Rivastigmine

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Chemical Structure| 123441-03-2 同义名 : 利凡斯的明 ;S-Rivastigmine; SDZ-ENA 713; Exelon; ENA 713 free base; SDZ-ENA 713 free base
CAS号 : 123441-03-2
货号 : A248924
分子式 : C14H22N2O2
纯度 : 98%
分子量 : 250.34
MDL号 : MFCD00871496
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(199.73 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • AChR

    AChR, IC50:5.5 μM
描述 Rivastigmine is a pseudo-irreversible, carbamate-type, brain-selective, dual AChE−BuChE inhibitor. In vitro, in male Wistar rats showed greater inhibitory potency (half maximal inhibitory concentration [IC50]) of rivastigmine toward brain BuChE and AChE compared with donepezil under optimal assay conditions (BuChE: 31 vs 7,400 nM; AChE: 4.3 vs 6.7 nM) [3]. Rivastigmine (1 mg/kg) also reduced myeloperoxidase activity and IL-6 by >60%, and the infiltration of CD11b expressing cells by 80%[4]. Rivastigmine can modify the levels of several shedding proteins and directs APP processing toward the non-amyloidogenic pathway[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02860338 - Completed - -
NCT01401582 Dementia Not Applicable Active, not recruiting March 2018 Germany ... 展开 >> Institute for Community Medicine Greifswald, Mecklenburg- Western Pommerania, Germany, 17489 收起 <<
NCT00291421 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.99mL

0.80mL

0.40mL

19.97mL

3.99mL

2.00mL

39.95mL

7.99mL

3.99mL
参考文献

[1]Abdel-Aal RA, Assi AA, Kostandy BB. Rivastigmine reverses aluminum-induced behavioral changes in rats. Eur J Pharmacol. 2011 Jun 1;659(2-3):169-76.

[2]Jann MW. Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease. Pharmacotherapy. 2000 Jan;20(1):1-12.

[3]Kandiah N, Pai MC, Senanarong V, Looi I, Ampil E, Park KW, Karanam AK, Christopher S. Rivastigmine: the advantages of dual inhibition of acetylcholinesterase and butyrylcholinesterase and its role in subcortical vascular dementia and Parkinson's disease dementia. Clin Interv Aging. 2017 Apr 18;12:697-707. doi: 10.2147/CIA.S129145. PMID: 28458525; PMCID: PMC5402908.

[4]Shifrin H, Nadler-Milbauer M, Shoham S, Weinstock M. Rivastigmine alleviates experimentally induced colitis in mice and rats by acting at central and peripheral sites to modulate immune responses. PLoS One. 2013;8(2):e57668. doi: 10.1371/journal.pone.0057668. Epub 2013 Feb 28. PMID: 23469045; PMCID: PMC3585220.

[5]Ray B, Maloney B, Sambamurti K, Karnati HK, Nelson PT, Greig NH, Lahiri DK. Rivastigmine modifies the α-secretase pathway and potentially early Alzheimer's disease. Transl Psychiatry. 2020 Feb 3;10(1):47. doi: 10.1038/s41398-020-0709-x. Erratum in: Transl Psychiatry. 2020 Mar 2;10(1):81. PMID: 32066688; PMCID: PMC7026402.