Safinamide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 MAO-B 抑制剂，IC50 为 98 nM。

A potent and selective inhibitor of MAO-B with IC50 of 98 nM; displays >5,000-fold selectivity over MAO-A; also inhibits glutamate release and dopamine reuptake, inhibits voltage-dependent Na+ and Ca2+ channels; is used for treatment ofParkinson's disease.Parkinson's Disease Approved.

Safinamide (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 with a lower IC50?value (8?μM) in rat cortical neurons.

Safinamide (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 (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 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 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. Animal Model:Focal cerebral ischemia C57/BL6 male mouse ModelDosage:90 mg/kg Administration:Intraperitoneal?injection; once daily; 14 days Result:Significantly decreased infarction volume in brain areas.

EMD-1195686 | FCE-26743

Metabolic Enzyme/Protease

MAO

MAO

Neurological Disease

Parkinson Disease

133865-89-1

302.3434

C17H19FN2O2

>98% (HPLC)

10 mM in DMSO

CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F

Propanamide, 2-[[[4-[(3-fluorophenyl)methoxy]phenyl]methyl]amino]-, (2S)-

(-20℃)

With Ice Pack

≥ 2 years