Target intelligence / Profile preview

Muscarinic acetylcholine receptor M2 and M3 (CHRM2/CHRM3)

Target
CHRM2/CHRM3
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The muscarinic acetylcholine receptors M2 (CHRM2) and M3 (CHRM3) are G protein-coupled receptors that play central roles in the parasympathetic nervous system's response to acetylcholine [1, 2]. CHRM2 is primarily coupled to Gi proteins and is highly expressed in the heart and central nervous system, where it acts to decrease heart rate and modulate neurotransmitter release [2, 11]. CHRM3 is coupled to Gq proteins and is found in smooth muscles and exocrine glands, where it mediates contraction of the bladder and airways and stimulates glandular secretions [2, 15]. These receptors are critical therapeutic targets; for instance, antagonists are used to treat overactive bladder by relaxing the detrusor muscle and to manage COPD and asthma by inducing bronchodilation [8, 15]. However, the lack of subtype selectivity in many current drugs leads to common side effects such as dry mouth, constipation, and tachycardia [2, 5]. Beyond autonomic functions, CHRM2 and CHRM3 are also implicated in cognitive processes, and their dysregulation is associated with Alzheimer's disease and certain cancers [6, 12, 17].

Other names
M2 receptorM3 receptorCholinergic receptor muscarinic 2Cholinergic receptor muscarinic 3M2RM3RMuscarinic acetylcholine receptor 2Muscarinic acetylcholine receptor 3
02

Mechanism of action

Muscarinic receptor antagonist

03

Biological functions

Signal transductionSmooth muscle contractionHeart rate regulationGlandular secretionNeurotransmission regulationCognitive processing
04

Disease associations

Overactive bladderChronic obstructive pulmonary disease (COPD)AsthmaBradycardiaAlzheimer's diseaseSchizophreniaCancer
05

Safety considerations

Dry mouth (xerostomia)ConstipationBlurred visionUrinary retentionTachycardiaCognitive impairmentConfusion
06

Interacting drugs

Atropine

9 more in the full profile.

07

Biomarkers

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

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