Rivastigmine tartrate (ENA 713; SDZ-ENA 713) 是一种口服有效的胆碱酯酶 (ChE) 抑制剂，抑制丁酰胆碱酯酶 (BChE) 和乙酰胆碱酯酶 (AChE) 的 IC50 值分别为 0.037 μM 和 4.15 μM。
| Cas No. | 129101-54-8 |
| 别名 | 酒石酸卡巴拉汀; ENA 713; SDZ-ENA 713 |
| 化学名 | (2R,3R)-2,3-dihydroxybutanedioic acid;[3-[(1S)-1-(dimethylamino)ethyl]phenyl] N-ethyl-N-methylcarbamate |
| Canonical SMILES | CCN(C)C(=O)OC1=CC=CC(=C1)C(C)N(C)C.C(C(C(=O)O)O)(C(=O)O)O |
| 分子式 | C14H22N2O2.C4H6O6 |
| 分子量 | 400.42 |
| 溶解度 | ≥ 20.021mg/mL in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Rivastigmine tartrate, an cholinesterase inhibitor(IC50= 5.5 uM), inhibits both butyrylcholinesterase and acetylcholinesteraseIC50 value: 5.5 uMTarget: AChERivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects, which typically include nausea and vomiting. The drug is eliminated through the urine, and appears to have relatively few drug-drug interactions. Rivastigmine, a cholinesterase inhibitor, inhibits both butyrylcholinesterase and acetylcholinesterase. It is thought to work by inhibiting these cholinesterase enzymes, which would otherwise break down the brain chemical acetylcholine. References:
[1]. Kurz A, Farlow M, Lefèvre G. Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review. Int J Clin Pract. 2009 May;63(5):799-805.
[2]. 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.
[3]. Stryjer R, Ophir D, Bar F et al. Rivastigmine treatment for the prevention of electroconvulsive therapy-induced memory deficits in patients with schizophrenia. Clin Neuropharmacol. 2012 Jul-Aug;35(4):161-4.
[4]. Han HJ, Lee JJ, Park SA 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. |
