Optical Control of GABAA Receptors with a Fulgimide‐Based Potentiator

URN to cite this document:: urn:nbn:de:bvb:355-epub-431396
DOI to cite this document:: 10.5283/epub.43139

Rustler, Karin

; Gomila, Alexandre

; Maleeva, Galyna ; Gorostiza, Pau

; Bregestovski, Piotr

; König, Burkhard

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Date of publication of this fulltext: 08 May 2020 06:01

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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 gamma-aminobutyric acid receptors (GABA(A)Rs) and displays full and reversible photoswitching in vitro and in vivo. ...