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关于新合成的苯甲酰基吡唑啉酮衍生物的抗炎作用机制

On the mechanism of the anti-inflammatory action of the newly-synthesized benzoylpyrazolone derivatives.

作者信息

Vlaskovska M V

出版信息

Acta Physiol Pharmacol Bulg. 1978;4(1):49-54.

PMID:726916
Abstract

One of the basic mechanisms of action of the nonsteroid anti-inflammatory agents is associated with prostaglandin synthesis. The effects of 1-phenyl-3-methyl-4 (4)-chlorbenzoylpyrazolone-5 (No. 151) and 1-phenyl-2-benzoyl-3-methylpyrazolone-5 (No. 76) on the quantity of prostaglandins and on the invasion of polymorphonuclear leucocytes in inflammatory exudate have been studied. Experimental inflammation is induced after Higgs et al. (1976). The level of prostaglandins in the exudate is determined through cascade superfusion of isolated smooth-muscle organs. The level of prostaglandins is found to decrease in animals treated with No. 151 and indomethacine, and to increase under the effect of No. 76. The invasion of the focus with polymorphonuclear leucocytes is inhibited by No. 151 and indomethacine. On the basis of the results obtained, No. 151 is assumed to belong to the group of prostaglandin-synthetase inhibitors, according to its mechanism of action.

摘要

非甾体抗炎药的基本作用机制之一与前列腺素的合成有关。研究了1-苯基-3-甲基-4(4)-氯苯甲酰吡唑酮-5(151号)和1-苯基-2-苯甲酰基-3-甲基吡唑酮-5(76号)对前列腺素数量以及对炎性渗出物中多形核白细胞浸润的影响。实验性炎症是按照希格斯等人(1976年)的方法诱导的。通过对分离的平滑肌器官进行级联灌流来测定渗出物中前列腺素的水平。结果发现,用151号药物和吲哚美辛处理的动物,其前列腺素水平降低,而在76号药物的作用下则升高。151号药物和吲哚美辛抑制多形核白细胞向病灶处浸润。根据所获得的结果,就其作用机制而言,151号药物被认为属于前列腺素合成酶抑制剂类。

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