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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 ; Bregestovski, Piotr



Abstract

Background and Purpose Anion-selective Cys-loop receptors (GABA and glycine receptors) provide the main inhibitory drive in the CNS. Both types of receptor operate via chloride-selective ion channels, though 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 ...

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