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尼可地尔对犬冠状动脉舒张作用的机制

Mechanism of relaxant effects of nicorandil on the dog coronary artery.

作者信息

Imai S, Ushijima T, Nakazawa M, Nabata H, Sakai K

出版信息

Arch Int Pharmacodyn Ther. 1983 Oct;265(2):274-82.

PMID:6228201
Abstract

In order to search into the mechanism of the relaxant effects of nicorandil, a new coronary vasodilator, on the dog coronary artery, the effects of this substance on the potassium contracture were studied, and compared with those of nitroglycerin and nifedipine. All the three substances induced a dose-related relaxation (nifedipine greater than nitroglycerin greater than nicorandil). However, the increase in La3+-resistant 45Ca uptake was inhibited only by nifedipine. In a calcium-free EGTA containing medium caffeine induced a phasic contraction in the fully-depolarized preparation. Nicorandil produced an inhibition of this contraction, while nitroglycerin and nifedipine did not. It was concluded that nicorandil differs from the so-called calcium antagonists in the mechanism of relaxant action on the coronary artery. It also differs from nitroglycerin in that it produced an inhibition of caffeine-induced contraction.

摘要

为了探究新型冠状动脉扩张剂尼可地尔对犬冠状动脉舒张作用的机制,研究了该物质对钾离子收缩的影响,并与硝酸甘油和硝苯地平进行了比较。这三种物质均引起剂量相关的舒张作用(硝苯地平>硝酸甘油>尼可地尔)。然而,仅硝苯地平抑制了镧离子抗性45钙摄取的增加。在不含钙的乙二胺四乙酸(EGTA)培养基中,咖啡因在完全去极化的制剂中诱导了阶段性收缩。尼可地尔抑制了这种收缩,而硝酸甘油和硝苯地平则没有。得出的结论是,尼可地尔在冠状动脉舒张作用机制上不同于所谓的钙拮抗剂。它与硝酸甘油的不同之处还在于它能抑制咖啡因诱导的收缩。

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