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

来源：

BIOCHEMICAL PHARMACOLOGY | 1984年 / 33卷 / 11期

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

页码：1757 / 1762

页数：6

共 30 条

[1] MULTIPLE EFFECTS OF A NEW ANTI-INFLAMMATORY AGENT, TIMEGADINE, ON ARACHIDONIC-ACID RELEASE AND METABOLISM IN NEUTROPHILS AND PLATELETS [J].