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OPRM1 Gene Record

  • Summary
  • Interactions
  • Claims
  • 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
    MU-TYPE OPIOID RECEPTOR (MOR-1). [SOURCE:UNIPROT/SWISSPROT;ACC:P35372]
    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
    Gene Biotype PROTEIN_CODING
    (8 More Sources)

    Gene Categories: Category Details

    KINASE
    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Picker, 1997, Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists., J. Pharmacol. Exp. Ther.
    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
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Codd et al., 1995, Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception., J. Pharmacol. Exp. Ther.
    Tyers, 1980, A classification of opiate receptors that mediate antinociception in animals., Br. J. Pharmacol.
    Ulens et al., 1999, Norpropoxyphene-induced cardiotoxicity is associated with changes in ion-selectivity and gating of HERG currents., Cardiovasc. Res.
    Kato, 2008, [Pharmacological effects of a mu-opioid receptor antagonist naltrexone on alcohol dependence]., Nihon Arukoru Yakubutsu Igakkai Zasshi
    Herz, 1998, Opioid reward mechanisms: a key role in drug abuse?, Can. J. Physiol. Pharmacol.
    Goodman et al., 2007, Mu opioid receptor antagonists: recent developments., ChemMedChem
    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
    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
    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
    Roche DJO et al., 2019, Lack of Association between Opioid-Receptor Genotypes and Smoking Cessation Outcomes in a Randomized, Controlled Naltrexone Trial., Alcohol Alcohol
    Oslin DW et al., 2015, Naltrexone vs Placebo for the Treatment of Alcohol Dependence: A Randomized Clinical Trial., JAMA Psychiatry
    Foulds JA et al., 2015, OPRM1 genotype and naltrexone response in depressed alcohol-dependent patients., Pharmacogenet Genomics
    Jonas DE et al., 2014, Genetic polymorphisms and response to medications for alcohol use disorders: a systematic review and meta-analysis., Pharmacogenomics
    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
    Coller JK et al., 2011, OPRM1 A118G genotype fails to predict the effectiveness of naltrexone treatment for alcohol dependence., Pharmacogenet Genomics
    Ray R et al., 2006, Association of OPRM1 A118G variant with the relative reinforcing value of nicotine., Psychopharmacology (Berl)
    McWhinney-Glass S et al., 2013, Cumulative genetic risk predicts platinum/taxane-induced neurotoxicity., Clin Cancer Res
    Muriel J et al., 2019, Pharmacogenetics and prediction of adverse events in prescription opioid use disorder patients., Basic Clin Pharmacol Toxicol
    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
    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.
    Frink et al., 1996, Influence of tramadol on neurotransmitter systems of the rat brain., Arzneimittelforschung
    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.
    Minami et al., 2007, Pharmacological aspects of the effects of tramadol on G-protein coupled receptors., J. Pharmacol. Sci.
    Gillen et al., 2000, Affinity, potency and efficacy of tramadol and its metabolites at the cloned human mu-opioid receptor., Naunyn Schmiedebergs Arch. Pharmacol.
    Ide et al., 2006, Mu opioid receptor-dependent and independent components in effects of tramadol., Neuropharmacology
    Barakat A, 2019, Revisiting Tramadol: A Multi-Modal Agent for Pain Management., CNS Drugs
    DeHaven-Hudkins et al., 1999, Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity., J. Pharmacol. Exp. Ther.
    di Bosco et al., 2008, Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors., Chem Biol Drug Des
    Giagnoni et al., 1983, Loperamide: evidence of interaction with mu and delta opioid receptors., Life Sci.
    Tan-No et al., 2003, Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice., Eur J Pharm Sci
    Roge et al., 1993, The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide., Scand. J. Gastroenterol.
    Guy et al., 1997, Comparison of remifentanil and fentanyl in patients undergoing craniotomy for supratentorial space-occupying lesions., Anesthesiology
    Scott et al., 2005, Spotlight on remifentanil for general anaesthesia., CNS Drugs
    Scott et al., 2005, Remifentanil: a review of its use during the induction and maintenance of general anaesthesia., Drugs
    Patel et al., 1996, Remifentanil., Drugs
    Warner et al., 1996, Intracranial pressure and hemodynamic effects of remifentanil versus alfentanil in patients undergoing supratentorial craniotomy., Anesth. Analg.
    Hoke et al., 1997, Comparative pharmacokinetics and pharmacodynamics of remifentanil, its principle metabolite (GR90291) and alfentanil in dogs., J. Pharmacol. Exp. Ther.
    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.
    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.
    Jacobs et al., 1992, Opioid receptor affinity for agonist-antagonist analgesics., J Am Podiatr Med Assoc
    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
    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.
    Meerpohl et al., 2008, [News from the cochrane library: mu opioid antagonists for opioid-induced bowel dysfunction]., Z Gastroenterol
    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
    McNicol et al., 2008, Mu-opioid antagonists for opioid-induced bowel dysfunction., Cochrane Database Syst Rev
    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.)
    Kishioka et al., 2000, Diltiazem enhances the analgesic but not the respiratory depressant effects of morphine in rhesus monkeys., Eur. J. Pharmacol.
    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
