Nicotinic Acetylcholine Receptor Subunit Alpha-4 Beta-2 (α4β2 nAChR)

The α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) is a pentameric ligand-gated ion channel composed of alpha-4 (CHRNA4) and beta-2 (CHRNB2) subunits. It is the most abundant nicotinic receptor subtype in the mammalian brain and plays a central role in mediating the effects of nicotine, including its addictive properties. The receptor is implicated in cognitive processes such as learning and attention, as well as growth hormone secretion. Upon binding acetylcholine or agonists like nicotine, the receptor undergoes conformational changes that open its ion channel, allowing Na^+ and K^+ ions to flow across neuronal membranes. This leads to neuronal excitation both pre-synaptically and post-synaptically. Activation enhances neurotransmitter release and modulates synaptic plasticity. Mutations in CHRNA4 have been linked with autosomal dominant nocturnal frontal lobe epilepsy and paroxysmal kinesogenic dyskinesia.

Other names

CHRNA4/CHRNB2 receptoralpha4beta2 nicotinic receptor

Agonist-induced opening of cation channel allowing Na^+ and K^+ influx, leading to neuronal excitation; partial agonism modulating receptor activity.