Metabolism and excretion of imrecoxib in rat
文献类型：期刊论文
| 作者 | Xu, H.; Zhang, Y.; Sun, Y.; Zhang, P.; Chu, F.; Guo, Z.; Zhang, H.; Zhong, D. |
| 刊名 | XENOBIOTICA
 |
| 出版日期 | 2006-05 |
| 卷号 | 36期号:5页码:441-455 |
| 关键词 | imrecoxib metabolism |
| ISSN号 | 0049-8254 |
| DOI | 10.1080/00498250600595524 |
| 文献子类 | Article |
| 英文摘要 | The metabolism and excretion of imrecoxib, a novel and moderately selective cyclooxygenase-II inhibitor, were investigated in rat. The structures of metabolites were identified by mass spectrometry (MSn) and nuclear magnetic resonance. Metabolic profiles of imrecoxib in urine, bile and faeces were obtained by HPLC and LC/MSn, and cumulative excretion was determined by LC/MSn. Imrecoxib was extensively metabolized in rat after intravenous administration, with less than 2% of the dose excreted as parent drug in either urine or faeces. The major metabolic pathway was that the 4'- methyl group of imrecoxib was first oxidized to the 4'-hydroxymethyl metabolite (M4), followed by additional oxidation to 4'-carboxylic acid metabolite (M2). The dihydroxylated metabolite, 4'-hydroxymethyl-5-hydroxyl imrecoxib (M3), was further oxidized to 4'-hydroxymethyl-5-carbonyl metabolite (M5), and glucuronide conjugates of M2-4 were formed. After intravenous (5mg kg(-1)) administration, the majority of the dose was recovered in the faeces. The dose was primarily excreted as the carboxylic acid metabolite in addition to the 4'-hydroxymethyl metabolite. The carboxylic acid metabolite was mainly excreted in faeces, while the 4'-hydroxymethyl metabolite was mainly excreted in urine. |
| WOS关键词 | NONSTEROIDAL ANTIINFLAMMATORY DRUGS ; CYCLOOXYGENASE-2 INHIBITOR ; COX-2 INHIBITORS ; OSTEOARTHRITIS ; NSAIDS |
| WOS研究方向 | Pharmacology & Pharmacy ; Toxicology |
| 语种 | 英语 |
| WOS记录号 | WOS:000238834600006 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273616]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Zhong, D. |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Peking Union Med Coll, Beijing 100050, Peoples R China 3.Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China 4.Shenyang Pharmaceut Univ, Lab Drug Metab & Pharmacokinet, Shenyang 110016, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xu, H.,Zhang, Y.,Sun, Y.,et al. Metabolism and excretion of imrecoxib in rat[J]. XENOBIOTICA,2006,36(5):441-455. |
| APA | Xu, H..,Zhang, Y..,Sun, Y..,Zhang, P..,Chu, F..,...&Zhong, D..(2006).Metabolism and excretion of imrecoxib in rat.XENOBIOTICA,36(5),441-455. |
| MLA | Xu, H.,et al."Metabolism and excretion of imrecoxib in rat".XENOBIOTICA 36.5(2006):441-455. |
入库方式： OAI收割
来源：上海药物研究所
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