Human α7 nicotinic acetylcholine receptor (α7 nAChR)

The human α7 nicotinic acetylcholine receptor is a homo-pentameric ligand-gated ion channel that belongs to the Cys-loop superfamily. Highly permeable to calcium ions, this receptor plays essential roles in fast synaptic transmission, especially within the central nervous system, modulating cognition, neuroprotection, pain, and the cholinergic inflammatory pathway. Its structural and functional properties—including rapid desensitization—make it an important drug target for neurodegenerative diseases, cognitive impairment, inflammatory conditions, and, paradoxically, certain cancers. Both orthosteric and allosteric drug modulators are under clinical investigation, though fast desensitization and translational gaps—such as the influence of the human-specific CHRFAM7A gene—pose therapeutic challenges.

Other names

α7 nAChRα7 nicotinic receptorα7 receptorNicotinic acetylcholine receptor alpha-7 subunitCHRNA7

Agonists: Activate the receptor leading to opening of the ion channel and cation (primarily Ca²⁺) influx. Positive allosteric modulators: Increase efficacy or prolong activation of the ligand-gated ion channel in the presence of agonist. Antagonists: Block ion channel opening by competing with endogenous ligands or binding allosteric sites.