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Safinamide mesylate

CAS No. : 202825-46-5

MCE 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 ?M)，对 MAO-A (IC₅₀=580 ?M) 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??M) 比静息电位 (IC₅₀=262 ?M) 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??M) reduces the amplitude of the peak sodium currents in a concentration-dependent manner.?When currents are stimulated to a?V_test?of +10 mV from a?V_h?of -110 mV, the IC₅₀?value was 262??M. When the holding potential is depolarized to -53 mV, the inhibitory effect of Safinamide mesylate with a lower IC₅₀?value (8??M) 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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