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Updated: Dec 23, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Optical Control of GABAA Receptors with a Fulgimide-Based Potentiator
Karin Rustler1, Galyna Maleeva2,3, Alexandre M J Gomila3
1Institute of Organic Chemistry, Department of Chemistry and Pharmacy, University of Regensburg, 93053, Regensburg, Germany.
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 (GABAA 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.
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