9,11-氮杂前列腺-5,13-二烯酸对人血小板血栓素合成酶的抑制作用。
Inhibition of human platelet thromboxane synthetase by 9,11-azoprosta-5,13-dienoic acid.
作者信息
Gorman R R, Bundy G L, Peterson D C, Sun F F, Miller O V, Fitzpatrick F A
出版信息
Proc Natl Acad Sci U S A. 1977 Sep;74(9):4007-11. doi: 10.1073/pnas.74.9.4007.
Abstract
The synthetic prostaglandin analog 9,11-azoprosta-5,13-dienoic acid (azo analog I) has been found to be a potent inhibitor of human platelet thromboxane synthetase by three independent analytical methods: electron-capture gas chromatography, radioisotopic thin-layer chromatography, and radioimmunoassay. In the presence of azo analog I, human platelet aggregation induced by either the prostaglandin endoperoxide PGH2 or arachidonic acid was antagonized. The addition of azo analog I shifted the transformation of endoperoxides away from thromboxane synthesis and toward prostaglandin E2 synthesis. The specificity of azo analog I is demonstrated by its selective inhibition of the second wave of either ADP- or epinephrine-induced platelet aggregation. These data indicate that PGH2 must be converted to thromboxane A2 in order to induce human platelet aggregation.
摘要
通过三种独立的分析方法
电子捕获气相色谱法、放射性同位素薄层色谱法和放射免疫分析法，已发现合成前列腺素类似物9,11-氮杂前列腺素-5,13-二烯酸（氮杂类似物I）是人类血小板血栓素合成酶的有效抑制剂。在氮杂类似物I存在的情况下，由前列腺素内过氧化物PGH2或花生四烯酸诱导的人类血小板聚集受到拮抗。氮杂类似物I的加入使内过氧化物的转化从血栓素合成转向前列腺素E2合成。氮杂类似物I的特异性通过其对ADP或肾上腺素诱导的血小板聚集第二波的选择性抑制得以证明。这些数据表明，PGH2必须转化为血栓素A2才能诱导人类血小板聚集。
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