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Names & Taxonomy

Uniprot ID:: P35372
Entry Name:: OPRM_HUMAN
Status:: reviewed
Protein Names:: Mu-type opioid receptor (M-OR-1) (MOR-1) (Mu opiate receptor) (Mu opioid receptor) (MOP) (hMOP)
Gene Names:: OPRM1 MOR1
Gene Names Primary:: OPRM1
Organism:: Homo sapiens (Human)

Structure

Length:: 400
Sequence:: MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCPPTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALATSTLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDFRTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFIFAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHIYVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNIEQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Proteomes:: UP000005640

Subcellular location

Subcellular Location:: Cell membrane

Function

Function:: Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors. The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extend to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15. They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B. Also couples to adenylate cyclase stimulatory G alpha proteins. The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4. Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization. Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction. The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins. The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation. Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling. Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling. Endogenous ligands induce rapid desensitization, endocytosis and recycling whereas morphine induces only low desensitization and endocytosis. Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties. Involved in neurogenesis. Isoform 12 couples to GNAS and is proposed to be involved in excitatory effects. Isoform 16 and isoform 17 do not bind agonists but may act through oligomerization with binding-competent OPRM1 isoforms and reduce their ligand binding activity.
Cross Reference Drug Bank:: DB00802 DB06274 DB00321 DB00913 DB00921 DB00611 DB00318 DB00514 DB00647 DB01209 DB01081 DB09272 DB01466 DB00813 DB01452 DB00956 DB00327 DB01221 DB06738 DB00504 DB01227 DB00854 DB00836 DB00333 DB01433 DB06800 DB00295 DB00844 DB09049 DB01183 DB00704 DB00904 DB00497 DB01192 DB00652 DB00454 DB00899 DB00708 DB06204 DB00193
Gene Ontology Go:: cell
dendrite cytoplasm
dendrite membrane
endoplasmic reticulum
focal adhesion
Golgi apparatus
integral component of plasma membrane
membrane raft
neuron projection
perikaryon
plasma membrane
postsynapse
sarcolemma
beta-endorphin receptor activity
G-protein alpha-subunit binding
G-protein beta-subunit binding
G-protein coupled receptor activity
morphine receptor activity
neuropeptide binding
voltage-gated calcium channel activity
acute inflammatory response to antigenic stimulus
adenylate cyclase-activating dopamine receptor signaling pathway
adenylate cyclase-inhibiting opioid receptor signaling pathway
behavioral response to ethanol
cellular response to morphine
cellular response to stress
eating behavior
estrous cycle
excitatory postsynaptic potential
G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
locomotory behavior
negative regulation of adenylate cyclase activity
negative regulation of cAMP-mediated signaling
negative regulation of cell proliferation
negative regulation of cytosolic calcium ion concentration
negative regulation of nitric oxide biosynthetic process
negative regulation of Wnt protein secretion
neuropeptide signaling pathway
phospholipase C-activating G-protein coupled receptor signaling pathway
positive regulation of appetite
positive regulation of cAMP-mediated signaling
positive regulation of cytosolic calcium ion concentration
positive regulation of ERK1 and ERK2 cascade
positive regulation of neurogenesis
positive regulation of nitric oxide biosynthetic process
regulation of N-methyl-D-aspartate selective glutamate receptor activity
regulation of sensory perception of pain
response to cocaine
response to food
response to growth factor
response to lipopolysaccharide
response to radiation
sensory perception
sensory perception of pain
wound healing
Gene Ontology Biological Process:: acute inflammatory response to antigenic stimulus
adenylate cyclase-activating dopamine receptor signaling pathway
adenylate cyclase-inhibiting opioid receptor signaling pathway
behavioral response to ethanol
cellular response to morphine
cellular response to stress
eating behavior
estrous cycle
excitatory postsynaptic potential
G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
locomotory behavior
negative regulation of adenylate cyclase activity
negative regulation of cAMP-mediated signaling
negative regulation of cell proliferation
negative regulation of cytosolic calcium ion concentration
negative regulation of nitric oxide biosynthetic process
negative regulation of Wnt protein secretion
neuropeptide signaling pathway
phospholipase C-activating G-protein coupled receptor signaling pathway
positive regulation of appetite
positive regulation of cAMP-mediated signaling
positive regulation of cytosolic calcium ion concentration
positive regulation of ERK1 and ERK2 cascade
positive regulation of neurogenesis
positive regulation of nitric oxide biosynthetic process
regulation of N-methyl-D-aspartate selective glutamate receptor activity
regulation of sensory perception of pain
response to cocaine
response to food
response to growth factor
response to lipopolysaccharide
response to radiation
sensory perception
sensory perception of pain
wound healing
Gene Ontology Molecular Function:: beta-endorphin receptor activity
G-protein alpha-subunit binding
G-protein beta-subunit binding
G-protein coupled receptor activity
morphine receptor activity
neuropeptide binding
voltage-gated calcium channel activity
Gene Ontology Cellular Component:: cell
dendrite cytoplasm
dendrite membrane
endoplasmic reticulum
focal adhesion
Golgi apparatus
integral component of plasma membrane
membrane raft
neuron projection
perikaryon
plasma membrane
postsynapse
sarcolemma
Keywords:: Alternative splicing
Cell membrane
Complete proteome
Cytoplasm
Disulfide bond
G-protein coupled receptor
Glycoprotein
Lipoprotein
Membrane
Palmitate
Phosphoprotein
Polymorphism
Receptor
Reference proteome
Transducer
Transmembrane
Transmembrane helix
Ubl conjugation
Interacts With:: Q9Y679; Q92905; Q8TEW6; P21333; P35212; P01210; Q96S59; Q8IUQ4; O43255; Q9P0L0; Q5T9L3; Q15942

Names & Taxonomy

Structure

Subcellular location

Function

Publication