Zhengzhou Yuanli Biological Technology Co., Ltd.
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Donepezil is a reversible acetylcholinesterase inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine. It has a half-life in circulation of about 70 hours. As acetylcholine modulates plasticity, excitability, and arousal in the central nervous system, donepezil is commonly used in the treatment of Alzheimer’s disease to improve cognition, memory, and behavior. In this way, it is intended to prevent or reverse dementia. Studies on these effects have been equivocal, indicating that more research into the therapeutic potential of donepezil is warranted.
Molecular Formula:
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C24H29NO3
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CAS No.:
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120014-06-4
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Appearance:
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White Solid
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Assay:
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99%
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Synonyms:
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2,3-Dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one;(±)-E 2020; 1-Benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine; Donepezil; Neuripezil; Tonizep
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Sinoway Industrial Co.Ltd.
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Product name
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Donepezil
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CAS No.
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120014-06-4
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Molecular Formula
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C24H29NO3
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Molecular Weight
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379.49
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Quality Standard
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99% up by HPLC
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Appearance
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White powder
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ITEMS
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SPECIFICATIONS
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RESULTS
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APPEARANCE
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WHITE OR ALMOST WHITE CRYSTALLINE POWDER
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CONFORMS
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SOLUBILITY
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TO MATCH WORKING STANDARD
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CONFORMS
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IDENTIFICATION
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1) BY UV ABSORPTION,TO MATCH WORKING STANDARD
2) BY IR ABSORPTION,TO MATCH WORKING STANDARD
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CONFORMS
CONFORMS
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MELTING POINT
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86-90℃
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87.5-88.5℃
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RELATED SUBSTANCE
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TOTAL
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≤1.0%
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0.14%
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SINGLE IMPURITY (UNKNOWN)
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≤0.80%
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<0.8%
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LOSS ON DRYING
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≤1.0%
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0.3%
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RESIDUE ON IGNITION
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≤0.10%
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0.02%
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HEAVY METAL
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≤10 PPM
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<10 PPM
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ASSAY
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≥99.0%
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99.87%
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CONCLUSION
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CONFORMS TO THE ENTERPRISE STANDARD
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Function of Donepezil
Donepezil is a potent, reversible, specific and noncompetitive acetylcholinesterase (AChE) inhibitor for the treatment of mild to moderate dementia.
In vitro studies:
Donepezil has a reversible and non-competitive inhibitory effect on AChE. It is 500-1000-fold more selective for AChE than for BuChE. Short- and long-term drug exposure to human SH-SY5Y neuroblastoma cells induces a concentration-dependent inhibition of cell proliferation independent of muscarinic or nicotinic receptor blockade and apoptosis. Donepezil reduces the number of cells in the S-G2/M phase of the cell cycle, increases the number in the G0/G1 phase, and reduces the expression of two cyclins in the G1/S and G2/M transitions: cyclinE and cyclinB. At the same time, it also increased the expression of the cell cycle repressor p21. In addition, donepezil increases action potential-dependent dopamine release and modulates nicotinic receptors in substantia nigra dopaminergic neurons.
In vivo studies:
Donepezil absorbs Chemicalbook slowly from the gastrointestinal tract in vivo, with a terminal half-life of 50-70 hours in young volunteers and more than 100 hours in elderly. After extensive hepatic metabolism, the parent compound is 93% bound to plasma proteins. Donepezil is metabolized in the liver by the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, donepezil was unchanged in the brain and no metabolites were found in neural tissue. In plasma, urine and bile, most donepezil metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are reached within 3-5 hours, and its absorption is not affected by food. Donepezil has linear pharmacokinetics in the concentration range of 1-10 mg/day. 96% of circulating donepezil is protein bound.
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