Molecular tools for GABA_A receptors: High affinity ligands for β1-containing subtypes.

ABSTRACT: γ-Aminobutyric acid type A (GABA_A) receptors are pentameric GABA-gated chloride channels that are, in mammalians, drawn from a repertoire of 19 different genes, namely α1-6, β1-3, γ1-3, δ, ε, θ, π and ρ1-3. The existence of this wide variety of subunits as well as their diverse assembly into different subunit compositions result in miscellaneous receptor subtypes. In combination with the large number of known and putative allosteric binding sites, this leads to a highly complex pharmacology. Recently, a novel binding site at extracellular α+/β- interfaces was described as the site of modulatory action of several pyrazoloquinolinones. In this study we report a highly potent ligand from this class of compounds with pronounced β1-selectivity that mainly lacks α-subunit selectivity.

SUBMITTER: Simeone X 

PROVIDER: S-EPMC5516028 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature