Topiramate 是镇痉化合物,能拮抗GluR5受体,还可作为GABA受体介导的电流阳性变构调节剂。
Topiramate is a mutil-targeted inhibitor, including voltage-gated sodium channel and calcium channel, AMPA/kainate receptor and carbonic anhydrase, used to treat epilepsy.
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] Taverna S, et al. J Pharmacol Exp Ther, 1999, 288(3), 960-968.
[2] Dodgson et al (2000) Topiramate as an inhibitor of carbonic anhydrase isoenzymes. Epilepsia 41 S35. Gryder and Rogawski (2003)
分子式 C12H21NO8S |
分子量 339.36 |
CAS号 97240-79-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 68 mg/mL |
Water <1 mg/mL |
Ethanol 68 mg/mL |
体内溶解度
NCT02169830 | Migraine Disorders | Drug: nortriptyline|Drug: Topiramate | St. Louis University | 2014-06-01 | 2016-11-30 | |
NCT00606411 | Sleep-Related Eating Disorder | Drug: Topiramate or Placebo | Massachusetts General Hospital | Early Phase 1 | 2008-01-01 | 2016-03-22 |
NCT00550394 | Bipolar Disorder|Alcohol Abuse | Drug: quetiapine + placebo|Drug: Quetiapine + Topiramate | University of Cincinnati|National Institute on Alcohol Abuse and Alcoholism (NIAAA) | Phase 4 | 2008-04-01 | 2014-10-01 |
NCT00300742 | Alcohol Dependence|Binge Eating | Drug: Topiramate | University of Virginia | Phase 2 | 2006-03-01 | 2012-02-06 |
NCT01135602 | Alcohol Dependence | Drug: Topiramate | Chiang Mai University | Phase 4 | 2010-07-01 | 2011-08-12 |
NCT00846495 | Migraine | Drug: topiramate|Drug: frovatriptan | Clinvest|Endo Pharmaceuticals|Cady, Roger, M.D. | Phase 4 | 2009-08-01 | 2012-01-11 |
NCT01145677 | Alcohol Dependence | Drug: Topiramate | Chiang Mai University | Phase 2|Phase 3 | 2010-06-01 | 2011-06-22 |
NCT01682681 | Epilepsy | Drug: Topiramate | Janssen Korea, Ltd., Korea | Phase 4 | 2007-07-01 | 2013-08-21 |
NCT01408641 | Alcohol Dependence|Alcoholism|Alcohol Abuse|Alcohol Use Disorder|PTSD|Posttraumatic Stress Disorder | Drug: Topiramate|Drug: Placebo | University of Maryland|VA Office of Research and Development | 2012-09-01 | 2012-09-10 | |
NCT00394095 | Bipolar Disorder|Weight Gain | Drug: Topiramate|Drug: Placebo | University of Cincinnati|Eli Lilly and Company | Phase 4 | 2006-12-01 | 2013-04-03 |
NCT00626925 | Alcohol Drinking | Drug: topiramate|Drug: placebo | UConn Health|National Institute on Alcohol Abuse and Alcoholism (NIAAA)|National Center for Research Resources (NCRR) | Phase 4 | 2008-02-01 | 2016-08-02 |
NCT00203463 | PTSD | Drug: topiramate | Tuscaloosa Research & Education Advancement Corporation|Ortho-McNeil Janssen Scientific Affairs, LLC | Phase 4 | 2001-07-01 | 2009-07-28 |
NCT02808533 | Schizophrenia, Schizoaffective Disorder | Drug: Topiramate|Other: Placebo | Centre for Addiction and Mental Health|Ontario Ministry of Health and Long Term Care | 2016-04-01 | 2017-01-17 | |
NCT00902473 | Healthy | Drug: Topiramate | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2001-09-01 | 2009-05-14 | |
NCT01110434 | Cannabis Abuse|Cannabis Dependence | Drug: Topiramate|Drug: Placebo | Brown University|National Institute on Drug Abuse (NIDA) | Phase 2 | 2009-12-01 | 2012-07-11 |
NCT01641445 | Alcohol Drinking | Drug: Topiramate|Drug: Placebo | Brown University | Phase 1|Phase 2 | 2012-07-01 | 2016-01-11 |
NCT00901784 | Healthy | Drug: Topiramate | Ranbaxy Laboratories Limited|Ranbaxy Inc. | 2001-09-01 | 2009-06-17 | |
NCT02138058 | Compulsive Shopping | Drug: Topiramate|Behavioral: Cognitive restructuring intervention | University of Sao Paulo | Phase 2 | 2015-01-01 | 2015-12-01 |
NCT00167245 | Alcoholism|Cocaine Dependence | Drug: Topiramate|Drug: placebo | Kyle Kampman|National Institute on Alcohol Abuse and Alcoholism (NIAAA)|University of Pennsylvania | Phase 2 | 2004-09-01 | 2014-08-21 |
NCT00802412 | Nicotine Dependence|Alcohol Dependence | Drug: Topiramate|Drug: Placebo | VA Office of Research and Development | Phase 2 | 2009-01-01 | 2016-12-06 |
NCT00223626 | Cocaine-Related Disorders | Drug: Topiramate | Bankole Johnson|National Institute on Drug Abuse (NIDA)|University of Virginia | Phase 2 | 2007-01-01 | 2012-04-17 |
NCT02424318 | Migraine Disorders | Drug: Topiramate | SMG-SNU Boramae Medical Center | Phase 4 | 2008-12-01 | 2015-04-18 |
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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