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Synonyms | Aricept, Donepezilo | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H29NO3 |
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分子量 | 379.49 | CAS No. | 120014-06-4 | |
Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (197.63 mM) | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Donepezil (Aricept, Donepezilo) is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type. |
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in vitro | Donepezil has reversible and noncompetitive inhibition effects on AChE. It has 500-1000-fold more selective for AChE over butyrylcholinesterase (BuChE). Short- and long-exposure of SH-SY5Y human neuroblastoma cells to donepezil induces a concentration-dependent inhibition of cell proliferation unrelated to muscarinic or nicotinic receptor blockade or apoptosis. Donepezil reduces the number of cells in the S-G2/M phases of the cell cycle, increases the G0/G1 population, and reduces the expression of two cyclins of the G1/S and G2/M transitions, cyclin E and cyclin B, in parallel with an increase in the expression of the cell cycle inhibitor p21. In addition, donepezil increases action potential-dependent dopamine release and modulates nicotinic receptors of substantia nigra dopaminergic neurons[1]. |
in vivo | Donepezil is slowly absorbed from the gastrointestinal tract and has a terminal elimination half-life of 50-70 hours in young volunteers (>100 hours in elderly subjects). After extensive metabolization in the liver, the parent compound is 93% bound to plasma proteins. Donepezil is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, donepezil is found unchanged in brain, and no metabolites are detected in the nervous tissue. In plasma, urine, and bile, most donepezil metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are achieved in 3-5 hours and its absortion is not affected by food. Donepezil has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound[1]. |
細胞アッセイ | 細胞株 | retinal ganglion cells (RGCs) |
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濃度 | 100 nM-10 μM | |
反応時間 | 3 days | |
実験の流れ | RGC survival after exposure to each reagent (glutamate, donepezil, tacrine, galanthamine, and HA14-1) is measured by calcein-AM staining after 3 days in culture, Briefly, cells are incubated in 1 μM calcein-AM in PBS for 15 minutes at 37℃. After the medium is replaced with fresh PBS, cells are examined under a fluorescence microscope using a fluorescein filter. The total number of surviving RGCs defined as cells with a calcein-AM stained cell body and a process extending at least two cell diameters from the cell body is counted in each well. The number of surviving RGCs without any drug served as a control. |
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動物実験 | 動物モデル | Age-matched (10-12 weeks old, 21–24 g) male C57BL/6 wild-type and CGRP(−/−) mice |
投薬量 | 1.5 mg/kg | |
投与方法 | oral |
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Inhibition of Th17 cells by donepezil ameliorates experimental lung fibrosis and pulmonary hypertension [ Theranostics, 2023, 13(6):1826-1842] | PubMed: 37064881 |
Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain [ Front Bioeng Biotechnol, 2022, 10:855755] | PubMed: 35372313 |
Donepezil Ameliorates Pulmonary Arterial Hypertension by Inhibiting M2-Macrophage Activation [ Front Cardiovasc Med, 2021, 8:639541] | PubMed: 33791350 |
Entry of therapeutics into the brain: Influence of exposed polarity calculated in silico and measured in vitro by supercritical fluid chromatography. [ Int J Pharm, 2019, 560:294-305] | PubMed: 30771469 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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