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Donepezil 120014-06-4

Donepezil 120014-06-4

99% up by HPLC
  • Product Details

Product Information


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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