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120014-06-4 Donepezil 120014-06-4 Donepezil
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Product name |
Donepezil |
CAS No. |
120014-06-4 |
Molecular Formula |
C24H29NO3 |
Molecular Weight |
379.49 |
Quality Standard |
99% up by HPLC |
Appearance |
White powder |
COA of Donepezil |
ITEMS |
SPECIFICATIONS |
RESULTS |
APPEARANCE |
WHITE OR ALMOST WHITE CRYSTALLINE POWDER |
CONFORMS |
SOLUBILITY |
TO MATCH WORKING STANDARD |
CONFORMS |
IDENTIFICATION |
1) BY UV ABSORPTION,TO MATCH WORKING STANDARD 2) BY IR ABSORPTION,TO MATCH WORKING STANDARD
|
CONFORMS
CONFORMS |
MELTING POINT |
86-90℃ |
87.5-88.5℃ |
RELATED SUBSTANCE |
||
TOTAL |
≤1.0% |
0.14% |
SINGLE IMPURITY (UNKNOWN) |
≤0.80% |
<0.8% |
LOSS ON DRYING |
≤1.0% |
0.3% |
RESIDUE ON IGNITION |
≤0.10% |
0.02% |
HEAVY METAL |
≤10 PPM |
<10 PPM |
ASSAY |
≥99.0% |
99.87% |
CONCLUSION |
CONFORMS TO THE ENTERPRISE STANDARD |
Usage |
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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