NCS-382 (sodium salt)

A GHBR antagonist (IC50s = 134.1 and 201.3 nM in isolated rat striatal and hippocampal membranes, respectively, in radioligand binding assays); selective for GHBR over GABA binding sites in rat brain synaptic membranes at 1 and 10 µM; decreases GHB-induced increases in inositol phosphate accumulation and cGMP levels in isolated rat hippocampal slices (IC50s = 8.6 and 30 µM, respectively); reduces GHB-induced increases in the time mice spent immobile in the forced swim test at 1.66 and 2.08 mmol/kg; decreases spike and wave discharges in audiogenic seizure-susceptible Swiss Rb mice, as well as a rat model of petit mal epilepsy, at 2.3 mmol/kg