Ganglionic nicotinic acetylcholine receptor (gAChR) (gAChR)

The ganglionic nicotinic acetylcholine receptor (gAChR) is a pentameric ligand-gated ion channel that serves as the primary mediator of fast synaptic transmission within the autonomic nervous system (PubMed ID: 18567861, 11005892). These receptors are situated on the postsynaptic membranes of neurons in sympathetic, parasympathetic, and enteric ganglia and are predominantly composed of alpha-3 and beta-4 subunits (PubMed ID: 17405096). Upon binding of acetylcholine released from preganglionic fibers, the gAChR opens to allow an influx of cations, leading to neuronal depolarization and the propagation of autonomic signals that regulate heart rate, vascular tone, and visceral motility (PubMed ID: 18567861). In the disease state of autoimmune autonomic ganglionopathy (AAG), the receptor is targeted by pathogenic autoantibodies, causing comprehensive autonomic failure (PubMed ID: 11005892). While ganglionic blockers like hexamethonium and mecamylamine were historically the first effective treatments for hypertension, their non-selective blockade of both autonomic branches causes significant side effects, such as orthostatic hypotension and dry mouth, which has largely restricted their modern clinical application (Wikipedia: Ganglionic blocker).

Other names

Autonomic nicotinic acetylcholine receptorNeuronal nicotinic acetylcholine receptor subunit alpha-3Alpha-3-beta-4 nicotinic receptorNN receptorN2 receptorAutonomic ganglion-type nicotinic receptor

Binding to the ganglionic nicotinic acetylcholine receptor to either antagonize (blockade) or agonize (stimulate) fast synaptic transmission between pre- and postganglionic autonomic neurons.