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FLASH GENE
Symbol OPRM1 contributors: mct/npt - updated : 12-10-2015
HGNC name opioid receptor, mu 1
HGNC id 8156
PROTEIN
PHYSICAL PROPERTIES
STRUCTURE
motifs/domains
  • seven transmembrane segments (7TM) receptor
    • HOMOLOGY
    interspecies homolog to murine Oprm
    Homologene
    FAMILY
  • G-protein coupled receptor 1 family
    • CATEGORY receptor membrane G
    SUBCELLULAR LOCALIZATION     intracellular
    intracellular,cytoplasm,organelle,membrane
    intracellular,cytoplasm,organelle,endoplasmic reticulum
    intracellular,cytoplasm,organelle,Golgi
    basic FUNCTION
  • principal sites of action of several endogenous opioid peptides, also major target for opioid analgesic agents and heroin
  • playing an important role in mediating the actions of morphine and morphine-like drugs
  • OPRM1 is more dependent on cholesterol for efficient signaling than OPRD1 which can be partly explained by localization of OPRM- but not OPRD receptors in cholesterol- and caveolin-enriched membrane domains
  • depressing cAMP levels, opening a G protein-modulated K+ channel and a third spliced variant acting as a morphine-6 beta-glucuronide receptor
  • both OPRD1 and OPRM1 agonists reduce depolarization-induced Ca(2+) currents in single small dorsal root ganglia neurons and inhibit afferent C-fiber synaptic transmission in the dorsal spinal cord
  • is the G-protein coupled receptor primarily responsible for mediating the analgesic and rewarding properties of opioid agonist drugs such as morphine, fentanyl, and heroin
    • CELLULAR PROCESS
    PHYSIOLOGICAL PROCESS
    PATHWAY
    metabolism
    signaling
    a component
  • form heteromers with OPRM1 and negatively regulate OPRM1-mediated spinal analgesia
    • INTERACTION
    DNA
    RNA
    small molecule
    protein
  • REST (by NRSE element)
  • interacting with HINT1 and RGS20 for modulation of its signaling)
  • at the cellular level, PPP1R9B associates with OPRM1 in striatum and modulates OPRM1 signaling and endocytosis
  • interacting with RGS4 (acts as a GTPase accelerating protein to modulate OPRM1 and OPRD1 signaling)
  • PCBP1 is an expressional regulator of the mu-opioid receptor (OPRM1) gene
  • activation of OPRM1 leads to internalization of a cold-sensor TRPM8, which can be reversed by a follow-up treatment with the inverse OPRM1 agonist naloxone
    • cell & other
  • principle molecular target of opioid analgesics (
    • REGULATION
    activated by endomorphism 1 and 2
    ASSOCIATED DISORDERS
    corresponding disease(s)
    Susceptibility
  • heroin/cocaine dependence
  • to idiopathic generalized epilepsy or absence epilepsy
  • to drug and alcohol dependence
    • Variant & Polymorphism other
  • G118 allele increases the risk of idiopathic generalized epilepsy
  • SNP increasing the risk of drug and alcohol dependence
  • polymorphisms that may explain the variability seen in the clinical response to opiates, both from an analgesic and polymorphisms in OPRM1 that may explain the variability seen in the clinical response to opiates, both from an analgesic and alcohol and substance use disorders (ASUD) stand-point (Ravindranathana 2009)
    • Candidate gene
    Marker
    Therapy target
    SystemTypeDisorderPubmed
    miscelleaneouspain 
    dissociation of OPRM1 from OPRD1 in the cell membrane is a potential strategy to improve opioid analgesic therapies
    ANIMAL & CELL MODELS
  • Mor-1 KO mice with a disruption of exon 1 are unresponsive to morphine