Rivastigmine tartrate (酒石酸卡巴拉汀) 是胆碱酯酶抑制剂,IC50为5.5 uM,还能抑制丁酰胆碱酯酶和乙酰胆碱酯酶。
Rivastigmine Tartrate is a cholinesterase inhibitor with IC50 of 5.5 μM, and used as a parasympathomimetic or cholinergic agent for the treatment of mild to moderate Alzheimer disease.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] A Servello et. Al. Effect of AChE and BuChE inhibition by rivastigmin in a group of old-old elderly patients with cerebrovascular impairment (SIVD type). Minerva medica, 105(2), 167-174 (2014).
[2] Steven H Ferris and Martin Farlow. Language impairment in Alzheimer's disease and benefits of acetylcholinesterase inhibitors. Clinical Interventions in Aging, 8, 1007-1014 (2013)
分子式 C18H28N2O8 |
分子量 400.42 |
CAS号 129101-54-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 42 mg/mL |
Water 80 mg/mL |
Ethanol 80 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00624663 | Rivastigmine Toxicity | Drug: Rivastigmine | Tel-Aviv Sourasky Medical Center|Medical Corps, Israel Defense Force | 2009-01-01 | 2014-03-26 | |
NCT02063269 | Alzheimer's Disease | Drug: Rivastigmine | Seoul National University Hospital|Novartis Korea Ltd. | 2014-02-01 | 2015-05-12 | |
NCT01073319 | Methamphetamine Dependence|Substance Abuse|Methamphetamine Abuse | Other: Placebo|Drug: Rivastigmine|Drug: Rivastigmine | Baylor College of Medicine|National Institute on Drug Abuse (NIDA) | Phase 1 | 2009-07-01 | 2012-07-25 |
NCT00623103 | Parkinson's Disease Dementia | Drug: Rivastigmine capsule|Drug: Rivastigmine transdermal patch | Novartis | Phase 3 | 2008-01-01 | 2011-10-19 |
NCT01146041 | Healthy | Drug: Rivastigmine | Dr. Reddy's Laboratories Limited | Phase 1 | 2004-02-01 | 2010-06-16 |
NCT01146067 | Healthy | Drug: Rivastigmine | Dr. Reddy's Laboratories Limited | Phase 1 | 2004-01-01 | 2012-01-12 |
NCT01183806 | Alzheimer Disease | Drug: Rivastigmine|Other: Exercise training program | Federal University of Bahia | Phase 3 | 2010-07-01 | 2012-03-19 |
NCT01585272 | Alzheimer's Dementia | Drug: ENA713 | Novartis Pharmaceuticals|Novartis | Phase 4 | 2012-08-01 | 2016-09-22 |
NCT01948791 | Alzheimer's Disease | Drug: ENA713 | Novartis Pharmaceuticals|Novartis | Phase 4 | 2014-08-01 | 2016-12-20 |
NCT02703636 | Mild to Moderate Alzheimer's Disease | Drug: Rivastigmine Patch | Novartis Pharmaceuticals|Novartis | Phase 4 | 2016-05-01 | 2016-11-18 |
NCT00622713 | Alzheimer's Disease | Drug: Rivastigmine transdermal patch | Novartis | Phase 4 | 2008-01-01 | 2011-06-27 |
NCT01084135 | Down Syndrome | Drug: Rivastigmine|Other: Liquid Placebo | Duke University|Taishoff Family Foundation|Hugo W. Moser Research Institute at Kennedy Krieger, Inc. | Phase 1|Phase 2 | 2009-11-01 | 2015-03-17 |
NCT02444637 | Alzheimer Disease|CVA (Cerebrovascular Accident) | Drug: Rivastigmine | National Neuroscience Institute | Phase 4 | 2015-04-01 | 2015-05-11 |
NCT00835159 | Delirium|Postoperative Cognitive Dysfunction | Drug: Rivastigmine Patch|Other: Placebo Patch | New York University School of Medicine|Novartis | Phase 4 | 2008-12-01 | 2015-01-26 |
NCT00748007 | Down Syndrome | Drug: Rivastigmine | National Taiwan University Hospital | 2008-01-01 | 2012-11-27 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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