Disulfiram是氨基甲酸酯衍生物,可作用于多巴胺-β-羟化酶。
Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.
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] Chen D, et al. Cancer Res, 2006, 66(21), 10425-10433.
[2] Helen L Wiggins et. Al. Disulfiram-induced cytotoxicity and endo-lysosomal sequestration of zinc in breast cancer cells. Biochemical Pharmacology, 93(3), 332-342 (2015).
[3] Ruijin Zheng et. Al. Differential metabolism of 4-hydroxynonenal in liver, lung and brain of mice and rats. Toxicology and Applied Pharmacology, 279(1), 43-52 (2014).
分子式 C10H20N2S4 |
分子量 296.54 |
CAS号 97-77-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 60 mg/mL |
Water 5 mg/mL |
Ethanol 72 mg/mL |
体内溶解度
NCT02735577 | Alcohol Use Disorder | Drug: Disulfiram | New York State Psychiatric Institute | Phase 4 | 2016-03-01 | 2016-09-20 |
NCT00731133 | Methamphetamine Dependence | Drug: Disulfiram | University of Arkansas | Phase 1|Phase 2 | 2008-08-01 | 2012-01-20 |
NCT00149630 | Cocaine Dependence|Opioid Dependence | Drug: Disulfiram|Drug: Methadone|Behavioral: CBT|Other: Lactose | Baylor College of Medicine|National Institute on Drug Abuse (NIDA)|Yale University | Phase 2 | 2005-01-01 | 2017-02-04 |
NCT01944371 | HIV|Human Immunodeficiency Virus | Drug: Disulfiram | University of California, San Francisco|Monash University|amfAR, The Foundation for AIDS Research|National Institute of Allergy and Infectious Diseases (NIAID) | Phase 1|Phase 2 | 2013-08-01 | 2014-10-27 |
NCT00878306 | HIV Infections|Drug Abuse | Drug: Disulfiram|Drug: Disulfiram + Efavirenz|Drug: Disulfiram + Atazanavir|Drug: Disulfiram + Ritonavir | University of California, San Francisco|National Institute on Drug Abuse (NIDA) | Phase 1 | 2008-11-01 | 2014-05-04 |
NCT00218608 | Cocaine-Related Disorders|Opioid-Related Disorders | Drug: Disulfiram | University of Arkansas|Yale University | Phase 2 | 2001-04-01 | 2012-01-26 |
NCT00571116 | Metastatic Melanoma | Drug: Disulfiram|Drug: Arsenic trioxide | University of California, Irvine | Phase 1|Phase 2 | 2006-09-01 | 2016-12-31 |
NCT01286259 | HIV-1 Infection | Drug: Disulfiram | University of California, San Francisco|Johns Hopkins University | 2011-01-01 | 2014-10-28 | |
NCT00742911 | Cancer | Drug: Disulfiram|Drug: Copper Gluconate | University of Utah | Phase 1 | 2008-07-01 | 2014-10-29 |
NCT00721526 | Alcohol Dependence|Anxiety Disorder | Drug: disulfiram plus lorazepam | University of New Mexico|National Institute on Alcohol Abuse and Alcoholism (NIAAA) | Phase 4 | 2009-08-01 | 2013-01-28 |
NCT00395850 | Cocaine Dependence | Drug: Disulfiram | University of Arkansas|National Institute on Drug Abuse (NIDA) | Phase 2 | 2007-04-01 | 2013-09-06 |
NCT00913484 | Cocaine Dependence|Opioid Dependency | Drug: Disulfiram|Drug: Placebo | Yale University|National Institute on Drug Abuse (NIDA) | Phase 2 | 2000-10-01 | 2009-06-03 |
NCT00256230 | Stage IV Melanoma | Drug: Disulfiram (DSF) | John P. Fruehauf|University of California, Irvine | Phase 1|Phase 2 | 2002-01-01 | 2016-12-06 |
NCT01907165 | Glioblastoma | Drug: Temozolomide|Drug: Disulfiram|Dietary Supplement: Copper gluconate | Washington University School of Medicine | Early Phase 1 | 2013-10-10 | 2017-03-14 |
NCT00580827 | Cocaine-Related Disorder|Opiate Dependence | Drug: Placebo|Drug: Disulfiram|Drug: Disulfiram|Drug: Disulfiram | Yale University|National Institute on Drug Abuse (NIDA) | 2003-09-01 | 2007-12-25 | |
NCT01777919 | Glioblastoma Multiforme | Drug: Temozolomide|Drug: Disulfiram|Drug: Copper | Olympion Medical Center|University of Ioannina|University of Eastern Finland|University of Ulm | Phase 2 | 2017-01-01 | 2016-10-14 |
NCT02101008 | Melanoma | Drug: disulfiram and chelated zinc | University of Utah | Phase 2 | 2010-03-01 | 2015-12-21 |
NCT00002065 | HIV Infections | Drug: Disulfiram | St. Vincent's Medical Center|NIH AIDS Clinical Trials Information Service | null | 2005-06-23 | |
NCT00000278 | Alcohol-Related Disorders|Cocaine-Related Disorders | Drug: Disulfiram | Yale University|National Institute on Drug Abuse (NIDA)|VA Connecticut Healthcare System | Phase 2 | 1994-09-01 | 2013-07-24 |
NCT03034135 | Recurrent Glioblastoma | Drug: Disulfiram/Copper | Cantex Pharmaceuticals | Phase 2 | 2017-03-09 | 2017-03-10 |
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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