Neuronal acetylcholine receptor subunit alpha-4 beta-2 (α4β2 nicotinic acetylcholine receptor)

The neuronal acetylcholine receptor subunit alpha-4 beta-2 forms a pentameric ligand-gated ion channel that mediates fast cholinergic synaptic transmission in the central nervous system. It is the major high-affinity nicotine binding site and plays key roles in learning, memory, and attention, as well as being implicated in multiple neurological and psychiatric disorders. The receptor exists in two principal stoichiometries—(α4)_2_(β2)_3_ and (α4)_3_(β2)_2_—which differ in sensitivity to agonists and permeability to calcium. Drugs commonly target this receptor for smoking cessation and for modulating cognitive function, but its role in addiction and neurological disease makes it a primary focus for ongoing research and pharmacological intervention.

Other names

α4β2 nicotinic acetylcholine receptorCHRNA4/CHRNB2 receptorα4β2 nAChRBeta-2 nicotinic receptorNeuronal nicotinic acetylcholine receptor alpha-4 beta-2 subtype

Agonists (e.g., nicotine, varenicline) bind to the receptor, causing channel opening and inflow of Na^+^/K^+^/Ca^2+^ Partial agonists modulate the receptor response, used therapeutically to manage withdrawal (e.g., varenicline for smoking cessation) Antagonists block acetylcholine binding, inhibiting receptor activation Allosteric modulation potentiates or inhibits receptor response based on drug binding to non-canonical sites