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CAS No. : 202825-46-5
MCE 国际站:Safinamide mesylate
产品活性:Safinamide (FCE 26743; EMD 1195686) mesylate 是一种有效的、选择性的、可逆的单胺氧化酶 B (MAO-B) 的抑制剂 (IC50=0.098 µM),对 MAO-A (IC50=580 µM) 选择性较低。Safinamide mesylate 也阻断钠通道和调节谷氨酸 (Glu) 释放,在去极化时 (IC50= 8 µM) 比静息电位 (IC50=262 µM) 时,显示出更大的亲和力。Safinamide mesylate 具有神经保护作用,可用于帕金森病、缺血脑卒中等疾病的研究。
研究领域:Neuronal Signaling
作用靶点:Monoamine Oxidase
In Vitro: Safinamide mesylate (1-300 µM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When currents are stimulated to a Vtest of +10 mV from a Vh of -110 mV, the IC50 value was 262 µM. When the holding potential is depolarized to -53 mV, the inhibitory effect of Safinamide mesylate with a lower IC50 value (8 µM) in rat cortical neurons.
In Vivo: Safinamide mesylate (intraperitoneal injection; 90 mg/kg; once daily; 14 days) 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 mesylate (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. At the dose 30 mg/kg, Safinamide mesylate prevents the effect of veratridine both on Glu (treatment F1,8=1.31; time×treatment interaction F8,64=2.4) and GABA (treatment F1,8=4.04; time F8,64=3.76, time×treatment interaction F8,64=2.83) release.Safinamide mesylate causes a slight, albeit not significant, reduction of veratridine-stimulated Glu release at 0.5 mg/kg and full inhibition at 5 and 15 mg/kg in rat.
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