Noguchi K, Sunagawa R, Kato T, Nagamine F, Sakanashi M
Department of Pharmacology, School of Medicine, Faculty of Medicine, University of the Ryukyus, Okinawa, Japan.
Eur J Pharmacol. 1987 Dec 1;144(2):201-10. doi: 10.1016/0014-2999(87)90520-6.
The study was conducted to evaluate the effects of intracoronary administration of dl-propranolol on coronary blood flow and regional myocardial function in anesthetized open-chest dogs. The results were compared with those obtained with d-propranolol, atenolol and lidocaine. Bolus intracoronary injections of dl-propranolol (0.02-2 mg) dose dependently produced transient increases in coronary blood flow and subsequent depression in regional segment shortening which qualitatively resembled those produced by the dextro isomer (0.02-2 mg) and lidocaine (0.2-10 mg). Atenolol (up to 2 mg) was almost devoid of these effects. Isoproterenol-induced responses were abolished by dl-propranolol and atenolol but only incompletely blocked by d-propranolol. These results demonstrate that propranolol at high doses has direct coronary vasodilating and cardiodepressant effects in situ, and indicate that the major part of these effects can be attributed to the membrane-stabilizing action rather than beta-adrenoceptor blockade.
本研究旨在评估在麻醉开胸犬体内冠状动脉内注射消旋普萘洛尔对冠状动脉血流量和局部心肌功能的影响。并将结果与右旋普萘洛尔、阿替洛尔和利多卡因的结果进行比较。冠状动脉内推注消旋普萘洛尔(0.02 - 2毫克)剂量依赖性地使冠状动脉血流量短暂增加,随后局部节段缩短出现抑制,这在性质上类似于右旋异构体(0.02 - 2毫克)和利多卡因(0.2 - 10毫克)所产生的作用。阿替洛尔(高达2毫克)几乎没有这些作用。消旋普萘洛尔和阿替洛尔可消除异丙肾上腺素诱导的反应,但右旋普萘洛尔只能不完全阻断。这些结果表明,高剂量的普萘洛尔在体内具有直接的冠状动脉扩张和心脏抑制作用,并表明这些作用的主要部分可归因于膜稳定作用而非β-肾上腺素能受体阻滞。