assay
≥98% (HPLC)
form
solid
color
white
solubility
H2O: 16 mg/mL
General description
A brain-penetrating, reversible, and selective piperidine acetylcholinesterase inhibitor with an IC50 = 5.7 nM in vitro, and a 1250-fold selectivity over butylcholinesterase. In vivo, there is a marked and significant increase in acetylcholine content in rat cerebral cortex at a p.o. dose of 5 mg/kg. Furthermore, it inhibits brain cholinesterase (ChE) dose-dependently (ID50 = 2.6 mg/kg) without any marked adverse effects on ChE in the heart and small intestine. In a clinical trial, it has been shown to reduce AChE activity by 63.7% for the 5mg/d group and 77.3% for the 10mg/d group in Alzheimer′s disease patients. Its off-target effects are indicated with the reversibly of inhibited voltage-gated K+/Na+ channels.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
存储类别
10-13 - German Storage Class 10 to 13
法规信息
监管及禁止进口产品
此项目有
S L Rogers et al.
Neurology, 50(1), 136-145 (1998-01-27)
The efficacy and safety of donepezil as a treatment for patients with mild to moderate Alzheimer's disease (AD) was investigated in a multicenter, double-blind study. Patients were randomly assigned to treatment with placebo (n = 162), 5 mg/d donepezil (n
H Sugimoto et al.
Journal of medicinal chemistry, 38(24), 4821-4829 (1995-11-24)
Following the discovery of a new series of anti-acetylcholinesterase (anti-AChE) inhibitors such as 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine (1), we reported that its rigid analogue, 1-benzyl-4-(2-isoindolin-2-ylethyl)piperidine (5), had more potent activity. We have extended the structure-activity relationship (SAR) study for the rigid analogue and
Bo Yu et al.
European journal of pharmacology, 508(1-3), 15-21 (2005-02-01)
Donepezil (E2020) is a novel cholinesterase inhibitor for the treatment of Alzheimer's disease. Recent studies show that it may act on targets other than acetylcholinesterase in the brain. In the present study, the actions of donepezil on voltage-gated Na+ and
H Ogura et al.
Nihon yakurigaku zasshi. Folia pharmacologica Japonica, 115(1), 45-51 (2000-07-06)
One of the most consistent changes associated with Alzheimer's disease (AD) is a deficit in central cholinergic neurotransmission. Donepezil hydrochloride (DPZ), a novel class of cholinesterase (ChE) inhibitors, inhibits degradation of acetylcholine (ACh) and activates central cholinergic system. In in
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