Target intelligence / Profile preview

Muscarinic Acetylcholine Receptor (mAChR)

Target
mAChR
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

Muscarinic acetylcholine receptors (mAChRs) are a family of G protein-coupled receptors that mediate the effects of the neurotransmitter acetylcholine in both the central and peripheral nervous systems. There are five subtypes (M1-M5), which differ in tissue distribution, signaling mechanisms, and physiological roles. They are major drug targets, with agonists used for conditions with reduced cholinergic activity and antagonists used to treat symptoms of cholinergic excess or block unwanted parasympathetic activity.

Other names
Muscarinic receptormACh receptorsCholinergic muscarinic receptor
02

Mechanism of action

Agonists or antagonists binding to mAChRs, modulating intracellular signaling cascades through G proteins, leading to changes in effector protein activity and downstream physiological effects.

03

Biological functions

Signal transductionParasympathetic nervous system regulationCentral nervous system modulationRegulation of smooth muscle contractionRegulation of cardiac muscle contractionRegulation of glandular secretionModulation of neurotransmitter releaseLearning and memoryRegulation of heart rateControl of sweat gland activity
04

Disease associations

Neurodegenerative diseaseCardiovascular diseaseGastrointestinal disordersCognitive disordersDementiaAlzheimer's disease
05

Safety considerations

Anticholinergic side effects (e.g., dry mouth, blurred vision, constipation, urinary retention)Cardiac effects (e.g., bradycardia or tachycardia)Central nervous system effects (e.g., confusion, hallucinations)
06

Interacting drugs

Acetylcholine

4 more in the full profile.

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