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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

This publication is part of the DEAL contract with Wiley.


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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