<p style=/line-height:25px/>Donepezil(E 2020) is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM, respectively.<br>Target: AChE<br>Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively [1]. Donepezil inhibits the carbachol-stimulated increase in intracellular Ca2+ concentration in human SHSY5Y neuroblastoma cells in a concentration dependent manner, indicating that Donepezil have muscarinic antagonist activity. Intraperitoneal administration of Donepezil in rats produces a dose dependent increase in salivation and tremor, which are overt cholinergic behavioural signs, with an ED50 of 6 μmol/kg. Donepezil is found to be somewhat less potent with a ED50 of 50 μmol/kg following oral administration [2]. A recent study shows that Donepezil can protect human umbilical vein endothelial cells (HUVECs) against H2O2-induced cell injury. This may be useful as a potential therapy for oxidative stress in cardiovascular and cerebrovascular diseases [3].<br></p>
| Catalog Number | I000736 |
| CAS Number | 120014-06-4 |
| Synonyms | Aricept® |
| Molecular Formula | C24H29NO3 |
| Purity | 95% |
| Target | AChE |
| Solubility | acetone: ~25 mg/ml |
| Storage | -20°C |
| InChIKey | ADEBPBSSDYVVLD-UHFFFAOYSA-N |
| Reference | </br>1:Inhibitory effect of donepezil on bradykinin-induced increase in the intracellular calcium concentration in cultured cortical astrocytes. Makitani K, Nakagawa S, Izumi Y, Akaike A, Kume T.J Pharmacol Sci. 2017 Apr 24. pii: S1347-8613(17)30059-2. doi: 10.1016/j.jphs.2017.03.008. [Epub ahead of print] PMID: 28499726 Free Article</br>2:Evaluation of neuroprotective effect of quercetin with donepezil in scopolamine-induced amnesia in rats. Pattanashetti LA, Taranalli AD, Parvatrao V, Malabade RH, Kumar D.Indian J Pharmacol. 2017 Jan-Feb;49(1):60-64. doi: 10.4103/0253-7613.201016. PMID: 28458424 Free PMC Article</br>3:Design, synthesis, and evaluation of multitarget-directed ligands against Alzheimer/’s disease based on the fusion of donepezil and curcumin. Yan J, Hu J, Liu A, He L, Li X, Wei H.Bioorg Med Chem. 2017 Apr 18. pii: S0968-0896(16)31533-4. doi: 10.1016/j.bmc.2017.02.048. [Epub ahead of print] PMID: 28454848 </br>4:The efficacy of donepezil administration on acetylcholinesterase activity and altered redox homeostasis in Alzheimer/’s disease. Atukeren P, Cengiz M, Yavuzer H, Gelisgen R, Altunoglu E, Oner S, Erdenen F, Yuceakın D, Derici H, Cakatay U, Uzun H.Biomed Pharmacother. 2017 Jun;90:786-795. doi: 10.1016/j.biopha.2017.03.101. Epub 2017 Apr 18. PMID: 28427041 </br>5:All-Solid-State, PVC Membrane, and Carbon Paste Ion-Selective Electrodes for Determination of Donepezil Hydrochloride in Pharmaceutical Formulation. Khamees N, Mohamed TA, Derar AR, Aziz A.J AOAC Int. 2017 Apr 18. doi: 10.5740/jaoacint.16-0299. [Epub ahead of print] PMID: 28421986 </br>6:Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors. Lan JS, Zhang T, Liu Y, Yang J, Xie SS, Liu J, Miao ZY, Ding Y.Eur J Med Chem. 2017 Jun 16;133:184-196. doi: 10.1016/j.ejmech.2017.02.045. Epub 2017 Mar 23. PMID: 28388521 </br>7:Effect of Metformin on Adult Hippocampal Neurogenesis: Comparison with Donepezil and Links to Cognition. Ahmed S, Mahmood Z, Javed A, Hashmi SN, Zerr I, Zafar S, Zahid S.J Mol Neurosci. 2017 May;62(1):88-98. doi: 10.1007/s12031-017-0915-z. Epub 2017 Apr 4. PMID: 28378260 </br>8:Donepezil, an Acetylcholinesterase Inhibitor, Can Attenuate Gabapentinoid-Induced Somnolence in Patients with Neuropathic Pain: A Retrospective Chart Review. Kogure T, Sumitani M, Ikegami K, Abe H, Hozumi J, Inoue R, Kawahara K, Yamada Y.J Pain Palliat Care Pharmacother. 2017 Mar;31(1):4-9. doi: 10.1080/15360288.2017.1279500. Epub 2017 Feb 22. PMID: 28287355 </br>9:Design, synthesis and evaluation of novel feruloyl-donepezil hybrids as potential multitarget drugs for the treatment of Alzheimer/’s disease. Dias KS, de Paula CT, Dos Santos T, Souza IN, Boni MS, Guimarães MJ, da Silva FM, Castro NG, Neves GA, Veloso CC, Coelho MM, de Melo IS, Giusti FC, Giusti-Paiva A, da Silva ML, Dardenne LE, Guedes IA, Pruccoli L, Morroni F, Tarozzi A, Viegas C Jr.Eur J Med Chem. 2017 Apr 21;130:440-457. doi: 10.1016/j.ejmech.2017.02.043. Epub 2017 Feb 21. PMID: 28282613 </br>10:Treatment with Sildenafil and Donepezil Improves Angiogenesis in Experimentally Induced Critical Limb Ischemia. Constantinescu IM, Bolfa P, Constantinescu D, Mironiuc AI, Gherman CD.Biomed Res Int. 2017;2017:9532381. doi: 10.1155/2017/9532381. Epub 2017 Jan 24. PMID: 28243607 Free PMC Article |
