Ganaxolone is a synthetic neurosteroid which functions as a stereoselective modulator of GABAA receptors. Studies indicate that ganaxolone enhances GABA-evoked chloride currents in Xenopus oocytes. It is known that the compound modulates GABAA receptors by inhibiting GABAA receptor-chloride channel ligand binding and enhancing ligand binding at the benzodiazepine site. Alternatively, ganaxolone increases serotonergic neuron firing in rats after 3 to 7 days. Studies conducted on animal seizure models demonstrate that ganaxolone displays anticonvulsant effects. Furthermore, ganaxolone suppresses seizures in mice induced by maximal electroshock (ED50 of 29.7 mg/kg i.p.).
