Safinamide mesylate_product_DataBase

Bioactivity	Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM)[1]. Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al[2][3].
Invitro	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[1].
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[3].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[3].
Name	Safinamide mesylate
CAS	202825-46-5
Formula	C18H23FN2O5S
Molar Mass	398.45
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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]. C Caccia, et al.Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23. [3]. Michele Morari, et al. Safinamide Differentially Modulates In Vivo Glutamate and GABA Release in the Rat Hippocampus and Basal Ganglia.J Pharmacol Exp Ther. 2018 Feb;364(2):198-206.

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Safinamide mesylate

CAS: 202825-46-5 F: C18H23FN2O5S W: 398.45