Probenecid是一种经典的有机阴离子运输竞争性抑制剂,同时也是一种瞬时感受器电位香草素受体亚家族2(TRPV2)的激动剂和人苦味觉感受器TAS2R16的抑制剂。
Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16.
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] McDonough PM, et al. Cell Calcium, 1989, 10(3), 171-180.
[2] Hammond et al (2007) Glutathione export during apoptosis requires functional multidrug resistance-associated proteins. J.Biol.Chem. 282 14337.
[3] Silverman et al (2008) Probenecid, a gout remedy, inhibits pannexin 1 channels. Am.J.Physiol.Cell Physiol. 295 C761.
[4] Ishikawa et al (2010) Function and expression of ATP-binding cassette transporters in cultured human Y79 retinoblastoma cells. Biol.Pharm.Bull. 33 504.
分子式 C13H19NO4S |
分子量 285.36 |
CAS号 57-66-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 56 mg/mL |
Water <1 mg/mL |
Ethanol 20 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01428284 | Healthy | Drug: Canagliflozin/Probenecid | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. | Phase 1 | 2011-08-01 | 2012-02-16 |
NCT01029782 | Cellulitis | Drug: IV cefazolin plus oral probenecid and placebo cephalexin|Drug: Oral cephalexin and saline IV plus probenecid placebo | Kelowna General Hospital|Canadian Society of Hospital Pharmacists|Capital Health, Canada|Interior Health Authority, Canada | Phase 2 | 2010-05-01 | 2015-01-13 |
NCT01814319 | Systolic Heart Failure | Drug: Probenecid 1 gr oral twice daily|Drug: Placebo | University of Cincinnati | Phase 2 | 2013-03-01 | 2015-08-24 |
NCT00842400 | Obesity | Drug: Metformin, VI-0521, Sitagliptan, Probenecid | VIVUS, Inc. | Phase 1 | 2009-02-01 | 2010-01-20 |
NCT02243631 | Calcium Pyrophosphate Deposition Disease | Drug: Probenecid | VA Office of Research and Development | Early Phase 1 | 2014-10-01 | 2017-01-04 |
NCT01937026 | Healthy Volunteers | Drug: Baricitinib|Drug: Probenecid | Eli Lilly and Company | Phase 1 | 2013-09-01 | 2013-12-03 |
NCT00000670 | HIV Infections | Drug: Probenecid|Drug: Zidovudine | National Institute of Allergy and Infectious Diseases (NIAID) | 2012-03-15 | ||
NCT00000706 | HIV Infections | Drug: Quinine sulfate|Drug: Probenecid|Drug: Zidovudine | National Institute of Allergy and Infectious Diseases (NIAID) | 2012-03-15 | ||
NCT00024245 | Unspecified Adult Solid Tumor, Protocol Specific | Drug: pralatrexate|Drug: probenecid | Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) | Phase 1 | 2001-05-01 | 2013-06-25 |
NCT01907373 | Drug Interaction of Olmesartan in Healthy Chinese Volunteers | Drug: olmesartan medoxomil|Drug: olmesartan medoxomil+probenecid | Central South University | Phase 4 | 2009-08-01 | 2013-07-24 |
NCT00610532 | Epilepsy | Drug: phenytoin|Drug: phenytoin and probenecid | Jim McAuley|Ohio State University | Phase 4 | 2006-03-01 | 2013-05-13 |
NCT01634100 | Healthy | Drug: Probenecid|Drug: Rifampicin|Drug: Empagliflozin|Drug: Empagliflozin|Drug: Rifampicin|Drug: Probenecid|Drug: Empagliflozin (BI 10773) | Boehringer Ingelheim | Phase 1 | 2012-06-01 | 2014-06-27 |
NCT00304434 | Influenza | Drug: Oseltamivir|Drug: Probenecid | VA Office of Research and Development|Brooke Army Medical Center|National Institutes of Health (NIH) | Phase 4 | 2005-02-01 | 2009-09-21 |
NCT00323219 | Cellulitis | Drug: Cefazolin and Moxifloxacin | University of British Columbia | Phase 3 | 2004-01-01 | 2012-02-06 |
NCT00690014 | Kidney Disease | Drug: probenecid | University of Maryland|National Institutes of Health (NIH) | 2007-08-01 | 2008-06-03 | |
NCT00439530 | Avian Influenza A Virus | Drug: oseltamivir|Drug: probenecid | Mahidol University|National Institute of Allergy and Infectious Diseases (NIAID)|Southeast Asia Influenza Clinical Research Network | Phase 1 | 2006-11-01 | 2009-07-24 |
NCT01322009 | Pediatric Traumatic Brain Injury | Drug: Probenecid and N-acetyl cysteine|Drug: Placebo | University of Pittsburgh|National Institutes of Health (NIH)|National Institute of Neurological Disorders and Stroke (NINDS) | Phase 1|Phase 2 | 2011-03-01 | 2016-07-01 |
NCT01816646 | Blood And Marrow Transplantation | Drug: Cidofovir|Drug: Probenecid | M.D. Anderson Cancer Center|Gilead Sciences | Phase 1 | 2013-09-01 | 2016-12-02 |
NCT01021020 | Healthy | Drug: Colchicine|Drug: Colchicine|Drug: Colchicine/Probenecid | Mutual Pharmaceutical Company, Inc. | Phase 1 | 2007-09-01 | 2009-12-01 |
NCT00002437 | Cytomegalovirus Retinitis|HIV Infections | Drug: Cidofovir|Drug: Probenecid | Gilead Sciences|NIH AIDS Clinical Trials Information Service | Phase 2 | 2005-06-23 |
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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