A photoswitchable GABA receptor channel blocker.

08:00 EDT 13th April 2019 | BioPortfolio

Summary of "A photoswitchable GABA receptor channel blocker."

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 available GABAR and GlyR channel blockers effectively suppress inhibitory currents in neurons, but their systemic administration is highly toxic. Aiming to develop an efficient light-controllable modulator of GABA receptors we constructed Azo-NZ1, which is composed of a nitrazepam moiety merged to an azobenzene photoisomerizable group.


Journal Details

This article was published in the following journal.

Name: British journal of pharmacology
ISSN: 1476-5381


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Medical and Biotech [MESH] Definitions

Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.

Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.

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