| CAS NO: | 120011-70-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 416 |
|---|---|
| Formula | C24H29NO3.HCl |
| CAS No. | 120011-70-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: <1 mg/mL |
| Water: 5 mg/mL (12.01 mM) | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | 30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL |
| Synonyms | E-2020; E2020; Aricept; E 2020; Donepezil HCl |
| In Vitro | In vitro activity: Donepezil 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. 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. Kinase Assay: Donepezil HCL is a piperidine-class AChE inhibitor containing an N-benzylpiperdine and an indanone moiety, which confers it a longer and more selective action against AchE as compared to BuChE (IC50: 7.4 μM). |
|---|---|
| In Vivo | 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. When administered separately in vivo, 5-HT(4) receptor inducer, RS67333 (0.3 and 1 mg/kg) and Donepezil (1 mg/kg) improves recognition performances compared to saline treated mice, while co-administration of subactive doses of RS67333 (0.1mg/kg) and Donepezil (0.3 mg/kg) improves memory. However, this improvement is prevented if a 5-HT(4)R antagonist (GR125487, 10 mg/kg) is also administered. |
| Animal model | Rats |
| Formulation & Dosage | 1 mg/kg |
| References | Neuropharmacology. 1999 Jan;38(1):181-93; CNS Neurosci Ther. 2012 Feb;18(2):185-7. |
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