    Pu J et al., 2019, Correlation between gene polymorphism and opioid efficacy in patients with gastric or intestinal cancer., Eur Rev Med Pharmacol Sci
    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
    Naito T et al., 2011, CYP3A5*3 affects plasma disposition of noroxycodone and dose escalation in cancer patients receiving oxycodone., J Clin Pharmacol
    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
    Dietis et al., 2009, Simultaneous targeting of multiple opioid receptors: a strategy to improve side-effect profile., Br J Anaesth
    Zhang S et al., 2009, A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors., Bioorg Med Chem Lett
    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.)
    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.
    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.
    Dosen-Micovic et al., 2006, Steric interactions and the activity of fentanyl analogs at the mu-opioid receptor., Bioorg. Med. Chem.
    Hajiha et al., 2009, Opioid receptor mechanisms at the hypoglossal motor pool and effects on tongue muscle activity in vivo., J. Physiol. (Lond.)
    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.
    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.
    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.
    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.)
    Emmerson et al., 1996, Characterization of opioid agonist efficacy in a C6 glioma cell line expressing the mu opioid receptor., J. Pharmacol. Exp. Ther.
    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
    Kamei et al., 1994, Effects of diabetes on the antinociceptive effect of (+/-)pentazocine in mice., Res. Commun. Chem. Pathol. Pharmacol.
    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.
    Kvam et al., 2004, Genetic analysis of the murine mu opioid receptor: increased complexity of Oprm gene splicing., J. Mol. Med.
    Shi et al., 2002, Sequence variations in the mu-opioid receptor gene (OPRM1) associated with human addiction to heroin., Hum. Mutat.
    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
    Kakko et al., 2008, Mood and neuroendocrine response to a chemical stressor, metyrapone, in buprenorphine-maintained heroin dependence., Biol. Psychiatry
    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.
    Eap CB et al., 2002, Interindividual variability of the clinical pharmacokinetics of methadone: implications for the treatment of opioid dependence., Clin Pharmacokinet
    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
    Sánchez-Blázquez et al., 2001, Agonists determine the pattern of G-protein activation in mu-opioid receptor-mediated supraspinal analgesia., Brain Res. Bull.
    Kishioka et al., 2000, Buprenorphine and methoclocinnamox: agonist and antagonist effects on respiratory function in rhesus monkeys., Eur. J. Pharmacol.
    Ide et al., 2004, Buprenorphine antinociception is abolished, but naloxone-sensitive reward is retained, in mu-opioid receptor knockout mice., Neuropsychopharmacology
    Zubieta et al., 2000, Buprenorphine-induced changes in mu-opioid receptor availability in male heroin-dependent volunteers: a preliminary study., Neuropsychopharmacology
    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
    Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
    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., 2007, Population-specific effects of the Asn40Asp polymorphism at the mu-opioid receptor gene (OPRM1) on HPA-axis activation., Pharmacogenet Genomics
    Chong RY et al., 2006, The mu-opioid receptor polymorphism A118G predicts cortisol responses to naloxone and stress., Neuropsychopharmacology
    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
    Wand GS et al., 2002, The mu-opioid receptor gene polymorphism (A118G) alters HPA axis activation induced by opioid receptor blockade., Neuropsychopharmacology
    Freye et al., 1998, [The opioid tramadol demonstrates excitatory properties of non-opioid character--a preclinical study using alfentanil as a comparison]., Schmerz
    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.
    Spetea et al., 2003, Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist., Eur. J. Neurosci.
    Marek, 2003, Behavioral evidence for mu-opioid and 5-HT2A receptor interactions., Eur. J. Pharmacol.
    Neal et al., 2003, Binding and GTPgammaS autoradiographic analysis of preproorphanin precursor peptide products at the ORL1 and opioid receptors., J. Chem. Neuroanat.
    van Dorp et al., 2007, Naloxone treatment in opioid addiction: the risks and benefits., Expert Opin Drug Saf
    Prommer, 2007, Levorphanol: the forgotten opioid., Support Care Cancer
    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.
    Hennies et al., 1988, Receptor binding, analgesic and antitussive potency of tramadol and other selected opioids., Arzneimittelforschung
    Stoops et al., 2010, Intravenous oxycodone, hydrocodone, and morphine in recreational opioid users: abuse potential and relative potencies., Psychopharmacology (Berl.)
    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.
    Walsh et al., 2008, The relative abuse liability of oral oxycodone, hydrocodone and hydromorphone assessed in prescription opioid abusers., Drug Alcohol Depend
    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.
    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
    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
    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
    Lötsch et al., 2005, Are mu-opioid receptor polymorphisms important for clinical opioid therapy?, Trends Mol Med
    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.
    Leung et al., 2001, Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain., Pain
    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
