Analogs of α-conotoxin PnIC selectively inhibit α7β2- over α7-only subtype nicotinic acetylcholine receptors via a novel allosteric mechanism.

ABSTRACT: This study was undertaken to identify and characterize the first ligands capable of selectively identifying nicotinic acetylcholine receptors containing α7 and β2 subunits (α7β2-nAChR subtype). Basal forebrain cholinergic neurons express α7β2-nAChR. Here, they appear to mediate neuronal dysfunction induced by the elevated levels of oligomeric amyloid-β associated with early Alzheimer's disease. Additional work indicates that α7β2-nAChR are expressed across several further critically important cholinergic and GABAergic neuronal circuits within the central nervous system. Further studies, however, are significantly hindered by the inability of currently available ligands to distinguish heteromeric α7β2-nAChR from the closely related and more widespread homomeric α7-only-nAChR subtype. Functi

SUBMITTER: George AA 

PROVIDER: S-EPMC10782225 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature