Nicotinic acetylcholine receptor subunit beta-4 (CHRNB4)

The Nicotinic acetylcholine receptor subunit beta-4 (CHRNB4) is a protein that contributes to the formation of pentameric ligand-gated ion channels. These receptors are primarily located in the autonomic ganglia and specific brain regions such as the habenulo-interpeduncular pathway (UniProt: P30926). CHRNB4 typically co-assembles with alpha-3 subunits to form the α3β4 receptor subtype, which mediates fast excitatory neurotransmission. Activation by acetylcholine or exogenous agonists like nicotine triggers the influx of cations, leading to membrane depolarization (PubMed: 29101214). This subunit is a major focus in addiction research, as genetic variants in the CHRNA5-CHRNA3-CHRNB4 cluster are significantly linked to nicotine dependence and lung cancer susceptibility (NIH: Gene ID 1143). Therapeutic agents targeting this receptor include smoking cessation aids that act as partial agonists to reduce withdrawal symptoms and block the reinforcing effects of nicotine. Additionally, antagonists of CHRNB4-containing receptors are used to study or treat autonomic disorders and certain types of substance abuse (PubChem: CID 4033).

Other names

Neuronal acetylcholine receptor subunit beta-4nAChR beta-4Cholinergic receptor nicotinic beta 4 subunit

Drugs targeting CHRNB4-containing receptors function as agonists, partial agonists, or antagonists that modulate the opening of the ion channel pore, thereby regulating cation flow and neuronal excitability (StatPearls: NBK531463).