DGIdb - OPRM1 Gene Record

OPRM1 4988 Druggable Genome

Alternate Names:

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

(9 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.
Duttaroy et al., 2000, In vivo regulation of mu-opioid receptor density and gene expression in CXBK and outbred Swiss Webster mice., Synapse
Patel et al., 2002, Opioid agonists differentially regulate mu-opioid receptors and trafficking proteins in vivo., Mol. Pharmacol.
Gomes et al., 2002, Mu-opioid receptor down-regulation and tolerance are not equally dependent upon G-protein signaling., Pharmacol. Biochem. Behav.
Stafford et al., mu-Opioid receptor downregulation contributes to opioid tolerance in vivo., Pharmacol. Biochem. Behav.
Melone et al., 2000, Etorphine increases the number of mu-opioid receptor-positive cells in the cerebral cortex., Neuroscience
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
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
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
Gilbert et al., 2004, Pharmacological characterization of dihydromorphine, 6-acetyldihydromorphine and dihydroheroin analgesia and their differentiation from morphine., 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.
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.
Leung
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

ALFENTANIL OPRM1

Interaction Score: 4.63

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: 3.6

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: 2.57

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: 2.32

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
LEVALLORPHAN OPRM1

Interaction Score: 2.06

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:
9016350 8968334 7723747 9862398 8819494

Sources:
TdgClinicalTrial TEND GuideToPharmacology
ALVIMOPAN OPRM1

Interaction Score: 1.71

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 GuideToPharmacology
TIANEPTINE OPRM1

Interaction Score: 1.54

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
28303899 25026323

Sources:
PharmGKB
NALTREXONE OPRM1

Interaction Score: 1.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

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

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB
HYDROCODONE OPRM1

Interaction Score: 1.34

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 GuideToPharmacology PharmGKB
DAMGO OPRM1

Interaction Score: 1.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
18380425 24613457 20235611

Sources:
DTC GuideToPharmacology
LEVORPHANOL OPRM1

Interaction Score: 1.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17039381 12975489

Sources:
TdgClinicalTrial TEND GuideToPharmacology
PENTAZOCINE OPRM1

Interaction Score: 1.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6094791 3419842 8042002 8968334 2286420

Sources:
TdgClinicalTrial TEND
ETORPHINE OPRM1

Interaction Score: 1.2

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
10881033 12435815 11900797 11420091 11752352 11098106

Sources:
GuideToPharmacology
PROPOXYPHENE OPRM1

Interaction Score: 1.16

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
NALBUPHINE OPRM1

Interaction Score: 1.11

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

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

Sources:
TdgClinicalTrial TEND GuideToPharmacology
CHEMBL255300 OPRM1

Interaction Score: 1.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17616524

Sources:
DTC
ELUXADOLINE OPRM1

Interaction Score: 1.03

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:
ChemblInteractions GuideToPharmacology
AXELOPRAN OPRM1

Interaction Score: 1.03

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
OXYMORPHONE OPRM1

Interaction Score: 1.03

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: 1.03

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: 1.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17004724

Sources:
DTC
BEVENOPRAN OPRM1

Interaction Score: 1.03

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
REMIFENTANIL OPRM1

Interaction Score: 0.93

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: 0.89

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 GuideToPharmacology PharmGKB
SUFENTANIL OPRM1

Interaction Score: 0.88

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
31773688 22153130 3014923 1688220 2847746 11299311 6131653 11752352

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB
BUTORPHANOL OPRM1

Interaction Score: 0.88

Interaction Types & Directionality:

agonist (activating)

partial antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
12127012 9399970 10381785 12470863 8968334 17909753 7705457 15942128 8746803

Sources:
TdgClinicalTrial TEND GuideToPharmacology
ENDOMORPHIN-1 OPRM1

Interaction Score: 0.77

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
HYDROMORPHONE OPRM1

Interaction Score: 0.72

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
11305075 12479250 18789923 11869661

Sources:
TdgClinicalTrial TEND GuideToPharmacology
NABIXIMOLS OPRM1

Interaction Score: 0.69

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31246565 11840318 26264914

Sources:
PharmGKB
DIHYDROMORPHINE OPRM1

Interaction Score: 0.69

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
15178355 16777416 19474215

Sources:
GuideToPharmacology
BUPRENORPHINE OPRM1

Interaction Score: 0.62

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Partial agonist

PMIDs:
11275413 10729371 15100703 10942856 11752352 12435410 30549211

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB
CODEINE OPRM1

Interaction Score: 0.58

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:
15509185 17620111 8306082 11752352 25752520

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB
OXYCODONE OPRM1

Interaction Score: 0.57

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
DIACETYLMORPHINE OPRM1

Interaction Score: 0.55

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: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17616524

Sources:
DTC
DIFENOXIN HYDROCHLORIDE OPRM1

Interaction Score: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEVOMETHADYL ACETATE HYDROCHLORIDE OPRM1

Interaction Score: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name NKTR-181

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

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology

NALTALIMIDE OPRM1

Interaction Score: 0.51

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: 0.51

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Mu opioid receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions

METHYLNALTREXONE OPRM1

Interaction Score: 0.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
17504835

