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120014-06-4

120014-06-4 structure
120014-06-4 structure
  • Name: donepezil
  • Chemical Name: donepezil
  • CAS Number: 120014-06-4
  • Molecular Formula: C24H29NO3
  • Molecular Weight: 379.492
  • Catalog: API Nervous system medication Brain metabolism regulating drug
  • Create Date: 2018-07-05 11:50:31
  • Modify Date: 2024-01-02 08:26:21
  • Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.Target: AChEDonepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively [1]. 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. 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 [2]. 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 [3].

Name donepezil
Synonyms 2-((1-Benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one
2,3-Dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one
5,6-Dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-2,3-dihydro-1H-inden-1-one
n-1-one
2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one
1H-Inden-1-one, 2,3-dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-
Aricept
Donepezil hydrochloride monohydrate
(±)-E-2020
2-[(1-Benzyl-4-piperidinyl)methyl]-5,6-dimethoxy-1-indanone
2-[(1-Benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one
MFCD00912833
donepezil
1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE
5,6-Dimethoxy-2,3-dihydro-1H-inden-1-one
Donezepil
2-[(1-Benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-on
Donepezil Base
Description Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.Target: AChEDonepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively [1]. 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. 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 [2]. 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 [3].
Related Catalog
References

[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.

Density 1.1±0.1 g/cm3
Boiling Point 527.9±50.0 °C at 760 mmHg
Melting Point 207ºC
Molecular Formula C24H29NO3
Molecular Weight 379.492
Flash Point 273.1±30.1 °C
Exact Mass 379.214752
PSA 38.77000
LogP 4.71
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.578
Water Solubility 2.931 mg/L
Hazard Codes Xi: Irritant;
Risk Phrases R36/37/38
Safety Phrases 26-36
RIDADR UN 2811