Function: Hormones and Regulation of Endocrine Function of Drug, Antibiotic and Antimicrobial Agents, Original Drug Resistant Microbes, Immune System Drugs, Specialist Drugs, Drug Detoxification, Diagnostic Agents, Nervous System Drugs, Blood System Agents, Central Nervous System Agents, Antidote, Respiratory System Agents, Disinfectant and Preservatives
Certification: GMP, Reach, FDA
Grade Standard: Medicine Grade
Type: Chemical Reagent
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 is slowly absorbed from the gastrointestinal tract in vivo, with a terminal half-life of 50-70 hours in young volunteers, and a half-life of more than 100 hours in the 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. Uses Donepezil hydrochloride monohydrate is a centrally reversible acetylcholinesterase inhibitor.