期刊文献+

环氧化酶-2特异性抑制剂——艾瑞昔布 被引量:7

原文传递
导出
摘要 非甾体抗炎药(nonsteroidal anti—inflammatory drugs,NSAIDs)可改善风湿性疾病的炎性症状并可缓解疼痛,是全世界使用最广泛的一类药物。但使用NSAIDs的过程中,尤其是长期、大量服用时可出现胃肠道损害。为此人们研发了选择性环氧化酶-2(COX-2)抑制剂,目前已在全球普遍使用。但高选择性COX-2抑制剂易产生心血管事件。因此,中国医学科学院药物研究所与江苏恒瑞医药股份有限公司根据“适度抑制”COX-2的理念,用10年时间自主研发选择性COX-2抑制剂——艾瑞昔布(imrecoxib),希望在抑制炎症和疼痛的同时,降低胃肠道刺激和心血管损伤的几率。
作者 杜小莉
出处 《中国药学杂志》 CAS CSCD 北大核心 2012年第5期399-400,共2页 Chinese Pharmaceutical Journal
  • 相关文献

参考文献3

二级参考文献14

  • 1Ai Ping BAI,Zong Ru GUO,Wen Hui HU,Fang SHEN,Gui Fang CHENG.Design,Synthesis and in vitro Evaluation of a New Class of Novel Cyclooxygenase-2 Inhibitors:3,4-diaryl-3-pyrrolin-2-ones[J].Chinese Chemical Letters,2001,12(9):775-778. 被引量:7
  • 2Barrios-Rodiles M, Tiraloche G, Chadee K. Lipopolysaccharide modulates cyclooxygenase-2 transcriptionally and posttranscriptionally in human macrophages independently from endogenous IL-1 β and TNF-α. J Immunol 1999; 163:963 -9.
  • 3Cheng GF, Liu DP, Yang DX, He KQ, Bai JY, Zhu XY.Antiinflammatory effects of Tremulacin, a Salicin-related substance isolated from Populus Tomentosa Carr leaves.Phytomedicine 1994: 1: 209-11.
  • 4Dai M, Wei W, Shen YX, Zheng YQ. Glucosides of Chaenomeles specioca remit rat adjuvant arthritis by inhibiting synoviocyte activities. Acta Pharmacol Sin 2003; 24:1161-6.
  • 5Barrios-Rodiles M, Keller K, Belley A, Chadee K. Nonsteroidal anti-inflammatory drugs inhibit cyclooxygenase-2 enzyme activity but not mRNA expression in human macrophages. Biochem Biophys Res Commun 1996; 225:896-900.
  • 6Marnett LJ, Rowlinson SW, Goodwin DC, Kalgutkar AS, Lanzo CA. Arachidonic acid oxygenation by COX-1 and COX-2. Mechanisms of catalysis and inhibition. J Biol Chem 1999; 274: 22903-6.
  • 7Chandrasekharan NV, Dai H, Roos KL, Evanson NK, Tomsik J, Elton TS, etal. COX-3, a cyclooxygenase-1 variant inhibited by acetaminophen and other analgesic/antipyretic drugs:cloning, structure, and expression. Proc Natl Acad Sci USA2 002; 99: 13926-31.
  • 8Dinchuk JE, Liu RQ, Trzaskos JM. COX-3: in the wrong frame in mind. Immunol Lett 2003; 86: 121.
  • 9Warner TD, Giuliano F, Vojnovic I, Bukasa A, Mitchell JA,Vane JR. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis. Proc Natl Acad Sci USA 1999; 96: 7563-8.
  • 10FitzGerald GA, Patrono C. The coxibs, selective inhibitors of cyclooxygenase-2. N Engl J Med 2001; 345: 433-42.

共引文献31

同被引文献54

引证文献7

二级引证文献22

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部