Donepezil

製品コードS5073 バッチS507301

印刷

化学情報

Chemical Structure Synonyms Aricept, Donepezilo Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H29NO3
分子量 379.49 CAS No. 120014-06-4
Solubility (25°C)* 体外 DMSO 75 mg/mL (197.63 mM)
 
 
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Donepezil（アリセプト、ドネペジロ）は、アルツハイマー型認知症の軽度から中等度の治療に使用される、ピペリジンベースの強力で特異的な非競合的可逆的アセチルコリンエステラーゼ（AChE）阻害剤です。
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.
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.

プロトコル(参考用のみ)

細胞アッセイ 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.
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

参考

  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2654795/
  • https://pubmed.ncbi.nlm.nih.gov/16421021/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Enhancing striatal acetylcholine facilitates dopamine release and striatal output in parkinsonian mice [ Cell Biosci, 2024, 14(1):146] PubMed: 39627827
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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。