trapidil和其他s-三唑(1,5 -a)嘧啶衍生物对血小板血栓素B2形成的抑制作用

H.-U. Block, I. Hoffmann-Heinroth, Ch. Taube, M. Niebisch, H.-J. Mest
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引用次数: 5

摘要

Trapidil和其他一些具有抗血小板聚集作用的5,7-二取代s-三唑(1,5 -a)嘧啶衍生物(TPDs)也能抑制凝血人和兔全血以及花生四烯酸激活的富血小板人血浆中血小板血栓素A2 (TXA2)的体外生物合成。TPDs对TXB2形成的抑制作用与抗聚集作用在一定程度上平行,其抑制作用的强弱顺序为:AR 12456 >AR 12463≈AR 12464≈AR 12465 >trapidil。给家兔口服tpd, 2小时后采血,血清TXB2水平未见变化。家兔静脉注射TPDs后,活性最强的TPDs AR 12456和AR 12463可使血清TXB2短期降低61.4%和49.4%。80 min后TXB2水平恢复到预处理前水平。探讨了TPDs主要通过抑制磷酸二酯酶活性来阻止血小板TXA2形成的可能性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Inhibition of thromboxane B2 formation of blood platelets by trapidil and other s-triazolo(l,5-a)pyrimidine derivatives

Trapidil and some other 5,7-disubstituted s-triazolo(l,5-a)pyrimidine derivatives (TPDs) which were shown to have potent actions against platelet aggregation also inhibited in vitro platelet thromboxane A2 (TXA2) biosynthesis in clotting human and rabbit whole blood as well as in arachidonic acid-activated platelet-rich human plasma. The inhibitory potency of TPDs on TXB2 formation paralleled the antiaggregatory effectiveness to a certain extent and decreased in the following order: AR 12456 > AR 12463 ≈ AR 12464 ≈AR 12465 > trapidil. When TPDs were administered orally to rabbits and blood was taken 2 hours later, no changes of serum TXB2 level were observed. After i.v. injection of TPDs in rabbits, the most active TPDs AR 12456 and AR 12463 led to a short-lasting reduction of serum TXB2 by 61.4 and 49.4 %, resp.. The TXB2 levels returned nearly to pre-treatment level after 80 min. The possibility is discussed that TPDs mainly prevent platelet TXA2 formation by inhibiting phosphodiesterase activity.

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