    Chamberlin et al., 2007, Oral oxymorphone for pain management., Ann Pharmacother
    Gardell et al., 2006, Opioid receptor-mediated hyperalgesia and antinociceptive tolerance induced by sustained opiate delivery., Neurosci. Lett.
    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
    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.
    Baber M et al., 2015, The pharmacogenetics of codeine pain relief in the postpartum period., Pharmacogenomics J
    Neary et al., 2005, Alvimopan., Expert Opin Investig Drugs
    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.
    Schmidt, 2001, Alvimopan* (ADL 8-2698) is a novel peripheral opioid antagonist., Am. J. Surg.
    Saufl et al., 2006, Nurses are everywhere: a practical perspective on the surgical team in managing postoperative ileus., J. Perianesth. Nurs.
    Kraft, 2007, Emerging pharmacologic options for treating postoperative ileus., Am J Health Syst Pharm
    Yuan, 2007, Methylnaltrexone mechanisms of action and effects on opioid bowel dysfunction and other opioid adverse effects., Ann Pharmacother
    Zamponi GW et al., 2009, Scaffold-based design and synthesis of potent N-type calcium channel blockers., Bioorg Med Chem Lett
    Sarhill et al., 2001, Hydromorphone: pharmacology and clinical applications in cancer patients., Support Care Cancer
    Inturrisi, Clinical pharmacology of opioids for pain., Clin J Pain
    Kumar et al., 2008, Hydromorphone efficacy and treatment protocol impact on tolerance and mu-opioid receptor regulation., Eur. J. Pharmacol.
    Quigley, 2002, Hydromorphone for acute and chronic pain., Cochrane Database Syst Rev
    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
    Türkan H et al., 2019, The association between the OPRM1 A118G polymorphism and addiction in a Turkish population., Arh Hig Rada Toksikol
    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
    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
    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
    Haerian BS et al., 2013, OPRM1 rs1799971 polymorphism and opioid dependence: evidence from a meta-analysis., Pharmacogenomics
    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
    Tan EC et al., 2003, Mu opioid receptor gene polymorphisms and heroin dependence in Asian populations., Neuroreport
    Franke P et al., 2001, Nonreplication of association between mu-opioid-receptor gene (OPRM1) A118G polymorphism and substance dependence., Am J Med Genet
    Szeto CY et al., 2001, Association between mu opioid receptor gene polymorphisms and Chinese heroin addicts., Neuroreport
    Antonilli et al., 2005, Effect of repeated administrations of heroin, naltrexone, methadone, and alcohol on morphine glucuronidation in the rat., Psychopharmacology (Berl.)
    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.
    Greenwald et al., 2003, Effects of buprenorphine maintenance dose on mu-opioid receptor availability, plasma concentrations, and antagonist blockade in heroin-dependent volunteers., Neuropsychopharmacology
    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.
    Becker et al., 2004, MOR1 receptor mRNA expression in human brains of drug-related fatalities-a real-time PCR quantification., Forensic Sci. Int.
    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
    Colpaert et al., 1986, Epidural and intravenous sufentanil in the rat: analgesia, opiate receptor binding, and drug concentrations in plasma and brain., Anesthesiology
    Levron, 1991, [Pharmacokinetics and pharmacodynamics of morphinomimetics in the central nervous system]., Agressologie
    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.
    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.
    Leysen et al., 1982, In vitro binding properties of 3H-sufentanil, a superior ligand for the mu-opiate receptor., Arch Int Pharmacodyn Ther
    Tidgewell K et al., 2008, Herkinorin analogues with differential beta-arrestin-2 interactions., J Med Chem
    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
    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
    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.
    Johnson et al., 2006, Agonist-selective mechanisms of mu-opioid receptor desensitization in human embryonic kidney 293 cells., Mol. Pharmacol.
    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
    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
    Munafò MR et al., 2007, Association of the mu-opioid receptor gene with smoking cessation., Pharmacogenomics J
    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
    Corazziari, 1999, Role of opioid ligands in the irritable bowel syndrome., Can. J. Gastroenterol.
    De Luca et al., 1993, Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action., Naunyn Schmiedebergs Arch. Pharmacol.
    Coupar, 1995, The peristaltic reflex in the rat ileum: evidence for functional mu- and delta-opiate receptors., J. Pharm. Pharmacol.
    Baker, 2007, Loperamide: a pharmacological review., Rev Gastroenterol Disord
    Fujita et al., 2014, Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers., Biochem. Pharmacol.
    Dove et al., 2013, Eluxadoline benefits patients with irritable bowel syndrome with diarrhea in a phase 2 study., Gastroenterology
    Ide S et al., 2006, Linkage disequilibrium and association with methamphetamine dependence/psychosis of mu-opioid receptor gene polymorphisms., Pharmacogenomics J
    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
    Ibeas Bih C et al., 2015, Molecular Targets of Cannabidiol in Neurological Disorders., Neurotherapeutics
    Samuels BA et al., 2017, The Behavioral Effects of the Antidepressant Tianeptine Require the Mu-Opioid Receptor., Neuropsychopharmacology
    Gassaway MM et al., 2014, The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist., Transl Psychiatry
  • ALVIMOPAN   OPRM1

    Interaction Score: 5.35

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    15882122 19086236 11755894 16597533 11752352 17909271


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • ALFENTANIL   OPRM1

    Interaction Score: 5.35

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    19605407 16906017 15694871 10955836 11752352 11240090


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • DIPHENOXYLATE   OPRM1

    Interaction Score: 4.16

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10202212 8386327 8583364 18192961 11752352


    Sources:
    TdgClinicalTrial TEND

  • ANILERIDINE   OPRM1

    Interaction Score: 2.97

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    17016423 17139284 11752352


    Sources:
    TdgClinicalTrial TEND

  • DEZOCINE   OPRM1

    Interaction Score: 2.68

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

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

    PMIDs:
    9399970 10958085 9972766 11702089 12513698 1361946


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • DAMGO   OPRM1

    Interaction Score: 2.38

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    18380425 24613457 20235611


    Sources:
    DTC

  • LEVORPHANOL   OPRM1

    Interaction Score: 2.38

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    17039381 12975489


    Sources:
    TdgClinicalTrial TEND

  • LEVALLORPHAN   OPRM1

    Interaction Score: 2.08

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

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    9016350 8968334 7723747 9862398 8819494


    Sources:
    TdgClinicalTrial TEND

  • TIANEPTINE   OPRM1

    Interaction Score: 1.78

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    28303899 25026323


    Sources:
    PharmGKB

  • NALTREXONE   OPRM1

    Interaction Score: 1.49

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

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


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • HYDROCODONE   OPRM1

    Interaction Score: 1.43

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    2849950 20665209 14600248 11752352 18606504 10640321 16291875 23703421 31170174


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • PENTAZOCINE   OPRM1

    Interaction Score: 1.39

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    6094791 3419842 8042002 8968334 2286420


