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Optical Control of GABAA Receptors with a Fulgimide‐Based Potentiator

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Rustler, Karin ; Gomila, Alexandre ; Maleeva, Galyna ; Gorostiza, Pau ; Bregestovski, Piotr ; König, Burkhard
License: Creative Commons Attribution 4.0
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Date of publication of this fulltext: 08 May 2020 06:01


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. ...


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