Safinamide (FCE-26743) is a reversible and selective monoamine oxidase B (IC50 0.098μM) inhibitor, reducing the degradation of dopamine, and a glutamate release inhibitor (IC50 8μM). It also inhibits dopamine reuptake. Safinamide also blocks sodium and calcium channels. Potential additional uses of Safinamide might be Parkinson's disease, restless leg syndrome and epilepsy.

Safinamide (1–300 µM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When the holding potential is depolarized to -53 mV, the inhibitory effect of safinamide with a lower IC50 value (8 µM) in rat cortical neurons [1].

Daily intraperitoneal injections of Safinamide 1mg/kg were administered for 14 days and the treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice .Safinamide (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release in vivo [2].