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前列腺素合成酶竞争性抑制剂与螺内酯的利尿、促尿钠排泄、促尿钾排泄及前列腺素合成酶抑制活性比较

Comparative diuretic, saluretic, kaliuretic, and prostaglandin synthetase inhibitory activities of a competitive inhibitor of prostaglandin synthetase and spironolactone.

作者信息

Fretland D J, Cammarata P S

出版信息

Prostaglandins Leukot Med. 1985 Oct;20(1):29-44. doi: 10.1016/0262-1746(85)90092-7.

Abstract

A newly described in vivo and in vitro competitive inhibitor of prostaglandin synthetase, 2-methyl, 8-cis, 12-trans, 14-cis, eicosatrienoic acid, a functional and structural analog of the endogenous substrates of prostaglandin E biosynthesis, as well as an analog of a putative intermediate in PGE1 biosynthesis, was shown to increase long-term urine excretion, and decrease long-term prostaglandin metabolite excretion in a linear dose-related manner. The correlation of both responses with dose were large (0.94, and 0.91 respectively), and nearly identical, within the limits of experimental error. In parallel studies, similar properties and nearly identical correlation coefficients were demonstrated for spironolactone, a known diuretic, suggesting that both drugs may be acting on mechanisms which may be closely associated and which may be involved in regulation of water and salt.

摘要

一种新描述的前列腺素合成酶体内和体外竞争性抑制剂,2-甲基,8-顺式,12-反式,14-顺式,二十碳三烯酸,前列腺素E生物合成内源性底物的功能和结构类似物,以及PGE1生物合成中假定中间体的类似物,被证明能以线性剂量相关方式增加长期尿排泄,并减少长期前列腺素代谢物排泄。两种反应与剂量的相关性都很大(分别为0.94和0.91),并且在实验误差范围内几乎相同。在平行研究中,已知利尿剂螺内酯也表现出类似的性质和几乎相同的相关系数,这表明两种药物可能作用于密切相关且可能参与水盐调节的机制。

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