阿罗洛尔（一种α和β肾上腺素能受体拮抗剂）对大鼠肾皮质切片肾素释放的影响。

Effects of arotinolol, an alpha- and beta-adrenoceptor antagonist, on renin release from rat kidney cortical slices.

作者信息

Morimoto S, Miyawaki N, Sasaki Y, Matsumura Y

出版信息

Clin Exp Pharmacol Physiol. 1986 Jun;13(6):505-10. doi: 10.1111/j.1440-1681.1986.tb00931.x.

DOI:10.1111/j.1440-1681.1986.tb00931.x

Abstract

The effects of arotinolol on changes in renin release in rat kidney cortical slices in response to isoproterenol (IP) or norepinephrine (NE), were studied in comparison with those of AC-623, a main metabolite of arotinolol, and other typical adrenoceptor antagonists. Arotinolol, at concentrations of 10(-8) to 10(-4) mol/l, inhibited the increasing effect of 10(-6) mol/l IP on renin release, in a concentration-dependent manner. Similar results were observed with AC-623, propranolol or labetalol, although the inhibitory potencies of these agents were considerably lower than that of arotinolol. The blocking effect of arotinolol on the 10(-5) mol/l NE-induced decrease in renin release was much less potent than seen with other alpha-adrenoceptor blocking agents such as prazosin, phenoxybenzamine and labetalol. These data suggest that the potent blocking effects of arotinolol and its metabolite on the increased renin release in response to beta-adrenoceptor stimulation may contribute to the antihypertensive effect of this agent.

摘要

将阿罗洛尔与阿罗洛尔的主要代谢产物AC - 623及其他典型肾上腺素能受体拮抗剂相比较，研究了阿罗洛尔对大鼠肾皮质切片中肾素释放变化的影响，该变化是对异丙肾上腺素（IP）或去甲肾上腺素（NE）的反应。阿罗洛尔在浓度为10^(-8)至10^(-4) mol / l时，以浓度依赖的方式抑制10^(-6) mol / l IP对肾素释放的增加作用。AC - 623、普萘洛尔或拉贝洛尔也观察到类似结果，尽管这些药物的抑制效力明显低于阿罗洛尔。阿罗洛尔对10^(-5) mol / l NE诱导的肾素释放减少的阻断作用远不如其他α - 肾上腺素能受体阻断剂（如哌唑嗪、酚苄明和拉贝洛尔）明显。这些数据表明，阿罗洛尔及其代谢产物对β - 肾上腺素能受体刺激引起的肾素释放增加的强效阻断作用可能有助于该药物的降压作用。