抗高血压药尼普地洛对犬离体冠状动脉的作用。

Effects of an antihypertensive agent, nipradilol, on isolated coronary artery of the dog.

作者信息

Sakanashi M, Takeo S, Ito H, Noguchi K, Miyamato Y, Higa T

出版信息

Pharmacology. 1984;29(5):241-6. doi: 10.1159/000138019.

Abstract

Effects of nipradilol on proximal, middle and distal portions of left coronary arteries of the dog were investigated in vitro. Nipradilol (10(-7)-10(-3) M) produced a concentration-dependent relaxation in helical strips of isolated coronary artery under potassium contracture. The relaxation in the middle portions was most pronounced, it was 10% of the equimolar concentrations of nitroglycerin and significantly greater than that of propranolol. In the proximal portions of the coronary arteries, nipradilol (3 X 10(-8)-3 X 10(-7) M) showed a tendency to augment the contractile responses to norepinephrine; in the middle portions it reversed the relaxant responses to norepinephrine into contractile effects in a concentration-dependent manner. In distal portions, nipradilol significantly decreased the relaxant responses of the strips to norepinephrine. The findings demonstrate direct vasodilating and beta-adrenoceptor blocking actions of nipradilol in isolated coronary arteries of the dog.

摘要

在体外研究了尼普地洛对犬左冠状动脉近端、中段和远端的影响。尼普地洛（10⁻⁷ - 10⁻³ M）在钾收缩状态下，使离体冠状动脉螺旋条产生浓度依赖性舒张。中段的舒张最为明显，相当于硝酸甘油等摩尔浓度的10%，且显著大于普萘洛尔。在冠状动脉近端，尼普地洛（3×10⁻⁸ - 3×10⁻⁷ M）表现出增强对去甲肾上腺素收缩反应的趋势；在中段，它以浓度依赖性方式将对去甲肾上腺素的舒张反应转变为收缩作用。在远端，尼普地洛显著降低了条带对去甲肾上腺素的舒张反应。这些发现证明了尼普地洛在犬离体冠状动脉中的直接血管舒张和β - 肾上腺素受体阻断作用。