产品
编 号：F124655
分子式：C17H19FN2O2
分子量：302.34
分子式：C17H19FN2O2
分子量：302.34
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
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询价
结构图
CAS No: 133865-89-1
产品详情
生物活性：
Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM). Safinamide 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 has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
体内研究：
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 Model
Dosage:90 mg/kg
Administration:Intraperitoneal?injection; once daily; 14 days
Result:Significantly decreased infarction volume in brain areas.
体外研究：
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 is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM). Safinamide 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 has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
体内研究：
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 Model
Dosage:90 mg/kg
Administration:Intraperitoneal?injection; once daily; 14 days
Result:Significantly decreased infarction volume in brain areas.
体外研究：
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.
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