Safinamide

Safinamide 是一种强效、选择性和可逆的单胺氧化酶 B (MAO-B) 抑制剂 (IC50=0.098 μM)，优于 MAO-A (IC50=580 μM)。

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10mg

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50mg

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Background

Safinamide (FCE 26743) selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A[1].

Safinamide (FCE 26743) is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. In addition, Safinamide (FCE 26743) is voltage-dependent sodium and calcium channel blocker. Safinamide (FCE 26743) appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals[1].

参考文献:
[1]. Leonetti F, et al. Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase. J Med Chem, 2007, 50(20), 4909-4916.
[2]. Schapira AH.Safinamide in the treatment of Parkinson's disease.Expert Opin Pharmacother. 2010 Sep;11(13):2261-8.
[3]. Onofrj M, et al. An expert opinion on safinamide in Parkinson's disease.Expert Opin Investig Drugs. 2008 Jul;17(7):1115-25.
[4]. Chazot PL.Safinamide for the treatment of Parkinson's disease, epilepsy and restless legs syndrome.Curr Opin Investig Drugs. 2007 Jul;8(7):570-9.
[5]. Dal Bo L, et al. Bioassay of safinamide in biological fluids of humans and various animal species.Arzneimittelforschung. 2006;56(12):814-9.http://www.ncbi.nlm.nih.gov/pubmed/17260668