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Muscle-type nicotinic acetylcholine receptor subunit alpha-1 (CHRNA1) (CHRNA1)

Target
CHRNA1
Molecular classification
Ion channel, Ligand-gated ion channel, Nicotinic acetylcholine receptor, Receptor
01

Overview

The Muscle-type nicotinic acetylcholine receptor subunit alpha-1 (CHRNA1) is a fundamental component of the pentameric ligand-gated ion channel located at the postsynaptic membrane of the neuromuscular junction (UniProt P02708). It serves as the primary binding site for the neurotransmitter acetylcholine, which, upon binding, triggers a conformational change that opens the channel to allow the influx of cations, primarily sodium, leading to muscle membrane depolarization and subsequent contraction (PubMed: 21840469). This subunit is a major therapeutic target for neuromuscular blocking agents used during surgical procedures to induce muscle relaxation, categorized into depolarizing agents like succinylcholine and non-depolarizing agents like rocuronium (StatPearls: NBK535383). Clinically, CHRNA1 is highly significant as the primary target of pathogenic autoantibodies in myasthenia gravis, an autoimmune disorder characterized by muscle weakness (PubMed: 30535111). Mutations in the CHRNA1 gene are also linked to various congenital myasthenic syndromes and lethal multiple pterygium syndrome, highlighting its essential role in human motor function (NCBI Gene: 1134). Pharmacological modulation of this receptor requires precise dosing to avoid prolonged paralysis or respiratory failure, making it a critical focus in anesthesiology and emergency medicine (StatPearls: NBK535383).

Other names
ACHRACHRNACMS1ACMS1BFCCMSSCCMSAcetylcholine receptor subunit alpha
02

Mechanism of action

Competitive antagonism of acetylcholine binding to prevent depolarization (non-depolarizing blockers) or persistent activation and depolarization of the motor endplate leading to desensitization (depolarizing blockers).

03

Biological functions

Signal transductionNeuromuscular transmissionIon transportMuscle contraction
04

Disease associations

Myasthenia gravisCongenital myasthenic syndromeLethal multiple pterygium syndrome
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Safety considerations

Respiratory paralysisMalignant hyperthermiaHyperkalemiaAnaphylaxisPostoperative residual neuromuscular blockade
06

Interacting drugs

Succinylcholine

9 more in the full profile.

07

Biomarkers

Anti-AChR antibodiesTrain-of-four (TOF) ratioCompound muscle action potential (CMAP) amplitude

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