产品
编 号:F067873
分子式:C24H30ClNO3
分子量:415.95
产品类型
结构图
CAS No: 120011-70-3
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生物活性:
Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
体内研究:
Donepezil 处理 (3 mg/kg) 显著阻止东莨菪碱诱导的小鼠记忆障碍的进展。 Donepezil Hydrochloride 的药代动力学研究表明,口服处理 (3 和 10 mg/kg) 后,Donepezil Hydrochloride 的平均血浆峰值浓度分别约为 1.2 h 和 1.4 h;绝对生物利用度计算为 3.6%。Animal Model:Male imprinting control region (ICR) mice (6 weeks old)
Dosage:3-10 mg/kg
Administration:Administered orally
Result:Pretreatment with 3–10 mg/kg ameliorated scopolamine-induced memory impairment.
Animal Model:Hairless rats with an average weight of 300 g
Dosage:3 and 10 mg/kg (Pharmacokinetic Analysis)
Administration:Administered orally; and blood (250 μL) was collected through the tail vein
Result:After oral treatment (3 and 10 mg/kg), a maximum concentration (Cmax) was reached after approximately 1.2 ± 0.4 h and 1.4 ± 0.5 h, respectively, and gradually decreased.
体外研究:
Donepezil Hydrochloride 的神经保护机制与增强 Akt 和 GSK-3β 的磷酸化,降低tau和糖原合成酶的磷酸化有关。