Optical Control of GABA(A) Receptors with a Fulgimide-Based Potentiator

Rustler, Karin and Maleeva, Galyna and Gomila, Alexandre M. J. and Gorostiza, Pau and Bregestovski, Piotr and Koenig, Burkhard (2020) Optical Control of GABA(A) Receptors with a Fulgimide-Based Potentiator. CHEMISTRY-A EUROPEAN JOURNAL, 26 (56). pp. 12722-12727. ISSN 0947-6539, 1521-3765

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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 gamma-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.

Item Type: Article
Uncontrolled Keywords: IN-VIVO; PHARMACOLOGY; DERIVATIVES; fulgimides; GABA(A) Receptors; in vivo; photopharmacology
Subjects: 500 Science > 540 Chemistry & allied sciences
Divisions: Chemistry and Pharmacy > Institut für Organische Chemie
Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Depositing User: Dr. Gernot Deinzer
Date Deposited: 11 Mar 2021 12:47
Last Modified: 11 Mar 2021 12:47
URI: https://pred.uni-regensburg.de/id/eprint/43811

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