A Turn-on Imaging Probe for GABA(A) Receptors Allows for Construction of Fluorescent Biosensor

摘要

Fast inhibitory neurotransmission in the central nervous system is mainly mediated via ion-channel type GABAA receptors (GABAARs). 1,2 Since dysregulation of GABAAR is associated with a variety of neurological and psychiatric disorders, molecules that can control GABAAR functions are regarded as potential therapeutic agents. Among such kinds of molecules, allosteric modulators (AMs) have drawn intense attention because of their higher specificity and less toxicity relative to traditional compounds which bind to the orthosteric site of a target protein.