曲匹地尔及其衍生物对花生四烯酸和前列腺素内过氧化物类似物U 46619诱导的大鼠血压变化的影响。

Effects of trapidil and trapidil derivatives on arachidonic acid and prostaglandin endoperoxide analogue U 46619-induced blood pressure changes in rats.

作者信息

Heinroth-Hoffmann I, Hauser A, Taube C, Mest H J

机构信息

Department of Pharmacology and Toxicology, Martin Luther University Halle-Wittenberg, GDR.

出版信息

Biomed Biochim Acta. 1988;47(10-11):S145-8.

Abstract

The influence of trapidil (T) and two selected 5,7-disubstituted s-triazolo (1,5-a)pyrimidine derivatives (TD: AR 12456 and AR 12463) on arachidonic acid(AA)- and prostaglandin endoperoxide analogue U 46619-induced blood pressure changes in normotensive rats was investigated in comparison with the cyclooxygenase inhibitor acetylsalicylic acid (ASA) and the thromboxane A2 (TXA2) antagonist BM 13177. ASA and AR 12456 completely eliminated the second blood pressure depression after injection of AA and simultaneously diminished TXA2, TXB2 and 6-keto-PGF1a formation in murine blood, whereas BM 13177 prevented the return of the blood pressure to preinjection level after the initial brief fall in arterial pressure. BM 13177 and AR 12463 reduced the rise in U 46619-provoked blood pressure by 75% and 58%, respectively. Trapidil had no effect on blood pressure changes stimulated by AA and U 46619.

摘要

将曲匹地尔（T）和两种选定的5,7 - 二取代s - 三唑并[1,5 - a]嘧啶衍生物（TD：AR 12456和AR 12463）与环氧化酶抑制剂乙酰水杨酸（ASA）和血栓素A2（TXA2）拮抗剂BM 13177相比较，研究了它们对正常血压大鼠中花生四烯酸（AA）和前列腺素内过氧化物类似物U 46619诱导的血压变化的影响。ASA和AR 12456在注射AA后完全消除了第二次血压下降，同时减少了小鼠血液中TXA2、TXB2和6 - 酮 - PGF1a的生成，而BM 13177在动脉压最初短暂下降后阻止血压恢复到注射前水平。BM 13177和AR 12463分别使U 46619引起的血压升高降低了75%和58%。曲匹地尔对AA和U 46619刺激的血压变化没有影响。

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Effects of trapidil and trapidil derivatives on arachidonic acid and prostaglandin endoperoxide analogue U 46619-induced blood pressure changes in rats.曲匹地尔及其衍生物对花生四烯酸和前列腺素内过氧化物类似物U 46619诱导的大鼠血压变化的影响。

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Influence of the antianginal drug trapidil and its derivative AR 12463 on arachidonic acid liberation and thromboxane formation in thrombin-stimulated platelets.抗心绞痛药物曲匹地尔及其衍生物AR 12463对凝血酶刺激的血小板中花生四烯酸释放和血栓素形成的影响。

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Inhibition of thromboxane B2 formation of blood platelets by trapidil and other s-triazolo(1,5-a)pyrimidine derivatives.曲匹地尔及其他s-三唑并(1,5-a)嘧啶衍生物对血小板血栓素B2生成的抑制作用

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FEBS Lett. 1984 Jul 9;172(2):167-71. doi: 10.1016/0014-5793(84)81119-9.

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