A Pharmacophore for Drugs Targeting the α4α4 Binding Site of the (α4)<sub>3</sub>(β2)<sub>2</sub> Nicotinic Acetylcholine Receptor.
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ABSTRACT: Neuronal nicotinic acetylcholine receptors (nAChRs) have an established role in pain pathways and devastating neurodegenerative diseases; however, few drugs have been successfully developed to target them. The most abundant nAChR in the brain, the α4β2 nAChR, is assembled from five subunits in a 3α:2β stoichiometry-(α4)3(β2)2. This receptor contains a unique agonist-binding site at the α4α4 interface in addition to two classical agonist-binding sites at α4β2 interfaces. Most known agonists target both α4α4 and α4β2 sites, however, a few compounds with selectivity for the α4α4 site have been identified. These α4α4 selective compounds have a modulator-like effect akin to benzodiazepines in the γ-aminobutyric acid type A receptor, which is desirable from a drug developme
SUBMITTER: Kusay AS
PROVIDER: S-EPMC11836552 | biostudies-literature | 2025 Feb
REPOSITORIES: biostudies-literature
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