产品信息
抗原名称
MAO-B
商品描述
Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration.
分子量
302.34
纯度
>98%
可溶性
10 mM in DMSO
In vitro(体外研究)
The antiparkinson mechanism of safinamide is through reversible inhibition of selective MAO-B, thus reducing the degradation of dopamine. It inhibits glutamate release and dopamine reuptake in the brain. Safinamide also blocks sodium and calcium channels.
In vivo(体内研究)
Safinamide is absorbed quickly, with a bioavailability of 95%, and a demonstrated time to maximum plasma concentration of 1.8-2.8 hours. It exhibits extensive extravascular distribution with a volume of distribution of approximately 165 L. Safinamide does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. Safinamide is mediated by cytochrome P450 (CYP) 3A4 isoenzymes. It is 88% to 90% plasma protein-bound and is primarily eliminated through the kidneys (approximately 76%) in the form of its metabolites, with an elimination half-life of 20 to 30 hours. About 1.5% of safinamide is found excreted in the feces. Safinamide exhibits linear pharmacokinetics after oral administration of 50 mg to 300 mg (three times the maximum recommended daily dose) with a steady state reached within five to six days.
背景
别名
EMD 1195686; FCE 26743; EMD-1195686; EMD1195686; FCE-26743
分子式
C17H19FN2O2
CAS号
133865-89-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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