Target intelligence / Profile preview

Opioid Receptor (OR)

Target
OR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Opioid receptors are a group of inhibitory G protein-coupled receptors (GPCRs) that mediate the effects of endogenous and exogenous opioids. These receptors play a central role in pain modulation, reward, addiction, and various physiological processes. There are three main classical opioid receptor subtypes: Mu (μ), Delta (δ), and Kappa (κ), as well as the Nociceptin/orphanin FQ peptide (NOP) receptor. Activation results in decreased neuronal excitability and reduced neurotransmitter release.

Other names
Opioid receptorsOpioid receptor family
02

Mechanism of action

Agonist binding induces conformational change, activating G proteins. Gαi/o subunit inhibits adenylyl cyclase, reducing cAMP levels, and modulates ion channels, leading to decreased neuronal excitability and reduced neurotransmitter release.

03

Biological functions

Pain relief/analgesiaReward signalingRespiratory regulationGastrointestinal motility regulationStress response modulationSignal transduction
04

Disease associations

PainAddictionMood disorders
05

Safety considerations

Respiratory depressionAddictionToleranceDependenceOverdose
06

Interacting drugs

Morphine

6 more in the full profile.

07

Biomarkers

OPRM1 gene variations

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