Target intelligence / Profile preview

Muscarinic acetylcholine receptor family (M1–M5) (CHRM1–CHRM5)

Target
CHRM1–CHRM5
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Muscarinic acetylcholine receptors (M1–M5) are a family of G protein-coupled receptors widely expressed throughout the central and peripheral nervous systems[7]. The M1 receptor, in particular, plays a critical role in modulating cognitive functions and brain circuits relevant to neuropsychiatric disorders such as schizophrenia[4][10]. M1–M5 receptors respond to the neurotransmitter acetylcholine, mediating various physiological functions including neural plasticity, memory, and modulation of dopamine pathways[4][10]. Certain drugs, such as xanomeline and N-desmethylclozapine, act as agonists or allosteric modulators of muscarinic receptors and are under investigation for the treatment of cognitive and negative symptoms in schizophrenia[1][4][10]. Risperidone, however, does not act as an antagonist at muscarinic receptors and is not considered to exert its effects through direct interaction with the M1–M5 subtypes; its primary targets are dopamine D2 and serotonin 5-HT2A receptors[2][3][5][8]. Therefore, "Risperidone - Muscarinic M1–M5" is not a correct designation for a molecular target.

Other names
Muscarinic receptor M1CHRM1Acetylcholine receptor M1Muscarinic receptor familyCholinergic receptor muscarinic M1–M5
02

Mechanism of action

Agonists enhance cholinergic neurotransmission (e.g., xanomeline, N-desmethylclozapine as M1 agonists); Antagonists inhibit cholinergic signaling (e.g., biperiden, scopolamine); Positive allosteric modulators potentiate effects of endogenous acetylcholine.

03

Biological functions

Signal transductionCentral nervous system regulationModulation of neurotransmitter release
04

Disease associations

Neurodegenerative disease (e.g., Alzheimer’s disease)Schizophrenia and neuropsychiatric disordersParkinson’s diseaseOther CNS disorders
05

Safety considerations

Anticholinergic side effects (e.g., cognitive impairment, dry mouth, blurred vision, constipation)CNS toxicity (in overdose or in sensitive individuals, especially elderly)Potential worsening of cognitive symptoms in at-risk populations
06

Interacting drugs

Clozapine (and its active metabolite N-desmethylclozapine)

5 more in the full profile.

07

Biomarkers

M1 receptor expression (potential imaging biomarkers for patient selection in schizophrenia)

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