Target intelligence / Profile preview

Nicotinic acetylcholine receptor alpha 1 subunit (nAChRα1 (also CHRNA1))

Target
nAChRα1 (also CHRNA1)
Molecular classification
Ion channel, Ligand-gated ion channel, Receptor
01

Overview

The **nicotinic acetylcholine receptor alpha 1 subunit** is a protein encoded by the *CHRNA1* gene in humans. It forms part of the pentameric nicotinic acetylcholine receptors found primarily at neuromuscular junctions. The canonical adult muscle-type nicotinic receptor consists of two α1 subunits along with β1, δ, and ε subunits arranged symmetrically around a central pore. Upon binding acetylcholine released from motor neurons, these receptors undergo conformational changes that open their ion channels—permitting cation influx—which triggers skeletal muscle contraction. Mutations in this gene are associated with congenital myasthenic syndromes due to altered gating or ligand affinity. The α1-containing receptors are targets for several drugs including nicotine and varenicline; they also serve as pharmacological targets for certain paralytic agents used during anesthesia

Other names
Acetylcholine receptor subunit alphaCHRNA1Neuronal acetylcholine receptor subunit alpha-1nAChRα1
02

Mechanism of action

Agonists bind to the extracellular domain of the pentameric receptor, causing a conformational change that opens the central ion channel pore, allowing sodium and potassium ions to pass through and depolarize the muscle membrane, leading to muscle contraction

03

Biological functions

Signal transduction at neuromuscular junctionsMediates synaptic transmission by allowing cation flow upon acetylcholine bindingMuscle contraction control
04

Disease associations

Congenital myasthenic syndromes (e.g., slow-channel myasthenic syndrome)Neuromuscular disorders
05

Safety considerations

Risk of neuromuscular blockade or paralysis with antagonists or excessive agonism.
06

Interacting drugs

Varenicline (partial agonist, used for smoking cessation)

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