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曲匹地尔的药理特性:与其他冠状动脉扩张剂的比较(作者译)

[Pharmacological properties of trapidil: comparison with other coronary vasodilators (author's transl)].

作者信息

Ohnishi H, Kosuzume H, Yamaguchi K, Sato M, Umehara S, Funato H, Itoh C, Suzuki K, Kitamura Y, Suzuki Y, Itoh R

出版信息

Nihon Yakurigaku Zasshi. 1980 Sep;76(6):495-503.

PMID:7009345
Abstract

Effects of trapidil and other coronary vasodilators on retrograde blood flow in acute coronary-ligated dogs, isolated large and small coronary arteries of pig, platelet aggregation, biosynthesis of prostacyclin in isolated aortic rings and hyperlipemia in quails were investigated. Trapidil showed an increase in retrograde blood flow while dipyridamole, nifedipine, diltiazem and dilazep did not. Trapidil and nitroglycerin relaxed large coronary arteries, while dipyridamole, diltiazem, dilazep and adenosine relaxed small arteries. Trapidil, dipyridamole, diltiazem and aspirin protected against the secondary phase of ADP-induced platelet aggregation in guinea-pig platelet rich plasma more effectively than did nifedipine and dilazep. Trapidil and aspirin protected only against rabbit platelet aggregation as induced by arachidonic acid. Moreover, only trapidil protected against platelet aggregation as induced by prostaglandin G2-thromboxane A2 mixture. Trapidil and dipyridamole enhanced the platelet aggregation protection of prostacyclin. Trapidil also facilitated biosynthesis of prostacyclin more markedly than did the other drugs. Trapidil increased serum content of HDL cholesterol and significantly lowered serum content of triglyceride and the ratio of LDL cholesterol to HDL cholesterol in hyperlipemic quails. Dipyridamole, diltiazem, nifedipine and dilazep, however, showed little effect.

摘要

研究了曲匹地尔和其他冠状动脉扩张剂对急性冠状动脉结扎犬的逆行血流、猪离体大、小冠状动脉、血小板聚集、离体主动脉环中前列环素的生物合成以及鹌鹑高脂血症的影响。曲匹地尔可使逆行血流增加,而双嘧达莫、硝苯地平、地尔硫䓬和己酮可可碱则无此作用。曲匹地尔和硝酸甘油可使大冠状动脉舒张,而双嘧达莫、地尔硫䓬、己酮可可碱和腺苷可使小动脉舒张。在豚鼠富含血小板血浆中,曲匹地尔、双嘧达莫、地尔硫䓬和阿司匹林对ADP诱导的血小板聚集的二期抑制作用比硝苯地平和己酮可可碱更有效。曲匹地尔和阿司匹林仅对花生四烯酸诱导的兔血小板聚集有抑制作用。此外,只有曲匹地尔对前列腺素G2-血栓素A2混合物诱导的血小板聚集有抑制作用。曲匹地尔和双嘧达莫增强了前列环素对血小板聚集的抑制作用。曲匹地尔比其他药物更显著地促进前列环素的生物合成。曲匹地尔可增加高脂血症鹌鹑血清中高密度脂蛋白胆固醇含量,并显著降低血清甘油三酯含量以及低密度脂蛋白胆固醇与高密度脂蛋白胆固醇的比值。然而,双嘧达莫、地尔硫䓬、硝苯地平和己酮可可碱的作用甚微。

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