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Optical Control of GABA_A Receptors with a Fulgimide-Based Potentiator.

ABSTRACT: Optogenetic and photopharmacological tools to manipulate neuronal inhibition have limited efficacy and reversibility. We report the design, synthesis, and biological evaluation of Fulgazepam, a fulgimide derivative of benzodiazepine that behaves as a pure potentiator of ionotropic γ-aminobutyric acid receptors (GABA_A Rs) and displays full and reversible photoswitching in vitro and in vivo. The compound enables high-resolution studies of GABAergic neurotransmission, and phototherapies based on localized, acute, and reversible neuroinhibition.

SUBMITTER: Rustler K

PROVIDER: S-EPMC7589408 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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Optical Control of GABAA Receptors with a Fulgimide-Based Potentiator.

Rustler Karin K Maleeva Galyna G Gomila Alexandre M J AMJ Gorostiza Pau P Bregestovski Piotr P König Burkhard B

Chemistry (Weinheim an der Bergstrasse, Germany) 20200911 56

Optogenetic and photopharmacological tools to manipulate neuronal inhibition have limited efficacy and reversibility. We report the design, synthesis, and biological evaluation of Fulgazepam, a fulgimide derivative of benzodiazepine that behaves as a pure potentiator of ionotropic γ-aminobutyric acid receptors (GABAA Rs) and displays full and reversible photoswitching in vitro and in vivo. The compound enables high-resolution studies of GABAergic neurotransmission, and phototherapies ...[more]

PMID: 32307732

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