    Sources:
    TdgClinicalTrial TEND

  • PROPOXYPHENE   OPRM1

    Interaction Score: 1.34

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9399970 10379623 19604717 11752352 7562497 6249436 10690289


    Sources:
    TdgClinicalTrial TEND

  • CHEMBL255300   OPRM1

    Interaction Score: 1.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17616524


    Sources:
    DTC

  • ENDOMORPHIN-1   OPRM1

    Interaction Score: 1.19

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    22724433


    Sources:
    DTC

  • AXELOPRAN   OPRM1

    Interaction Score: 1.19

    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

  • METHYLNALTREXONE   OPRM1

    Interaction Score: 1.19

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Methylnaltrexone
    Novel drug target Established target

    PMIDs:
    17504835


    Sources:
    TdgClinicalTrial

  • OXYMORPHONE   OPRM1

    Interaction Score: 1.19

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    17006080 17595308 16343768 11752352 10854833 9712193


    Sources:
    TdgClinicalTrial TEND

  • ALFENTANIL HYDROCHLORIDE   OPRM1

    Interaction Score: 1.19

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    DTC ChemblInteractions

  • CLOCINNAMOX   OPRM1

    Interaction Score: 1.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17004724


    Sources:
    DTC

  • BEVENOPRAN   OPRM1

    Interaction Score: 1.19

    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

  • NALBUPHINE   OPRM1

    Interaction Score: 1.19

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

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

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


    Sources:
    TdgClinicalTrial TEND

  • REMIFENTANIL   OPRM1

    Interaction Score: 1.07

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name remifentanil,Ultiva
    Novel drug target Established target

    PMIDs:
    9066316 16332149 16114980 8875131 11752352 8694317 9103501


    Sources:
    TdgClinicalTrial TEND

  • NALOXONE   OPRM1

    Interaction Score: 0.97

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

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


    Sources:
    DTC TdgClinicalTrial TEND PharmGKB

  • SUFENTANIL   OPRM1

    Interaction Score: 0.93

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name ARX-01, sufentanil NanoTab
    Novel drug target Established target
    Trial Name ARX-03, sufentanil + triazolam NanoTab

    PMIDs:
    31773688 22153130 3014923 1688220 2847746 11299311 6131653 11752352


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • BUTORPHANOL   OPRM1

    Interaction Score: 0.93

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

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    12127012 9399970 10381785 12470863 8968334 17909753 7705457 15942128 8746803


    Sources:
    TdgClinicalTrial TEND

  • ELUXADOLINE   OPRM1

    Interaction Score: 0.89

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    25261794 23583433


    Sources:
    ChemblInteractions

  • NABIXIMOLS   OPRM1

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31246565 11840318 26264914


    Sources:
    PharmGKB

  • HYDROMORPHONE   OPRM1

    Interaction Score: 0.71

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name NMED-1077,Exalgo, Jurnista, Dilaudid
    Novel drug target Established target

    PMIDs:
    11305075 12479250 18789923 11869661


    Sources:
    TdgClinicalTrial TEND

  • OXYCODONE   OPRM1

    Interaction Score: 0.66

    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:
    31773688 25239082 21209234 17525040 18039433 19474215


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • BUPRENORPHINE   OPRM1

    Interaction Score: 0.65

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

    Interaction Info:
    Trial Name V1003
    Trial Name CAM2038
    Trial Name Butrans is a transdermal patch formulation of buprenorphine, a partial agonist at mu opioid receptors and an antagonist at kappa opioid receptors. It is indicated as an analgesic to deliver continuous pain relief for seven days. The efficacy of Butrans

    PMIDs:
    11275413 10729371 15100703 10942856 11752352 12435410 30549211


    Sources:
    TdgClinicalTrial ChemblInteractions TEND PharmGKB

  • DIACETYLMORPHINE   OPRM1

    Interaction Score: 0.64

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

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


    Sources:
    PharmGKB

  • CHEMBL13786   OPRM1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17616524


    Sources:
    DTC

  • DIFENOXIN HYDROCHLORIDE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • FENTANYL CITRATE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • LEVOMETHADYL ACETATE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    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: 0.59

    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: 0.59

    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: 0.59

    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: 0.59

    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: 0.59

    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: 0.59

    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: 0.59

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Mu opioid receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • MORPHINE SULFATE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name NKTR-181

