Nicotinic acetylcholine receptor α3β4 subunit (nAChR α3β4)

The nicotinic acetylcholine receptor α3β4 subunit (nAChR α3β4) is a pentameric ligand-gated ion channel formed by the assembly of α3 and β4 subunits, predominantly expressed in autonomic ganglia and select brain regions involved in reward circuitry and addiction. Upon binding endogenous acetylcholine or exogenous agonists like nicotine, the channel opens to conduct sodium and potassium ions, mediating fast synaptic transmission and modulating both peripheral and central nervous system signaling. The α3β4 nAChR is a validated therapeutic target for addiction, notably nicotine dependence, and is also implicated in neurodegenerative and cardiovascular diseases; numerous agonists, antagonists, and modulators, including selective small molecules such as AT-1001, are under investigation for clinical and research applications. The receptor's structure displays a pentameric arrangement, with high-resolution images revealing ligand binding domains that confer pharmacological selectivity; its physiological, therapeutic, and side effect profile remains a focal point for CNS and autonomic drug development.

Other names

Alpha3beta4 nicotinic receptorGanglion-type nicotinic receptorα3β4 nAChRα3β4 nicotinic acetylcholine receptor

Agonists induce channel opening to allow cation influx (Na+, K+), depolarizing post- or presynaptic neurons Antagonists block ion channel function, inhibiting neurotransmission Partial agonists modulate channel with lower efficacy Noncompetitive antagonists block function via allosteric or channel pore binding