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1-(间氯苯基)-3-N,N-二甲基氨基甲酰基-5-甲氧基吡唑(PZ-177)的抗水肿作用

[Anti-edematous action of 1-(m-chlorophenyl)-3-N, N-dimethylcarbamoyl-5-methoxypyrazole (PZ-177)].

作者信息

Tsurumi K, Abe A, Shibuya T, Fujimura H

出版信息

Nihon Yakurigaku Zasshi. 1975 Nov;71(8):833-41. doi: 10.1254/fpj.71.833.

Abstract

From the screening of a number of new pyrazole derivatives, the title compound, PZ-177, was selected as the most significant derivative for analgestic and anti-edematous actions, in this paper, we report the anti-edematous activity of PZ-177 as assessed by detailed analysis. PZ-177 showed a markedly inhibitory effect against rat paw edema induced by various phlogists (carragenin, dextran, egg albumin, serotonin, formalin and bradykinin). It also inhibited edema induced by anti-rat rabbit serum. The activity of PZ-177 was more potent than that of mepirizole and the same as that of phenylbutazone. Though this agent has a central depressive effect, it is considered that the action has actually little influence on anti-edematous effect, as carrageenin-induced edema was inhibited in spinal rats. On the other hand, the anti-edematous effect of PZ-177 was reduced significantly in adrenalectomized rats. It is therefore suggested that the potent anti-edematous action of PZ-177 is exerted partially by a direct action at the inflamed site and mediated partially by stimulation of the hypophysis-adrenal system.

摘要

从众多新型吡唑衍生物的筛选中,标题化合物PZ - 177被选为具有最显著镇痛和抗水肿作用的衍生物。在本文中,我们报告了通过详细分析评估的PZ - 177的抗水肿活性。PZ - 177对多种致炎剂(角叉菜胶、右旋糖酐、蛋清蛋白、血清素、福尔马林和缓激肽)诱导的大鼠爪肿胀显示出明显的抑制作用。它还抑制抗大鼠兔血清诱导的水肿。PZ - 177的活性比美吡唑更强,与保泰松相当。尽管该药物具有中枢抑制作用,但由于角叉菜胶诱导的水肿在脊髓大鼠中受到抑制,所以认为该作用实际上对抗水肿作用影响很小。另一方面,在肾上腺切除的大鼠中,PZ - 177的抗水肿作用显著降低。因此表明,PZ - 177强大的抗水肿作用部分是通过在炎症部位的直接作用发挥的,部分是通过刺激垂体 - 肾上腺系统介导的。

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