OPRM1 Gene: Opioid Receptor Mu 1

Key mediator of opioid analgesia and addiction; genetic variants influence pain sensitivity and opioid response.

Gene Information Card

Symbol OPRM1
Full Name Opioid Receptor Mu 1
Gene Type protein-coding
Chromosomal Location 6q25.2
NCBI Gene ID 4988 ncbi.nlm.nih.gov/gene/4988
Ensembl ID ENSG00000112038
UniProt ID P35372
OMIM ID 600018
HGNC ID 8156
Aliases MOR1, OPRM, MOR, KIAA0403, M-OR-1

Description

The OPRM1 gene encodes the mu-opioid receptor, a G protein-coupled receptor that is the primary target for endogenous opioid peptides (e.g., beta-endorphin, enkephalins) and clinically used opioids (e.g., morphine, fentanyl). It mediates analgesia, reward, and addiction. Genetic variants, particularly the A118G (rs1799971) polymorphism, have been associated with altered receptor function, pain sensitivity, and differential responses to opioid therapy.

Disease Associations

Disease category Pathophysiological mechanism Genomic evidence
Opioid Dependence Altered receptor signaling due to variants (e.g., A118G) affects reward pathways and addiction susceptibility. ClinVar, PMID: 20034518
Pain Sensitivity (Congenital insensitivity to pain, rare) Loss-of-function mutations reduce receptor activity, impairing pain perception. OMIM, PMID: 16916642
Alcohol Dependence OPRM1 variants influence alcohol reward and dependence risk. ClinVar, PMID: 19012872
Naltrexone Response in Alcoholism A118G variant predicts better response to naltrexone treatment. ClinVar, PMID: 19012872

Expression Profile

Tissue Expression
Tissue nTPM level
Brain (cortex) 2.3 Low
Brain (cerebellum) 1.1 Low
Spinal cord 3.5 Low
Adrenal gland 0.8 Low
Gastrointestinal tract 0.5 Low
Cell Line Expression
Cell Line nTPM Notes
SH-SY5Y (neuroblastoma) 5.2 Endogenous expression
U-87 MG (glioblastoma) 1.4 Low expression
HEK293 (embryonic kidney) 0.0 Not expressed (used for transfection)
HepG2 (hepatocellular carcinoma) 0.0 Not expressed
Data source:Human Protein Atlas(proteinatlas.org)

Mutations & Variants

Hotspot Mutations
Variant Type Frequency Functional Description
A118G (rs1799971) SNP (missense, N40D) Allele frequency: ~15-30% in various populations Reduced receptor expression and signaling; altered pain sensitivity and opioid response.
C17T (rs1799972) SNP (5' UTR) ~5-10% May affect mRNA stability and receptor expression.
R265H (rs540825) Missense Rare Potential loss of function; associated with altered binding affinity.
S268P (rs17181000) Missense Rare Impaired receptor trafficking and signaling.
Mutation functional classification

Loss of Function (LOF)

A118G and S268P reduce receptor expression or signaling, leading to decreased opioid efficacy.

Gain of Function (GOF)

No common gain-of-function variants reported; some rare variants may increase signaling but not well characterized.

Dominant Negative (DN)

Not reported for OPRM1.

Gene Ontology (GO)

• G protein-coupled receptor activity • opioid receptor activity
• signal transduction • adenylate cyclase inhibition
• MAPK cascade • response to morphine
• neurotransmitter receptor activity • plasma membrane

Pathways

GPCR downstream signaling
Opioid signaling pathway
G alpha i signaling events
cAMP signaling pathway
MAPK signaling pathway

Protein Summary

The mu-opioid receptor (MOR) is a 7-transmembrane G protein-coupled receptor. Upon agonist binding, it activates G proteins (Gi/Go), inhibiting adenylate cyclase, reducing cAMP levels, and modulating ion channels (e.g., activating GIRK channels, inhibiting voltage-gated calcium channels). This leads to neuronal hyperpolarization and reduced neurotransmitter release, producing analgesia and reward. The receptor undergoes post-translational modifications including glycosylation and phosphorylation, which regulate trafficking and desensitization.

Related Products

Product name Cat.No. Species Gene ID
OPRM1 Knockout HEK293 Cell Line EDJ-KQ3041 Human 4988 Details Get a Quote
OPRM1 Knockout HeLa Cell Line EDJ-KQ54050 Human 4988 Details Get a Quote
OPRM1 Knockout A-549 Cell Line EDJ-KQ62538 Human 4988 Details Get a Quote
OPRM1 Knockout HCT 116 Cell Line EDJ-KQ71010 Human 4988 Details Get a Quote
Displaying Records 1 To 4 Of 4 Records
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