一项关于几种β受体拮抗剂对突触前β肾上腺素能受体拮抗效力的动力学评估试验。

A trial for kinetic evaluation of the antagonistic potency of several beta-antagonists on presynaptic beta-adrenoceptors.

作者信息

Kuwahara M, Amano H, Kubo T, Misu Y

出版信息

Jpn J Pharmacol. 1987 Apr;43(4):445-8. doi: 10.1254/jjp.43.445.

DOI:10.1254/jjp.43.445

Abstract

The antagonistic potency, pA2, of several non-selective beta-antagonists on presynaptic beta-adrenoceptors was evaluated using a parallel line assay and MacKay's equation against isoproterenol-induced increases in 3H release in isolated guinea-pig pulmonary arteries preloaded with 3H-norepinephrine. Cumulatively applied isoproterenol at 10(-9) M, 10(-8) M and 10(-7) M dose-dependently increased 3H release evoked by transmural field stimulation at 1 Hz. beta-Antagonists tested dose-dependently antagonized the isoproterenol-induced increases. The order of pA2 was carteolol (11.23 +/- 0.09) greater than nadolol (9.78 +/- 0.05) greater than pindolol (9.59 +/- 0.03) greater than propranolol (9.26 +/- 0.17). Carteolol has the highest pA2 and is a useful tool for clarifying whether or not presynaptic beta-adrenoceptors tonically function.

摘要

使用平行线分析法和麦凯方程，针对异丙肾上腺素诱导的、预先用3H-去甲肾上腺素预加载的离体豚鼠肺动脉中3H释放量的增加，评估了几种非选择性β-拮抗剂对突触前β-肾上腺素能受体的拮抗效能（pA2）。以10(-9) M、10(-8) M和10(-7) M的剂量累积应用异丙肾上腺素，可使1 Hz跨壁电场刺激诱发的3H释放量呈剂量依赖性增加。所测试的β-拮抗剂呈剂量依赖性地拮抗异丙肾上腺素诱导的增加。pA2的顺序为：卡替洛尔（11.23±0.09）大于纳多洛尔（9.78±0.05）大于吲哚洛尔（9.59±0.03）大于普萘洛尔（9.26±0.17）。卡替洛尔具有最高的pA2，是阐明突触前β-肾上腺素能受体是否具有紧张性功能的有用工具。