Abernethy D R, Arendt R M, Greenblatt D J
Am Heart J. 1985 May;109(5 Pt 2):1120-5. doi: 10.1016/0002-8703(85)90695-7.
Studies in various animal models have shown acebutolol to be a relatively cardioselective beta-adrenoceptor-blocking agent possessing both partial agonist and membrane-stabilizing activities. The latter property may not be significant at clinically used doses. Acebutolol has both antihypertensive and antiarrhythmic effects. As with beta blockers in general, the antihypertensive mechanism of acebutolol is not known. The antiarrhythmic activity of acebutolol may be related to beta blockade. Acebutolol is relatively hydrophilic and does not readily cross the blood-brain barrier, a fact that may be clinically significant in reducing the frequency and severity of central nervous system adverse effects. The pharmacologic profile of diacetolol, acebutolol's major metabolite, is similar to that of the parent compound in beta-blocking potency, cardioselectivity, and partial agonist activity. Diacetolol, however, does not possess membrane-stabilizing activity.
在多种动物模型中进行的研究表明，醋丁洛尔是一种相对具有心脏选择性的β-肾上腺素受体阻滞剂，兼具部分激动剂和膜稳定活性。后一种特性在临床使用剂量下可能并不显著。醋丁洛尔具有抗高血压和抗心律失常作用。与一般的β受体阻滞剂一样，醋丁洛尔的抗高血压机制尚不清楚。醋丁洛尔的抗心律失常活性可能与β受体阻滞有关。醋丁洛尔相对亲水性强，不易穿过血脑屏障，这一事实在降低中枢神经系统不良反应的频率和严重程度方面可能具有临床意义。醋丁洛尔的主要代谢产物双醋洛尔在β受体阻滞效能、心脏选择性和部分激动剂活性方面的药理特性与母体化合物相似。然而，双醋洛尔不具有膜稳定活性。
