Light-Activated Agonist-Potentiator of GABA_A Receptors for Reversible Neuroinhibition in Wildtype Mice.

ABSTRACT: Gamma aminobutyric acid type A receptors (GABA_ARs) play a key role in the mammalian central nervous system (CNS) as drivers of neuroinhibitory circuits, which are commonly targeted for therapeutic purposes with potentiator drugs. However, due to their widespread expression and strong inhibitory action, systemic pharmaceutical potentiation of GABA_ARs inevitably causes adverse effects regardless of the drug selectivity. Therefore, therapeutic guidelines must often limit or exclude clinically available GABA_AR potentiators, despite their high efficacy, good biodistribution, and favorable molecular properties. One solution to this problem is to use drugs with light-dependent activity (photopharmacology) in combination with on-demand, localized illumination. Howe

SUBMITTER: Maleeva G 

PROVIDER: S-EPMC11503767 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature