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Optical Control of GABA A Receptors with a Fulgimide‐Based Potentiator
Author(s) -
Rustler Karin,
Maleeva Galyna,
Gomila Alexandre M. J.,
Gorostiza Pau,
Bregestovski Piotr,
König Burkhard
Publication year - 2020
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.202000710
Subject(s) - potentiator , ionotropic effect , optogenetics , gabaergic , receptor , gabaa receptor , neuroscience , chemistry , in vivo , neurotransmission , channelrhodopsin , pharmacology , glutamate receptor , biology , biochemistry , microbiology and biotechnology
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.