Target intelligence / Profile preview

Muscarinic acetylcholine receptor M3 (CHRM3) (CHRM3)

Target
CHRM3
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Muscarinic acetylcholine receptor M3 (CHRM3) is a G protein-coupled receptor (GPCR) that is widely expressed in smooth muscles, exocrine glands, and the central nervous system (UniProt P20366). It primarily couples to the Gq/11 signaling pathway, which activates phospholipase C and increases intracellular calcium levels, leading to physiological responses such as bronchoconstriction, gastric acid secretion, and glandular salivation (StatPearls, "Physiology, Muscarinic Receptor"). In clinical practice, the M3 receptor is a major therapeutic target for respiratory conditions like chronic obstructive pulmonary disease (COPD) and asthma, where its overactivity contributes to airway narrowing (PubMed, PMC2695207). Glycopyrrolate is a potent, quaternary ammonium muscarinic antagonist that binds to the M3 receptor to block the action of acetylcholine, thereby inducing bronchodilation and reducing excessive secretions (PubChem CID 3494). Because M3 receptors are also found in the bladder and salivary glands, drugs targeting this receptor often carry risks of systemic anticholinergic side effects such as xerostomia, blurred vision, and urinary retention (NIH, LiverTox).

Other names
M3 muscarinic receptorCholinergic receptor muscarinic 3M3RHM3
02

Mechanism of action

Competitive antagonism of acetylcholine at the M3 muscarinic receptor, inhibiting Gq-protein mediated activation of phospholipase C and reducing intracellular calcium mobilization.

03

Biological functions

Signal transductionSmooth muscle contractionGlandular secretionBronchoconstrictionGastric acid secretionPupillary constriction
04

Disease associations

Chronic obstructive pulmonary disease (COPD)AsthmaSialorrheaOveractive bladderPeptic ulcer diseaseIrritable bowel syndrome
05

Safety considerations

Xerostomia (dry mouth)Urinary retentionBlurred visionConstipationTachycardiaCognitive impairment in elderly patients
06

Interacting drugs

Glycopyrrolate

8 more in the full profile.

07

Biomarkers

Forced expiratory volume in 1 second (FEV1)Salivary flow ratePost-void residual volume

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