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Submit ReviewDonepezil hydrochloride is a potent and selective acetylcholinesterase inhibitor (IC50 = 5.7 nM). In animal models of Alzheimer's disease, Donepezil reduces brain tissue Aβ protein and plaque deposition, restores normal glucose metabolism, reduces neuroinflammation and rescues cognitive dysfunction and memory deficits. The pro-cognitive effects are potentiated by combination with Mefloquine (Cat. No. 6819). In vitro Donepezil reduces LPS-induced inflammation and protects against mitochondrial membrane potential damage.
分子量 | 415.95 |
公式 | C24H29NO3.HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 120011-70-3 |
PubChem ID | 5741 |
InChI Key | XWAIAVWHZJNZQQ-UHFFFAOYSA-N |
Smiles | O=C2C(CC3CCN(CC4=CC=CC=C4)CC3)CC1=CC(OC)=C(OC)C=C12.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 20.8 | 50 |
以下数据基于产品分子量 415.95。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.81 mL | 24.04 mL | 48.08 mL |
2.5 mM | 0.96 mL | 4.81 mL | 9.62 mL |
5 mM | 0.48 mL | 2.4 mL | 4.81 mL |
25 mM | 0.1 mL | 0.48 mL | 0.96 mL |
参考文献是支持产品生物活性的出版物。
Sugimoto et al (1995) Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. J.Med.Chem. 38 4821 PMID: 7490731
Kryger et al (1999) Structure of acetylcholinesterase complexed with E2020 (Aricept): implications for the design of new anti-Alzheimer drugs. Structure 7 297 PMID: 10368299
Sugimoto et al (2000) Donepezil hydrochloride (E2020) and other acetylcholinesterase inhibitors. Curr.Med.Chem. 7 303 PMID: 10637367
Romberg et al (2011) Impaired attention in the 3xTgAD mouse model of Alzheimer's disease: rescue by donepezil (Aricept). J.Neurosci. 31 3500 PMID: 21368062
Droguerre et al (2020) Efficacy of THN201, a combination of donepezil and mefloquine, to reverse neurocognitive deficits in Alzheimer's disease. Front.Neurosci. 14 PMID: 32612499
Hugon et al (2022) Impact of donepezil on brain glucose metabolism assessed using [18F]2-fluoro-2-deoxy-D-glucose positron emission tomography imaging in a mouse model of Alzheimer's disease induced by intracerebroventricular injection of amyloid-beta peptid Front.Neurosci. 16 PMID: 35281502
Kim et al (2021) Donepezil regulates LPS and Aβ-stimulated neuroinflammation through MAPK/NLRP3 inflammasome/STAT3 signaling. Int.J.Mol.Sci. 22 10637 PMID: 34638977
If you know of a relevant reference for Donepezil hydrochloride, please let us know.
关键词: Donepezil hydrochloride, Donepezil hydrochloride supplier, acetylcholinesterase, ache, selective, potent, inhibitors, inhibits, E2020, neurodegeneration, alzheimers, amyloid, beta, AB, neuroinflammation, Aβ, E, 2020, Cholinesterases, 4385, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Donepezil hydrochloride 的部分引用包括:
Morris et al (2015) Network dysfunction in α-synuclein transgenic mice and human Lewy body dementia. Ann Clin Transl Neurol 2 1012 PMID: 26732627
Mercedes et al (2017) The proof-of-concept of ASS234: Peripherally administered ASS234 enters the central nervous system and reduces pathology in a male mouse model of Alzheimer disease. J Psychiatry Neurosci 42 59-69 PMID: 27636528
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
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