DUAL INHIBITION OF CYCLOOXYGENASE AND LIPOXYGENASE BY 2-ACETYLTHIOPHENE 2-THIAZOLYLHYDRAZONE (CBS-1108) AND EFFECT ON LEUKOCYTE MIGRATION INVIVO

被引:23
作者
BERTEZ, C
MIQUEL, M
COQUELET, C
SINCHOLLE, D
BONNE, C
机构
[1] CTR RECH CHAUVIN BLACHE, F-34000 MONTPELLIER, FRANCE
[2] FAC PHARM NANCY, PHARMACOL LAB, F-54000 NANCY, FRANCE
关键词
D O I
10.1016/0006-2952(84)90346-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
CBS-1108, 2-acetylthiophene 2-thiazolyhydrazone, inhibits 5-lipoxygenase activity in [human and rabbit] polymorphonuclear leukocytes (PMN) (IC50 [median inhibitory concentration] = 2 .times. 10-6 M), 12-lipoxygenase (IC50 = 9 .times. 10-6 M) and cyclooxygenase (IC50 = 2 .times. 10-6 M) in platelets. Inhibitory of the 2 pathways of arachidonic acid cascade could lead to additional beneficial antiinflammatory activity by comparison with classical aspirin-like drugs. Only inhibitors of both cyclooxygenase and lipoxygenase such as NDGA [nordihydroquaiaretic acid] and CBS-1108 inhibit leukocyte migration in an animal model [rat] of acute inflammatory response.
引用
收藏
页码:1757 / 1762
页数:6
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