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A photoswitchable GABA receptor channel blocker

Maleeva, Galyna, Wutz, Daniel, Rustler, Karin , Nin-Hill, Alba, Alfonso-Prieto, Mercedes, Petukhova, Elena, Bautista-Barrufet, Antoni, Gomila-Juaneda, Alexandre, Scholze, Petra, Peiretti, Franck, Rovira, Carme, König, Burkhard , Gorostiza, Pau and Bregestovski, Piotr (2019) A photoswitchable GABA receptor channel blocker. British Journal of Pharmacology.

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Abstract

BACKGROUND AND PURPOSE: Anion-selective Cys-loop receptors (GABARs and GlyRs) provide main inhibitory drive in CNS. Both types of receptors are operating via chloride-selective ion channels, however with different kinetics, pharmacological profiles and localization. Disequilibrium in their function leads to a variety of disorders, which are often treated with allosteric modulators. The few ...

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Item type:Article
Date:2019
Institutions:Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Projects:PCIN-2015-163-C02-01
Identification Number:
ValueType
30981211PubMed ID
10.1111/bph.14689DOI
Keywords:Cys-loop receptors, GABAA receptors, GABAC receptors, photopharmacology, photoswitchable molecules, azobenzene, patch-clamp, pore-blocking molecules, benzodiazepines
Dewey Decimal Classification:500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Item ID:40161
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