Tolcapone是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂,Ki为30nM。
Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
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] Ricardo Sant'Anna,et al. Repositioning tolcapone as a potent inhibitor of transthyretin amyloidogenesis and associated cellular toxicity. Nat Commun. 2016; 7: 10787. Published online 2016 Feb 23. doi: 10.1038/ncomms10787.
[2] Aqilah M. McCane,et al. Tolcapone suppresses ethanol intake in alcohol preferring rats performing a novel cued access protocol. Alcohol Clin Exp Res. Author manuscript; available in PMC 2015 Sep 1. Published in final edited form as: Alcohol Clin Exp Res. 2014 Sep; 38(9): 2468–2478. doi: 10.1111/acer.12515.
[3] Sophia C. Magalona,et al. Inhibition of Comt with tolcapone slows progression of polycystic kidney disease in the more severely affected PKD/Mhm (cy/+) substrain of the Hannover Sprague-Dawley rat. CNS Drugs. Author manuscript; available in PMC 2014 Aug 18.
分子式 C14H11NO5 |
分子量 273.24 |
CAS号 134308-13-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 55 mg/mL |
Water <1 mg/mL |
Ethanol 55 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00927563 | Pathological Gambling | Drug: Tolcapone | University of Chicago | Phase 2 | 2009-06-01 | 2014-01-17 |
NCT02630043 | Neuroblastoma | Drug: Tolcapone|Drug: Oxaliplatin | Spectrum Health Hospitals | Phase 1 | 2015-12-01 | 2016-09-14 |
NCT02740582 | Alcohol Abuse|Impulsive Behavior | Drug: Tolcapone|Drug: Placebo | University of California, San Francisco | 2016-10-01 | 2017-01-12 | |
NCT01202955 | Nicotine Dependence | Drug: Tolcapone|Drug: Placebo | University of Pennsylvania | Phase 2 | 2008-07-01 | 2011-05-04 |
NCT02652598 | Brain Injuries, Traumatic|Neurocognitive Disorders|Brain Injuries | Drug: Tolcapone | Sheppard Pratt Health System|Lieber Institute for Brain Development (LIBD) | Phase 2 | 2015-11-01 | 2017-01-17 |
NCT02080715 | Healthy | Drug: Tolcapone|Drug: Placebo | University of Zurich | Phase 1 | 2013-06-01 | 2014-09-11 |
NCT00604591 | Frontotemporal Lobar Degeneration | Drug: Tolcapone|Drug: Placebo | Columbia University|National Institute of Neurological Disorders and Stroke (NINDS) | Phase 2 | 2011-07-01 | 2016-06-14 |
NCT00044083 | Schizophrenia | Drug: Tolcapone | National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) | Phase 2 | 2002-08-01 | 2016-08-31 |
NCT00033059 | Cocaine-Related Disorders | Drug: Tolcapone | National Institute on Drug Abuse (NIDA) | Phase 1 | 2001-07-01 | 2017-01-10 |
NCT02448654 | Nicotine Dependence | Drug: Tolcapone|Drug: Sugar Pill | Yale University|VA Office of Research and Development | 2015-10-01 | 2016-07-18 | |
NCT02191826 | Familial Amyloid Polyneuropathy (FAP) | Drug: SOM0226 | SOM Biotech SL|Hospital Vall d'Hebron | Phase 1|Phase 2 | 2014-07-01 | 2016-11-29 |
NCT02949934 | Alcohol Use Disorder | Drug: Tolcapone|Drug: Placebo | Medical University of South Carolina|National Institute on Alcohol Abuse and Alcoholism (NIAAA) | Phase 2 | 2016-05-01 | 2016-10-27 |
NCT01001520 | Tobacco Use Disorder | Drug: Tolcapone|Drug: Placebo | University of Pennsylvania|National Institute on Drug Abuse (NIDA) | Phase 2 | 2010-01-01 | 2014-05-29 |
NCT02929485 | Addiction | Drug: Tolcapone|Drug: Placebo|Drug: Bromocriptine | University of California, San Francisco|University of California, Berkeley | 2013-07-01 | 2016-10-10 | |
NCT02772978 | Pathological Gambling | Drug: Tolcapone|Drug: Placebo | University of California, San Francisco|National Center for Responsible Gaming | 2014-08-01 | 2016-05-12 | |
NCT02260570 | Mild Traumatic Brain Injury | Drug: Tolcapone|Drug: Placebo | VA Office of Research and Development|University of California, Berkeley|University of California, San Francisco | 2015-08-01 | 2017-03-13 | |
NCT01158950 | Impulsive Behavior | Drug: Tolcapone|Other: Placebo|Drug: Entacapone | University of California, San Francisco|University of California, Berkeley|United States Department of Defense | 2010-03-01 | 2016-04-12 | |
NCT00906828 | Parkinson Disease | Drug: levodopa/carbidopa|Drug: entacapone|Drug: tolcapone | Uppsala University|Swedish Parkinson's Disease Foundation|Swedish Society for Medical Research | Phase 4 | 2008-10-01 | 2010-01-15 |
NCT02994719 | Parkinson's Disease|Parkinsonian Disorders|Atypical Parkinson Disease|Progressive Supranuclear Palsy|Multiple System Atrophy|Corticobasal Degeneration|Gait, Frontal | Drug: Anti-Parkinson medication|Device: Deep Brain Stimulation | Beth Israel Deaconess Medical Center | 2016-03-01 | 2017-03-09 |
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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