Subtype selectivity of α+β− site ligands of<scp>GABA_A</scp>receptors: identification of the first highly specific positive modulators at α6β2/3γ2 receptors

Abstract

Pyrazoloquinolinones and pyrazolopyridinones represent the first prototypes of drugs exerting benzodiazepine-like modulatory effects via the α+β- interface of GABAA receptors. The discovery of modulators with functional subtype selectivity at this class of binding sites provides a highly useful tool for the investigation of α6β2/3γ2 receptor function, and may lead to novel therapeutic principles.