenorphine + naloxone,Suboxone
Novel drug target	Established target

Trial Name	COL-003, sustained release oxycodone
Novel drug target	Established target
Trial Name	PTI-801,Oxytrex

Specific Action of the Ligand	Biased agonist
Endogenous Drug?	False
Direct Interaction?	True

Mechanism of Interaction	Opioid receptors; mu/kappa/delta agonist
Direct Interaction	yes
Details of the Assay for Interaction	Radioligand binding assay

Trial Name	ALO-01, morphine sulfate and naltrexone hydrochloride,Embeda, Kadian NT
Novel drug target	Established target
Trial Name	intranasal morphine,Rylomine

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

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

4988	Entrez Gene Id
MU-TYPE OPIOID RECEPTOR	Uniprot Protein Name
ENSG00000112038	Ensembl Gene Id

OPRM1	Display Id
ENSG00000112038	Ensembl Gene Id
MU-TYPE OPIOID RECEPTOR (MOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35372]	Description

OPRM1 Gene Record

OPRM1 4988 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 16906017 11240090 11752352 15694871 19605407 10955836

Sources: TEND PharmGKB TdgClinicalTrial DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752352 17139284 17016423

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 20163389 6268422 11752352 19153939

Sources: DrugBank

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Mu opioid receptor partial agonist Trial Name -

PMIDs: 11702089 12513698 10958085 9399970 9972766 1361946

Sources: TEND TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality: partial agonist (activating) antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Details of the Assay for Interaction Competition binding assay- the calculated K<sub>i</sub> varies depending on the radioligand used.

PMIDs: 8819494 7723747 9016350 8968334 9862398

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8386327 18192961 8583364 11752352 10202212

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target Direct Interaction yes

PMIDs: 17909271 16597533 11755894 19086236 15882122 11752352

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 16580639 16682505 16530171 11752352 16580848

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Antagonist

PMIDs: 17487229 18354714 32020635 31961981 25715171 22515274 25760804 25410894 31206155 21946895 11752352 17661275 17918759 9673788 16960700 19068776

Sources: TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 15589524 16332149 16114980 19403616 11752352 16376082 16797997

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Full agonist

PMIDs: 24613457 18380425 20235611

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name ZX002, hydrocodone bitartrate Novel drug target Established target Trial Name PTI-701

PMIDs: 14600248 23703421 31170174 10640321 16291875 11752352 20665209 2849950 18606504

Sources: TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Agonist Endogenous Drug? False Direct Interaction? True

PMIDs: 17407276 9084061 18425947 18810678 10844102 19403853 16517095 15602503 9399970 8388112

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name oxymorphone hydrochloride, EN3202,Opana, Opana ER

PMIDs: 16343768 17595308 17006080 11752352 10854833 9712193

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 11561100 2471291 9360954 11752352 10911931

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17616524

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 25471070

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name TD-1211 Novel drug target Established target Direct Interaction yes

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16906017 11240090 11752352 15694871 19605407 10955836

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 17139284 17016423

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

agonist (activating)

PMIDs:
20163389 6268422 11752352 19153939

Sources:
DrugBank

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor partial agonist

Trial Name -

PMIDs:
11702089 12513698 10958085 9399970 9972766 1361946

Sources:
TEND TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Details of the Assay for Interaction Competition binding assay- the calculated K<sub>i</sub> varies depending on the radioligand used.

PMIDs:
8819494 7723747 9016350 8968334 9862398

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8386327 18192961 8583364 11752352 10202212

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Direct Interaction yes

PMIDs:
17909271 16597533 11755894 19086236 15882122 11752352

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
16580639 16682505 16530171 11752352 16580848

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
17487229 18354714 32020635 31961981 25715171 22515274 25760804 25410894 31206155 21946895 11752352 17661275 17918759 9673788 16960700 19068776

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
15589524 16332149 16114980 19403616 11752352 16376082 16797997

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
24613457 18380425 20235611

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name ZX002, hydrocodone bitartrate

Novel drug target Established target

Trial Name PTI-701

PMIDs:
14600248 23703421 31170174 10640321 16291875 11752352 20665209 2849950 18606504

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17407276 9084061 18425947 18810678 10844102 19403853 16517095 15602503 9399970 8388112

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name oxymorphone hydrochloride, EN3202,Opana, Opana ER

PMIDs:
16343768 17595308 17006080 11752352 10854833 9712193

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

agonist (activating)

PMIDs:
11561100 2471291 9360954 11752352 10911931

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
17616524

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
25471070

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name TD-1211

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
14744466 7957034 1656846 15028244 15001679

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
17139284 17016423 13651575

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
17004724

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

8156	HUGO Gene ID
8156	HUGO Gene Symbol
opioid receptor mu 1	HUGO Gene Name

OPRM1	DrugBank Gene Name
P35372	UniProt Accession
4988	Entrez Gene Id

MOR1	GENE_SYMBOL
OPRM1	GENE_SYMBOL
Mu-type opioid receptor	UNIPROT