Target intelligence / Profile preview

Muscarinic acetylcholine receptor M1, M2, M3, M4, and M5 (CHRM1, CHRM2, CHRM3, CHRM4, CHRM5)

Target
CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Molecular classification
Receptor, G protein-coupled receptor
01

Overview

Muscarinic acetylcholine receptors M1, M2, M3, M4, and M5 are a family of G protein-coupled receptors (GPCRs) that are activated by the neurotransmitter acetylcholine. They mediate parasympathetic neural effects throughout the central and peripheral nervous systems and are involved in a variety of physiological processes including neuromodulation, smooth muscle contraction, and exocrine gland secretion[3][5][7]. Diverse muscarinic receptor subtypes are distributed differentially across neural and non-neural tissues. Antipsychotic drugs such as olanzapine interact with these receptors, exhibiting antagonistic activity that may contribute both to therapeutic effects (particularly in neuropsychiatric disorders) and to adverse effects, such as anticholinergic side effects and metabolic disturbances[1][3][4][5]. Selective targeting of certain muscarinic subtypes is an area of therapeutic interest for conditions such as schizophrenia and Alzheimer’s disease[5][7].

Other names
Muscarinic receptorsmAChRCHRM1CHRM2CHRM3CHRM4CHRM5
02

Mechanism of action

Antagonism of muscarinic acetylcholine receptors blocks acetylcholine-mediated signal transduction, affecting parasympathetic activity and CNS processes[1][3][4][5]. Some drugs (like cevimeline) are agonists, stimulating muscarinic receptors.

03

Biological functions

Signal transductionNeurotransmissionModulation of synaptic plasticityRegulation of glandular secretionParasympathetic nervous system modulation
04

Disease associations

Neuropsychiatric disorders (e.g., schizophrenia, Alzheimer’s disease)Cardiovascular diseaseDiabetes/metabolic syndromeOther CNS disorders
05

Safety considerations

Anticholinergic side effects (dry mouth, constipation, urinary retention, blurred vision, cognitive impairment)CNS effects including confusion, delirium (especially in the elderly)Contribution to metabolic syndrome when antagonized by antipsychotics[3][5]
06

Interacting drugs

Olanzapine

8 more in the full profile.

07

Biomarkers

No established muscarinic receptor subtype–specific biomarkers in clinical use

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