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Donepezil

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Chemical Structure| 120014-06-4 同义名 : 多萘哌齐碱 ;E2020 free base;Aricept;HSDB 7743;Donepezilo
CAS号 : 120014-06-4
货号 : A127504
分子式 : C24H29NO3
纯度 : 98%
分子量 : 379.492
MDL号 : -
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(92.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AChE

    hAChE, IC50:11.6 nM

    bAChE, IC50:8.12 nM
描述 Donepezil, as a acetylcholinesterase (AChE) inhibitors, inhibits AChE activity thereby increasing the acetylcholine (ACh) levels. Pretreatment with donepezil suppressed the TNFα-induced sustained intracellular Ca2+ elevation in both rat HAPI and mouse primary microglial cells[3]. Exposure to donepezil resulted in a rapid and reversible block of Kv1.5 currents, with an IC50 value of 72.5 μM. Donepezil can directly block Kv1.5 channels in its open and closed states[4]. Donepezil itself enhances neurogenesis and improves cognitive function following TBI(Traumatic Brain Injury), even when injury-induced neurogenesis was inhibited[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.35mL

5.27mL

2.64mL
参考文献

[1]Ogura H, Kosasa T, et al. Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitro. Methods Find Exp Clin Pharmacol. 2000 Oct;22(8):609-13.

[2]Snape MF, Misra A, 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 Jan;38(1):181-93.

[3]Haraguchi Y, Mizoguchi Y, Ohgidani M, Imamura Y, Murakawa-Hirachi T, Nabeta H, Tateishi H, Kato TA, Monji A. Donepezil suppresses intracellular Ca2+ mobilization through the PI3K pathway in rodent microglia. J Neuroinflammation. 2017 Dec 22;14(1):258. doi: 10.1186/s12974-017-1033-0. PMID: 29273047; PMCID: PMC5741946.

[4]Li K, Cheng N, Li XT. Inhibitory effects of cholinesterase inhibitor donepezil on the Kv1.5 potassium channel. Sci Rep. 2017 Feb 13;7:41509. doi: 10.1038/srep41509. PMID: 28198801; PMCID: PMC5304190.

[5]Yu TS, Kim A, Kernie SG. Donepezil rescues spatial learning and memory deficits following traumatic brain injury independent of its effects on neurogenesis. PLoS One. 2015 Feb 25;10(2):e0118793. doi: 10.1371/journal.pone.0118793. PMID: 25714524; PMCID: PMC4340948.