Target intelligence / Profile preview

Opioid Receptor Mu-Type (MOR)

Target
MOR
Molecular classification
G protein-coupled receptor, GPCR, Class A GPCR, Receptor
01

Overview

The mu-type opioid receptor (MOR) is a G protein-coupled receptor (GPCR) that plays a central role in mediating the effects of both endogenous and exogenous opioids. It is primarily responsible for analgesia, euphoria, respiratory depression, sedation, and inhibition of gastrointestinal transit. Activation leads to inhibition of adenylyl cyclase and altered ion channel activity. Drugs targeting MOR are widely used for pain management but carry significant risks including addiction potential and respiratory depression.

Other names
MOPhMOPMOR1MOR-1Mu opiate receptor
02

Mechanism of action

Agonist binding leads to Gi/o-mediated inhibition of adenylyl cyclase/cAMP production, opening of potassium channels, and closing of calcium channels. Phosphorylation leads to β-arrestin recruitment and downstream signaling.

03

Biological functions

AnalgesiaEuphoriaRespiratory depressionSedationRegulation of gastrointestinal transitModulation of stressTemperature regulationEndocrine activity modulationMemory modulationMood modulationMotivation modulationReward pathway modulationSignal transduction
04

Disease associations

PainAddictionSubstance use disorder
05

Safety considerations

Addiction liabilityTolerance developmentPhysical dependenceRespiratory depressionConstipation
06

Interacting drugs

Morphine

4 more in the full profile.

07

Biomarkers

OPRM1 A118G polymorphism

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