Sources:
TdgClinicalTrial GuideToPharmacology

METHADONE HYDROCHLORIDE OPRM1

Interaction Score: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

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: 0.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
CHEMBL570176 OPRM1

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19892550

Sources:
DTC
CHEMBL409225 OPRM1

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21978284

Sources:
DTC
LEVORPHANOL TARTRATE OPRM1

Interaction Score: 0.51

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: 0.51

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LOPERAMIDE OPRM1

Interaction Score: 0.46

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Action of the Ligand Agonist

PMIDs:
10087042 18284554 6319884 11752352 14592702 8488368

Sources:
TdgClinicalTrial TEND GuideToPharmacology
TRAMADOL OPRM1

Interaction Score: 0.43

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

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

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB
TAPENTADOL OPRM1

Interaction Score: 0.41

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
10592235

Sources:
TdgClinicalTrial TEND GuideToPharmacology
DIPRENORPHINE OPRM1

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
20641600

Sources:
GuideToPharmacology
Z160 OPRM1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19815411

Sources:
DTC
NALMEFENE OPRM1

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
SAMIDORPHAN OPRM1

Interaction Score: 0.34

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:
ChemblInteractions GuideToPharmacology
MARAVIROC OPRM1

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ANILERIDINE HYDROCHLORIDE OPRM1

Interaction Score: 0.26

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: 0.26

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: 0.26

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: 0.26

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: 0.26

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: 0.26

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:
ChemblInteractions GuideToPharmacology
LEVALLORPHAN TARTRATE OPRM1

Interaction Score: 0.26

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: 0.22

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
15589524 16376082 16332149 16114980 19403616 16797997 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
MORPHINE OPRM1

Interaction Score: 0.2

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 GuideToPharmacology
METHADONE OPRM1

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
14991152 11933204 17016423 17139284 17850768 19717013 12405865

Sources:
TdgClinicalTrial TEND GuideToPharmacology
CODEINE SULFATE OPRM1

Interaction Score: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEPERIDINE OPRM1

Interaction Score: 0.17

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
11585443

Sources:
GuideToPharmacology
NALTRINDOLE OPRM1

Interaction Score: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

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: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
NALOXONE 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
ETONITAZENE 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
SUFENTANIL CITRATE 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
NALTRIBEN 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
NORBINALTORPHIMINE 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
COTININE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23223006

Sources:
PharmGKB
COCAINE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31246565 16387451 11840318

Sources:
PharmGKB
NICOTINE OPRM1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31246565 23223006 22260295 17224915 16960700 16387451 15007373 11840318

Sources:
PharmGKB
SUMATRIPTAN OPRM1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25096645

Sources:
PharmGKB
METHAMPHETAMINE OPRM1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16402083

Sources:
PharmGKB
AMPHETAMINE OPRM1

Interaction Score: 0.03

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
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

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:
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:
GO: OPRM1
- Version: 01-May-2021
Alternate Names:

MOR1 GO Gene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
Pharos: OPRM1
- Version: 01-May-2021
Alternate Names:

Mu-type opioid receptor Gene Name

P35372 UniProt ID

Gene Info:

Gene Categories:

KINASE, G PROTEIN COUPLED RECEPTOR

Publications:

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

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

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

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

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

Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

Mechanism of Interaction	Mu opioid receptor agonist
Direct Interaction	yes
Specific Action of the Ligand	Agonist

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

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

Trial Name	remifentanil,Ultiva
Novel drug target	Established target

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

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

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

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

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

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

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

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

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

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

OPRM1 Gene Record

OPRM1 4988 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 19605407 16906017 15694871 10955836 11752352 11240090

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 10202212 8386327 8583364 18192961 11752352

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 11752352

Sources: TdgClinicalTrial TEND

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

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: 9016350 8968334 7723747 9862398 8819494

Sources: TdgClinicalTrial TEND GuideToPharmacology

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 GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 28303899 25026323

Sources: PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

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

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

Sources: TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB

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 GuideToPharmacology PharmGKB

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 18380425 24613457 20235611

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 17039381 12975489

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 6094791 3419842 8042002 8968334 2286420

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10881033 12435815 11900797 11420091 11752352 11098106

Sources: GuideToPharmacology

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

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

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

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

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17616524

Sources: DTC

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: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: agonist (activating)

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

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

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
10202212 8386327 8583364 18192961 11752352

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND

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

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:
9016350 8968334 7723747 9862398 8819494

Sources:
TdgClinicalTrial TEND GuideToPharmacology

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 GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

PMIDs:
28303899 25026323

Sources:
PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

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

Sources:
TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB

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 GuideToPharmacology PharmGKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Full agonist

PMIDs:
18380425 24613457 20235611

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
17039381 12975489

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6094791 3419842 8042002 8968334 2286420

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Full agonist

Endogenous Drug? False

PMIDs:
10881033 12435815 11900797 11420091 11752352 11098106

Sources:
GuideToPharmacology

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

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

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

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
17616524

Sources:
DTC

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:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name TD-1211

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name oxymorphone hydrochloride, EN3202,Opana, Opana ER

PMIDs:
17006080 17595308 16343768 11752352 10854833 9712193

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Mu opioid receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
17004724

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

MOR1	GENE_SYMBOL
OPRM1	GENE_SYMBOL
Mu-type opioid receptor	UNIPROT