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • NALTALIMIDE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    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: 0.59

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CODEINE   OPRM1

    Interaction Score: 0.59

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

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    15509185 17620111 8306082 11752352 25752520


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • FRAKEFAMIDE   OPRM1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NALOXEGOL OXALATE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    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: 0.59

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Mu opioid receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL570176   OPRM1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19892550


    Sources:
    DTC

  • CHEMBL409225   OPRM1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21978284


    Sources:
    DTC

  • LEVORPHANOL TARTRATE   OPRM1

    Interaction Score: 0.59

    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: 0.59

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SAMIDORPHAN   OPRM1

    Interaction Score: 0.59

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Mu opioid receptor antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LOPERAMIDE   OPRM1

    Interaction Score: 0.48

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    10087042 18284554 6319884 11752352 14592702 8488368


    Sources:
    TdgClinicalTrial TEND

  • TRAMADOL   OPRM1

    Interaction Score: 0.46

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name tramadol,Tridural, Ryzolt
    Trial Name tramadol hydrochloride,Ultram
    Trial Name tramadol extended-release,Raliva ER

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


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • Z160   OPRM1

    Interaction Score: 0.4

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19815411


    Sources:
    DTC

  • TAPENTADOL   OPRM1

    Interaction Score: 0.36

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name tapentadol
    Novel drug target Established target
    Trial Name tapentadol hydrochloride, CG-5503, R331333

    PMIDs:
    10592235


    Sources:
    TdgClinicalTrial TEND

  • MARAVIROC   OPRM1

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ANILERIDINE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.3

    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: 0.3

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BUTORPHANOL TARTRATE   OPRM1

    Interaction Score: 0.3

    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: 0.3

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • LEVALLORPHAN TARTRATE   OPRM1

    Interaction Score: 0.3

    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: 0.24

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name AD 923
    Novel drug target Established target
    Trial Name AeroLEF

    PMIDs:
    15589524 16376082 16332149 16114980 19403616 16797997 11752352


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • MORPHINE   OPRM1

    Interaction Score: 0.21

    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 18193048 18380425 16580639 16530171 16580848 16682505 11752352


    Sources:
    DTC TdgClinicalTrial TEND

  • CODEINE SULFATE   OPRM1

    Interaction Score: 0.2

    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: 0.2

    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: 0.2

    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: 0.2

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NALBUPHINE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.2

    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 POLISTIREX   OPRM1

    Interaction Score: 0.2

    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: 0.2

    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: 0.2

    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: 0.2

    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: 0.2

    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: 0.2

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BENZHYDROCODONE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.2

    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: 0.2

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NALMEFENE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NALMEFENE   OPRM1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name nalmefene, CPH-101

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • DIPHENOXYLATE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.2

    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: 0.2

    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: 0.19

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    14991152 11933204 17016423 17139284 17850768 19717013 12405865


    Sources:
    TdgClinicalTrial TEND

  • NALOXONE HYDROCHLORIDE   OPRM1

    Interaction Score: 0.15

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SUFENTANIL CITRATE   OPRM1

    Interaction Score: 0.15

    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: 0.15

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • COTININE   OPRM1

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23223006


    Sources:
    PharmGKB

  • COCAINE   OPRM1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31246565 16387451 11840318


    Sources:
    PharmGKB

  • NICOTINE   OPRM1

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    31246565 23223006 22260295 17224915 16960700 16387451 15007373 11840318


    Sources:
    PharmGKB

  • SUMATRIPTAN   OPRM1

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25096645


    Sources:
    PharmGKB

  • METHAMPHETAMINE   OPRM1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16402083


    Sources:
    PharmGKB

  • AMPHETAMINE   OPRM1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ACETAMINOPHEN   OPRM1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21837673


    Sources:
    PharmGKB

  • DOCETAXEL   OPRM1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23963862


    Sources:
    PharmGKB

  • CARBOPLATIN   OPRM1

    Interaction Score: 0.02

    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:

  • 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

  • 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:

  • GO: OPRM1

    • Version: 01-February-2022

    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:

  • Pharos: OPRM1

    • Version: 01-February-2022

    Alternate Names:
    Mu-type opioid receptor Gene Name
    P35372 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE, G PROTEIN COUPLED RECEPTOR

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21