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Donepezil
別名：Aricept, Donepezilo
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.
CAS No. 120014-06-4
文献中Selleckの製品使用例（5）
製品安全説明書
現在のバッチを見る：
S507301
DMSO]
75 mg/mL]
false]
]
]
false]
]
]
false
純度：
99.96%
99.96
Donepezil関連製品
シグナル伝達経路
AChR阻害剤の選択性比較
生物活性
| 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. | ||
|---|---|---|---|
| Targets |
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| In Vitro | ||||
| 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 this compound induces a concentration-dependent inhibition of cell proliferation unrelated to muscarinic or nicotinic receptor blockade or apoptosis. This chemical 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, it increases action potential-dependent dopamine release and modulates nicotinic receptors of substantia nigra dopaminergic neurons. | |||
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| 細胞実験 | 細胞株 | retinal ganglion cells (RGCs) | ||
| 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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| In Vivo | ||
| 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. This compound is metabolized in the liver via the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related enzymes). In animals, it is found unchanged in brain, and no metabolites are detected in the nervous tissue. In plasma, urine, and bile, most of its metabolites are O-glucuronides. After oral ingestion, peak plasma concentrations are achieved in 3-5 hours and its absortion is not affected by food. This chemical has linear pharmacokinetics over a dose range of 1-10 mg/day. 96% of circulating donepezil is protein bound. | |
|---|---|---|
| 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 |
| 投与量 | 1.5 mg/kg | |
| 投与経路 | oral | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06373094 | Not yet recruiting | Alzheimer Disease |
Shanghai Synergy Pharmaceutical Sciences Co. Ltd.|Zhejiang Huahai Pharmaceutical Co. Ltd. |
June 1 2024 | Phase 1 |
| NCT05345509 | Recruiting | Alzheimer Disease |
Inventage Lab. Inc. |
April 1 2023 | Phase 1|Phase 2 |
| NCT04308304 | Completed | Alzheimer''s Disease |
Merck Sharp & Dohme LLC |
February 16 2021 | Phase 1 |
| NCT04617782 | Completed | Healthy Subjects |
Corium Inc. |
December 8 2020 | Phase 1 |
|
化学情報
| 分子量 | 379.49 | 化学式 | C24H29NO3 |
| CAS No. | 120014-06-4 | SDF | -- |
| Smiles | COC1=C(C=C2C(=C1)CC(C2=O)CC3CCN(CC3)CC4=CC=CC=C4)OC | ||
| 保管 | |||
|
In vitro |
DMSO : 75 mg/mL ( (197.63 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | |||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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