Nicotinic acetylcholine receptor alpha3 beta4 subunit-containing (nAChR α3β4)

The **Nicotinic acetylcholine receptor alpha3 beta4 subunit-containing** (nAChR α3β4) is a pentameric ligand-gated ion channel composed of combinations of α3 and β4 subunits[1][3][5]. It mediates fast synaptic transmission in autonomic ganglia by allowing Na⁺ and K⁺ influx upon activation by acetylcholine or other agonists. This receptor is highly expressed in the peripheral nervous system (autonomic ganglia, adrenal medulla) and certain brain regions linked to reward and addiction. The α3β4 subtype serves as a relay between central and peripheral nervous systems and is pivotal for modulating autonomic tone and reward circuitry. Antagonists selective for α3β4, such as AT-1001 or 18-MC, demonstrate utility in reducing drug-seeking behaviors and are under investigation as therapies for substance use disorders, especially nicotine addiction[2][3][5]. The receptor’s structural details have been resolved using cryo-EM, revealing key aspects of ligand selectivity and ion permeation[1][5][7].

Other names

Alpha3 beta4 nicotinic receptorα3β4 receptorGanglion-type nicotinic receptorNeuronal nicotinic acetylcholine receptor α3β4

Agonist (e.g. acetylcholine, nicotine) binding induces channel opening, resulting in increased Na⁺ and K⁺ ion permeability[3][5]. Competitive antagonists bind to the receptor’s ligand-binding site and block activation (e.g. DHβE, SR16584)[3]. Non-competitive antagonists inhibit function via allosteric/ion channel block (e.g. mecamylamine, AT-1001, 18-MC, bupropion)[2][3].