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Donepezil hydrochloride_Molecular_structure_CAS_120011-70-3)
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Donepezil hydrochloride

Catalog No. S2462 Name Selleck Chemicals
CAS Number 120011-70-3 Website http://www.selleckchem.com
M. F. C24H30ClNO3 Telephone (877) 796-6397
M. W. 415.9529 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 73033

SYNONYMS

IUPAC name
2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one hydrochloride
IUPAC Traditional name
donepezil hydrochloride
Synonyms
Aricept

DATABASE IDS

CAS Number 120011-70-3

PROPERTIES

Salt Data hydrochloride
Storage Condition -20°C

DETAILS

Description (English)
Research Area
Description Neurological Disease
Biological Activity
Description Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
Targets bAChE hAChE
IC50 8.12 nM 11.6 nM [1]
In Vitro 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. [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]
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. [2]. 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. [4]
Clinical Trials Donepezil is currently being evaluated in Phase III clinical trials for Parkinson' s disease (PD) patients with dementia.
Features
Protocol
Kinase Assay [1]
AChE inhibitory activity PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum (for the murine PDGF receptor) for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/ml) at 4 °C for 10 minutes, different concentrations of the drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-32P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
Animal Study [2]
Animal Models Male Lister Hooded rats
Formulation 0.9% w:v NaCl (saline)
Doses 18 μM/kg
Administration Administered via i.p. or p.o.
References
[1] Ogura H, et al. Methods Find Exp Clin Pharmacol. 2000, 22(8), 609-613.
[2] Snape MF, et al. Neuropharmacology. 1999, 38(1), 181-193.
[3] Huang ZH, et al. CNS Neurosci Ther. 2012, 18(2), 185-187.
[4] Freret T, et al. Behav Brain Res. 2012 http://dx.doi.org/10.1016/j.bbr.2012.02.012.