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.

MAO-B:98 nM, MAO-A:580 μM

Safinamide（1-300 µM）以浓度依赖的方式减少峰值钠电流的幅度。当保持电位去极化至-53 mV时，safinamide在大鼠皮质神经元中展现出较低的IC50值（8 µM）的抑制效果[1]。

每日通过腹腔注射施用Safinamide（1mg/kg），连续14天，此治疗方式在小鼠中脑缺血（MCAO）前显著减轻了因MCAO引起的脑梗死体积、神经功能缺失、脑-血屏障(BBB)的破坏，同时明显降低了紧密连接蛋白occludin与ZO-1的表达受损。此外，Safinamide（腹腔注射；剂量分别为5 mg/kg、15 mg/kg和30 mg/kg）呈剂量依赖性抑制经由veratridine引起的γ-氨基丁酸（GABA）释放和谷氨酸（Glu）释放[2]。