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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
    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
    De Luca et al., 1993, Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action., Naunyn Schmiedebergs Arch. Pharmacol.
    Baker, 2007, Loperamide: a pharmacological review., Rev Gastroenterol Disord
    Coupar, 1995, The peristaltic reflex in the rat ileum: evidence for functional mu- and delta-opiate receptors., J. Pharm. Pharmacol.
    Corazziari, 1999, Role of opioid ligands in the irritable bowel syndrome., Can. J. Gastroenterol.
    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
    Christensen, 1993, The opioid receptor binding profiles of ketobemidone and morphine., Pharmacol. Toxicol.
    Kristensen et al., 1996, The mu1 and mu2 opioid receptor binding of ketobemidone, norketobemidone and 3-dimethylamino-1,1-diphenylbutene., Pharmacol. Toxicol.
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    Gassaway MM et al., 2014, The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist., Transl Psychiatry
    Samuels BA et al., 2017, The Behavioral Effects of the Antidepressant Tianeptine Require the Mu-Opioid Receptor., Neuropsychopharmacology
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    Walczak et al., 1981, Acetylmethadol metabolites influence opiate receptors and adenylate cyclase in amygdala., Eur. J. Pharmacol.
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    Kobayashi T et al., 1996, Effects of sigma ligands on the cloned mu-, delta- and kappa-opioid receptors co-expressed with G-protein-activated K+ (GIRK) channel in Xenopus oocytes., Br J Pharmacol
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    Kaneto H et al., 1990, The opioid receptor selectivity for trimebutine in isolated tissues experiments and receptor binding studies., J Pharmacobiodyn
  • 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 &mu; 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 &mu; 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:

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