Potently (low nM) enhances GABA-evoked currents mediated by α4β3δ receptors. It has little effect on GABA responses mediated by α4β3 2 receptors. At similar concentrations, DS1 directly activates this receptor and is the most potent known agonist of α4β3δ receptors. This compound has an opportunity to be become an agonist golden stardard for δ-GABAA receptors.