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Optical Control of GABAA Receptors with a Fulgimide‐Based Potentiator
Rustler, Karin
, Gomila, Alexandre , Maleeva, Galyna, Gorostiza, Pau , Bregestovski, Piotr and König, Burkhard
(2020)
Optical Control of GABAA Receptors with a Fulgimide‐Based Potentiator.
Chemistry - A European Journal 26, pp. 12722-12727.
Date of publication of this fulltext: 08 May 2020 06:01
Article
DOI to cite this document: 10.5283/epub.43139
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. ...
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. The compound enables high-resolution studies of GABAergic neurotransmission, and phototherapies based on localized, acute, and reversible neuroinhibition.
Involved Institutions
Details
| Item type | Article | ||||||
| Journal or Publication Title | Chemistry - A European Journal | ||||||
| Publisher: | Wiley | ||||||
|---|---|---|---|---|---|---|---|
| Place of Publication: | WEINHEIM | ||||||
| Volume: | 26 | ||||||
| Page Range: | pp. 12722-12727 | ||||||
| Date | 2020 | ||||||
| Institutions | Chemistry and Pharmacy > Institut für Organische Chemie Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König | ||||||
| Identification Number |
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| Keywords | IN-VIVO; PHARMACOLOGY; DERIVATIVES; fulgimides; GABA(A) Receptors; in vivo; photopharmacology | ||||||
| Dewey Decimal Classification | 500 Science > 540 Chemistry & allied sciences 500 Science > 570 Life sciences 600 Technology > 615 Pharmacy | ||||||
| Status | Published | ||||||
| Refereed | Yes, this version has been refereed | ||||||
| Created at the University of Regensburg | Partially | ||||||
| URN of the UB Regensburg | urn:nbn:de:bvb:355-epub-431396 | ||||||
| Item ID | 43139 |
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