新型β-肾上腺素受体阻滞剂阿罗洛尔（S-596）在离体犬冠状动脉中可能具有的α-肾上腺素受体阻断活性。

Possible alpha-adrenoceptor blocking activity of arotinolol (S-596), a new beta-adrenoceptor blocking agent in isolated dog coronary artery.

作者信息

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

出版信息

Pharmacology. 1984;29(4):204-9. doi: 10.1159/000138014.

PMID:6208564

Abstract

Effects of arotinolol on dog coronary arteries were investigated in vitro. In distal portions of left circumflex coronary arteries contracted with 3 X 10(-2)M KCl, norephinephrine relaxed the strips in a concentration-dependent fashion. Propranolol (10(-6)M) converted the norepinephrine-induced relaxations to contractions, and arotinolol (10(-6)-10(-5)M) inhibited the relaxations induced by norepinephrine in a concentration-dependent manner. In proximal portions of the strips after potassium-contracture, norephinephrine produced concentration-dependent contractions which were augmented by propranolol (10(-6)M) and inhibited by arotinolol (10(-6)-10(-5)M). These results suggest that arotinolol has an alpha-adrenoceptor blocking activity in addition to a beta-adrenoceptor blocking action in dog coronary arteries.

摘要

在体外研究了阿罗洛尔对犬冠状动脉的作用。在左旋冠状动脉远端部分用3×10⁻²M氯化钾使其收缩后，去甲肾上腺素使血管条呈浓度依赖性舒张。普萘洛尔（10⁻⁶M）使去甲肾上腺素诱导的舒张转为收缩，而阿罗洛尔（10⁻⁶ - 10⁻⁵M）以浓度依赖性方式抑制去甲肾上腺素诱导的舒张。在钾收缩后血管条的近端部分，去甲肾上腺素产生浓度依赖性收缩，普萘洛尔（10⁻⁶M）增强该收缩，而阿罗洛尔（10⁻⁶ - 10⁻⁵M）抑制该收缩。这些结果表明，阿罗洛尔在犬冠状动脉中除具有β - 肾上腺素受体阻断作用外，还具有α - 肾上腺素受体阻断活性。