GABAA receptor modulator-13 is an orally active compound capable of crossing the blood-brain barrier, functioning as an α4β1δ GABAA receptor modulator (IC50= 9.02 μM). It reduces GABA-induced currents and destabilizes the M2-M3 loop of the α4β1δ GABAA receptor transmembrane domain, while showing selectivity for GABAA receptor subtypes containing γ2 and α6β3δ subtypes. This compound is useful for researching neurological disorders associated with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy.