Target intelligence / Profile preview

Opioid receptor mu-type 1 (MOR (also known as OPRM1))

Target
MOR (also known as OPRM1)
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The Opioid receptor mu-type 1, also known as mu opioid receptor, is a member of the G protein-coupled receptor family encoded by the *OPRM1* gene. It is primarily expressed in neurons throughout the nervous system. This receptor serves as the main binding site for endogenous peptides like beta‐endorphin and enkephalins, which regulate pain perception, reward mechanisms, mood, stress response, and addictive behaviors. It is also targeted by exogenous opioids—including prescription analgesics such as morphine, oxycodone, fentanyl, methadone—and illicit drugs like heroin. Activation leads to inhibition of neurotransmitter release via Gi/o protein signaling pathways. The mu opioid receptor plays a central role in mediating both therapeutic effects such as analgesia and adverse outcomes including tolerance development, physical dependence/addiction liability, respiratory depression risk during overdose situations. Genetic variants like A118G can influence individual differences in drug response and vulnerability to substance use disorders.

Other names
Mu opioid receptorMu opiate receptorMORMOPM-OR-1LMORMOR1OPRM1
02

Mechanism of action

Drugs targeting this molecule typically act as: Agonists—activate the mu opioid receptor to produce analgesia and euphoria (e.g., morphine, fentanyl); Partial agonists—partially activate the receptor with a ceiling effect on efficacy (e.g., buprenorphine); Antagonists—block the effects of opioids at this site to reverse overdose or prevent abuse (e.g., naloxone)

03

Biological functions

Signal transduction (via G proteins)Regulation of pain perception/analgesiaModulation of reward pathways and addictive behaviors
04

Disease associations

Substance dependence/addiction (opioids, alcohol, nicotine, cocaine)Pain disorders/chronic pain management
05

Safety considerations

Respiratory depression leading to fatal overdose when activated by high doses or potent agonistsHigh potential for addiction/dependence with chronic use or misuseGenetic variability may affect individual responses and risk profiles for both efficacy and adverse effects such as addiction or respiratory depression.
06

Interacting drugs

Morphine

9 more in the full profile.

07

Biomarkers

Risk of opioid addiction/substance dependence susceptibilityVariability in pain sensitivity and response to opioids

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