Modulation of the mammalian GABA_A receptor by type I and type II positive allosteric modulators of the α7 nicotinic acetylcholine receptor.

ABSTRACT:

Background and purpose

Positive allosteric modulators of the α7 nicotinic acetylcholine (nACh) receptor (α7-PAMs) possess promnesic and procognitive properties and have potential in the treatment of cognitive and psychiatric disorders including Alzheimer's disease and schizophrenia. Behavioural studies in rodents have indicated that α7-PAMs can also produce antinociceptive and anxiolytic effects that may be associated with positive modulation of the GABA_A receptor. The overall goal of this study was to investigate the modulatory actions of selected α7-PAMs on the GABA_A receptor.

Experimental approach

We employed a combination of cell fluorescence imaging, electrophysiology, functional competition and site-directed mutagenesis to investigate the function

SUBMITTER: Arias HR 

PROVIDER: S-EPMC9669183 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature