Optical Control of GABA A  Receptors with a Fulgimide‐Based Potentiator | Zendy

Rustler Karin | Zendy; Maleeva Galyna | Zendy; Gomila Alexandre M. J. | Zendy; Gorostiza Pau | Zendy; Bregestovski Piotr | Zendy; König Burkhard | Zendy

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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.

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