Neuronal acetylcholine receptor α4β2 (α4β2 nAChR)

The **neuronal acetylcholine receptor α4β2** is a pentameric ligand-gated ion channel predominant in the mammalian central nervous system. Comprising α4 and β2 subunits, it exists in two major stoichiometries: (α4)_2(β2)_3 (high-sensitivity) and (α4)_3(β2)_2 (low-sensitivity), influencing its biophysical properties such as sensitivity to agonists and calcium permeability[4][1][5]. It mediates fast synaptic transmission by conducting cations across the neuronal membrane upon binding the neurotransmitter acetylcholine or drugs like nicotine—the latter being the main site of action underlying nicotine addiction[4][5]. The receptor is crucial for modulating cognitive functions, attention, and neurodevelopment, and has a prominent role in diseases such as epilepsy, nicotine dependence, and neurodegenerative conditions. Drugs targeting this receptor act as agonists or antagonists, influencing neuronal signaling and offering therapeutic avenues for smoking cessation, neurological disorders, or cognitive enhancement[4][5][2].

Other names

Alpha-4 beta-2 nicotinic receptornAChR α4β2α4β2 nicotinic acetylcholine receptorCHRNA4/CHRNB2-containing nAChR

Agonists (e.g., nicotine): Stimulate receptor, increasing cation (Na^+, K^+, some Ca^2+^) permeability, causing neuronal excitation[4][5]; Partial agonists (e.g., varenicline): Partially activate the receptor, reducing withdrawal symptoms; Antagonists: Block acetylcholine/nicotine binding, preventing channel opening