Nicotinic acetylcholine receptor alpha4beta2 (α4β2 nAChR)

The nicotinic acetylcholine receptor alpha4beta2 (α4β2 nAChR) is a heteropentameric ligand-gated ion channel that mediates fast chemical neurotransmission in the brain. As the most abundant nicotinic subtype in the brain, it plays crucial roles in cognitive function, learning, and various neurological processes. The receptor exists in two stoichiometries with different sensitivities to nicotine and calcium permeability. It is the primary target for nicotine's addictive properties and is implicated in several neurological disorders including Parkinson's disease, Alzheimer's disease, and schizophrenia. The receptor's structure has been determined by X-ray crystallography, revealing insights into its complex architecture and function. Pharmacologically, it can be targeted by various agonists, antagonists, and positive allosteric modulators, making it an important therapeutic target for neurological and psychiatric conditions. Recent research has focused on developing subtype-selective compounds that can modulate α4β2 nAChR function with minimal side effects.

Other names

Alpha-4 beta-2 nicotinic receptorα4β2 receptorHeteromeric α4β2 nicotinic receptor

Agonism - direct activation of the receptor leading to cation influx; Positive allosteric modulation - enhancing the effect of endogenous agonists; Antagonism - blocking receptor activation