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Muscarinic acetylcholine receptor M3 (main example; also M2 subtype) (CHRM3, CHRM2)

Target
CHRM3, CHRM2
Molecular classification
G protein-coupled receptor, Ion channel, Motor protein
01

Overview

"Gastrointestinal smooth muscle targets" refers collectively to the variety of molecular entities in GI smooth muscle that regulate contraction and motility, with principal therapeutic focus on muscarinic acetylcholine receptors (M2 and M3 subtypes) which mediate cholinergic contraction in response to acetylcholine released from parasympathetic nerves[1][2][8]. These receptors are G protein-coupled receptors expressed abundantly in GI smooth muscle, where their activation triggers a cascade of signaling events, including inhibition of adenylyl cyclase, phosphoinositide hydrolysis, Ca²⁺ mobilization, and modulation of ion channel activity, all culminating in smooth muscle contraction[1][2]. Other relevant targets include myosin heavy chain (MYH11), L-type calcium channels, and various ion channels and intercellular signaling molecules involved in excitation–contraction coupling[3][4][7]. This terminology is not specific to a single molecule, and as such, any inquiry should target individual molecular entities (e.g., "muscarinic acetylcholine receptor M3") to obtain structured, actionable data. Use of "Gastrointestinal smooth muscle targets" is considered an umbrella term and not a canonical molecular target[1][2][3][4].

Other names
GI smooth muscle targetssmooth muscle muscarinic receptorsgastrointestinal muscarinic receptors(M2/M3 receptors in smooth muscle)
02

Mechanism of action

Muscarinic receptor antagonism (relaxes smooth muscle, reduces spasm); Muscarinic receptor agonism (stimulates contraction); Cholinesterase inhibition (increases acetylcholine, stimulates contraction); Calcium channel blockade (suppresses contraction)

03

Biological functions

Signal transductionMuscle contractionGastrointestinal motilityCellular excitation-contraction coupling
04

Disease associations

Gastrointestinal motility disorders (e.g., gastroparesis, irritable bowel syndrome)Obstructive bowel diseasesInflammationOther GI transit and contractility disturbances
05

Safety considerations

Non-selectivity of muscarinic drugs (off-target effects: dry mouth, blurred vision, tachycardia, urinary retention)GI obstruction risk with strong stimulationCardiac and central nervous system side effectsTolerance, desensitization with chronic therapy
06

Interacting drugs

Atropine (antagonist, nonselective mAChR blocker)

3 more in the full profile.

07

Biomarkers

MYH11 (smooth muscle myosin heavy chain, marker of differentiated SMC)Expression levels of M2 and M3 muscarinic receptorsc-Kit (marker for interstitial cells of Cajal, not SMC-specific but relevant in GI motility studies)

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