The role of loops B and C in determining the potentiation of GABA_A receptors by midazolam.

ABSTRACT: Many benzodiazepines are positive allosteric modulators (PAMs) of GABA_A receptors that cause sedation, hypnosis, and anxiolysis. Benzodiazepines bind GABA_A receptors at the extracellular interface of the α and γ subunits. Within the α subunit, the benzodiazepine binding site is defined by three highly conserved structural loops, loops A-C. Although previous mutagenesis studies have identified His102 in Loop A as important for benzodiazepine modulation of GABA_A receptors, the functional roles of many of the other conserved residues in loops A-C remain incompletely understood. In this study, we made single mutations in loops A-C of the benzodiazepine binding-site across all six α subunits. We used whole-cell patch clamp recording to measure the functional eff

SUBMITTER: Moody OA 

PROVIDER: S-EPMC6234229 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature