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Donepezil

CAS No. : 120014-06-4

MCE 站：Donepezil

产品活性：Donepezil (E2020 free base) 是 AChE 抑制剂，对牛 AChE 和人 AChE 的 IC₅₀ 分别为 8.12 nM 和 11.6 nM。

研究领域：Neuronal Signaling

作用靶点：Cholinesterase (ChE)

In Vitro: Donepezil (E2020 free base) inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity. Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation ａnd tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/kg following oral administration.
A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular ａnd cerebrovascular diseases.

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