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甲氯芬那酸钠(甲氯灭酸)——一种花生四烯酸级联反应的“双重抑制剂”的作用机制研究

Study of the mechanisms of action of sodium meclofenamic acid (Meclomen) a "double inhibitor" of the arachidonic acid cascade.

作者信息

Stadler I, Kapui Z, Ambrus J L

机构信息

Department of Internal Medicine, State University of NY at Buffalo, USA.

出版信息

J Med. 1994;25(6):371-82.

PMID:7769375
Abstract

Meclofenamic acid sodium (Meclomen) was found to inhibit both the cyclooxygenase and the lipoxygenase pathways of arachidonic acid metabolism. It inhibited both 5-lipoxygenase and 15-lipoxygenase activities. Meclomen was also shown to interfere with leukotriene receptors or possibly post-receptor mechanisms. In isolated lung parenchyma strip preparations Meclomen inhibited leukotriene C4 and D4 induced contractions, but had no effect on histamine induced contractions. Ibuprofen, naproxen and indomethacin had no effect on lipoxygenases or on leukotriene receptors but were powerful inhibitors of cyclooxygenases.

摘要

甲氯芬那酸钠(甲氯灭酸)被发现可抑制花生四烯酸代谢的环氧化酶和脂氧化酶途径。它同时抑制5-脂氧化酶和15-脂氧化酶的活性。甲氯灭酸还显示出可干扰白三烯受体或可能干扰受体后机制。在离体肺实质条制备中,甲氯灭酸抑制白三烯C4和D4诱导的收缩,但对组胺诱导的收缩没有影响。布洛芬、萘普生和吲哚美辛对脂氧化酶或白三烯受体没有影响,但却是环氧化酶的强效抑制剂。

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