Selective modulation of different GABAA receptor isoforms by diazepam and etomidate in hippocampal neurons.

Diazepam modulation of native γ2-containing GABA(A) (γGABA(A)) receptors increases channel conductance by facilitating protein interactions involving the γ2-subunit amphipathic (MA) region, which is found in the cytoplasmic loop between transmembrane domains 3 and 4 (Everitt et al., 2009). However, many drugs, predicted to act on different GABA(A) receptor subtypes, increase channel conductance leading us to hypothesize that conductance variation in GABA(A) receptors may be a general property, mediated by protein interactions involving the cytoplasmic MA stretch of amino acids.