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MCE 国际站:Donepezil
中文名:多奈哌齐
CAS:120014-06-4
品牌:MedChemExpress (MCE)
存储条件:4°C, sealed storage, away from moisture and light
生物活性:Donepezil (E2020 free base) 是一种特异有效的 AChE 抑制剂,对牛 AChE 和人 AChE 的 IC50 分别为 8.12 nM 和 11.6 nM ,分别为[1]。
体外:Donepezil (E2020 free base) 以浓度依赖性方式抑制人 SHSY5Y 神经母细胞瘤细胞中卡巴胆碱刺激的细胞内 Ca2+ 浓度增加,表明 Donepezil 具有毒蕈碱拮抗剂活性。在大鼠中腹膜内给予多奈哌齐会产生剂量依赖性的流涎和震颤增加,这是明显的胆碱能行为体征,ED50 为 6 μmol/kg。口服给药后,发现多奈哌齐的 ED50 为 50 μmol/kg[2],效力稍差。最近的一项研究表明,Donepezil 可以保护人脐静脉内皮细胞 (HUVEC) 免受 H2O2 诱导的细胞损伤。这可能有助于作为心脑血管疾病中氧化应激的潜在疗法[3]。
热销产品:OAC1 | Etifoxine | AS-252424 | R59949 | Hematoporphyrin monomethyl ether | Propargyl-PEG2-acid | Conivaptan (hydrochloride) | Effusol | 4-Azidobutylamine | 3,4-Dicaffeoylquinic acid
研究领域:Neuronal Signaling
作用靶点:Cholinesterase (ChE)
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Ogura, H., et al., Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol, 2000. 22(8): p. 609-13.
[2]. Snape, M.F., et al., A comparative study in rats of the in vitro and in vivo pharmacology of the acetylcholinesterase inhibitors tacrine, donepezil and NXX-066. Neuropharmacology, 1999. 38(1): p. 181-93.
[3]. Huang, Z.H., et al., Donepezil protects endothelial cells against hydrogen peroxide-induced cell injury. CNS Neurosci Ther, 2012. 18(2): p. 185-7.
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