地拉西普的新衍生物K-7259对腺苷心血管作用的影响:与地拉西普的比较。

A Hara, M Akahira, Y Abiko
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引用次数: 0

摘要

在豚鼠主动脉环和离体灌注心脏中研究了地拉西普的新衍生物K-7259对腺苷心血管作用的影响,并与地拉西普进行了比较。腺苷在苯肾上腺素(2 × 10(-6) M)收缩的主动脉环中产生浓度依赖性松弛,并在离体灌注心脏中表现出负的变时效应。地拉西普(10(-8)、10(-7)和10(-6)M)以浓度依赖性的方式显著增强腺苷对主动脉环的舒张作用。然而,K-7259 (10(-6) M)不增强腺苷的松弛作用,尽管高浓度K-7259 (10(-5) M)轻微但显著增强腺苷的松弛作用。地拉西普(10(-7)和10(-6)M)也能增强腺苷的负变时作用,而K-7259 (10(-6) M)则不能,说明与地拉西普相比,K-7259对腺苷心血管效应的增强作用非常弱。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Effect of K-7259, a novel derivative of dilazep, on cardiovascular actions of adenosine: comparison with dilazep.

The effect of K-7259, a novel derivative of dilazep, on the cardiovascular action of adenosine was studied in the aortic ring and isolated perfused heart in guinea-pigs, and compared with that of dilazep. Adenosine produced a concentration-dependent relaxation in phenylephrine (2 x 10(-6) M)-contracted aortic rings and exhibited a negative chronotropic effect in the isolated perfused heart. Dilazep (10(-8), 10(-7) and 10(-6) M) potentiated significantly the relaxing action of adenosine on the aortic ring in a concentration-dependent way. K-7259 (10(-6) M), however, did not potentiate the relaxing action of adenosine, although the high concentration of K-7259 (10(-5) M) potentiated it slightly but significantly. The negative chronotropic effect of adenosine was also potentiated by dilazep (10(-7) and 10(-6) M), but not by K-7259 (10(-6) M). These results suggest that the potentiating action of K-7259 on the cardiovascular effects of adenosine is very weak when compared with that of dilazep.

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