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Rivastigmine tartrate

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Chemical Structure| 129101-54-8 同义名 : L-酒石酸卡巴拉汀 ;SDZ-ENA 713;ENA 713;Exelon;Rivastigmine (tartrate)
CAS号 : 129101-54-8
货号 : A193069
分子式 : C18H28N2O8
纯度 : 98%
分子量 : 400.423
MDL号 : MFCD03700731
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(124.87 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Rivastigmine tartrate, a cholinesterase inhibitor (IC50= 5.5 μM), inhibits both butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE). Rivastigmine (0.6 mg/kg intraperitoneally [i.p.]) inhibited AChE and BuChE by 40% and 25%, respectively[3]. Both preclinical studies and studies in human volunteers have shown that rivastigmine induces substantially greater inhibition of AChE in the central nervous system compartment than in the periphery[4]. Moreover, Rivastigmine can modify the levels of several shedding proteins and directs APP processing toward the non-amyloidogenic pathway for Alzheimer's disease[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
NCT00291421 - 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 <<
NCT01401582 - Active, not recruiting - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.49mL

2.50mL

1.25mL

24.97mL

4.99mL

2.50mL
参考文献

[1]Nieto RA, Deardorff WJ, Grossberg GT. Efficacy of rivastigmine tartrate, transdermal system, in Alzheimer's disease. Expert Opin Pharmacother. 2016;17(6):861-70.

[2]Han HJ, Lee JJ, et al. Efficacy and safety of switching from oral cholinesterase inhibitors to the rivastigmine transdermal patch in patients with probable Alzheimer's disease. J Clin Neurol. 2011 Sep;7(3):137-42.

[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]Polinsky RJ. Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Clin Ther. 1998 Jul-Aug;20(4):634-47. doi: 10.1016/s0149-2918(98)80127-6. PMID: 9737824.

[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.