Zuranolone (SAGE-217) is an orally active, positive allosteric modulator of the GABAA receptor with EC50 of 375/299 nM (α1β2γ2/α4β3δ).
Zuranolone (SAGE-217)shows an IC50 of 7 nM in in the [35S]TBPS binding assays.
Zuranolone (SAGE-217) displays remarkably selectivity against a broad panel of enzymes and receptors (78 targets) in a pan-screen.
Acute administration of SAGE-217 (0.3-10 mg/kg, ip) effectively reduced pentylenetretazol (PTZ)-induced seizures in mice, as well as producing a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model.
