For research use only.
CAS No. 120011-70-3
Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
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Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
J Am Heart Assoc 2014 3(3), e000804. Donepezil HCl purchased from Selleck.
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Choose Selective AChR Inhibitors
|Description||Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.|
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. 
|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. |
|In vitro||Water||5 mg/mL (12.01 mM)|
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30% propylene glycol, 5% Tween 80, 65% D5W
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04308304||Not yet recruiting||Drug: MK-1942|Drug: Donepezil|Drug: Placebo||Alzheimer''s Disease||Merck Sharp & Dohme Corp.||February 15 2021||Phase 1|
|NCT03932916||Recruiting||Drug: Donepezil pamoate|Drug: Donepezil Hydrochloride||AD||Shanghai Synergy Pharmaceutical Sciences Co. Ltd.||July 2 2019||Phase 1|
|NCT03905096||Completed||Drug: BI 425809|Drug: Donepezil||Healthy||Boehringer Ingelheim||April 12 2019||Phase 1|
|NCT03438604||Completed||Drug: Donepezil TDS||Alzheimer''s Disease||Corium International Inc.||February 13 2018||Phase 1|
|NCT03432195||Completed||Drug: Donepezil TDS||Alzheimer''s Disease||Corium International Inc.||January 31 2018||Phase 1|
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