Rochette L, Didier J P, Moreau D, Bralet J, Opie L H
Am Heart J. 1984 Jun;107(6):1132-41. doi: 10.1016/0002-8703(84)90268-0.
The role of catecholamines in the genesis of ventricular arrhythmias during the reperfusion period following coronary occlusion remains incompletely understood. An isolated rat heart preparation, free from the influence of autonomic innervation or of circulating catecholamines, was used to assess the effects of beta-adrenoceptor blockade. The hearts were prelabeled with tritiated norepinephrine ( NE3H ), and the total radioactivity and that in NE3H were measured in the effluent coronary flow. The left main coronary artery was ligated for 10 minutes after which reperfusion followed. The liberation of NE3H and the development of ventricular tachycardia and fibrillation were monitored throughout. The cardioselective beta-antagonist agent, acebutolol, in a high concentration (1.1 X 10(-4)M), had good beta-antagonist effect in response to the added isoproterenol (10(-6)M); this concentration of acebutolol also suppressed sustained reperfusion ventricular arrhythmias but unexpectedly increased the release of NE3H . Atenolol, another cardioselective agent, did not prevent reperfusion ventricular arrhythmias even in a high concentration of 40 mg/L (1.5 X 10(-4)M). The d-isomer of propranolol, with poorer beta-antagonist properties than the l-isomer, prevented such ventricular arrhythmias in a concentration of 1.3 X 10(-5)M, which was low when compared to that of atenolol. It is proposed that the beta-antagonist activity of the compounds tested could not explain the inhibition of reperfusion ventricular arrhythmias and that another quality such as membrane-stabilizing activity may be involved.
儿茶酚胺在冠状动脉闭塞后再灌注期室性心律失常发生中的作用仍未完全明了。采用一种不受自主神经支配或循环儿茶酚胺影响的离体大鼠心脏标本,来评估β-肾上腺素能受体阻断的作用。心脏预先用氚标记的去甲肾上腺素(NE3H)标记,然后测量流出的冠状动脉血流中的总放射性及NE3H的放射性。结扎左冠状动脉主干10分钟,随后进行再灌注。全程监测NE3H的释放以及室性心动过速和心室颤动的发生情况。高浓度(1.1×10(-4)M)的心脏选择性β-拮抗剂醋丁洛尔,对加入的异丙肾上腺素(10(-6)M)有良好的β-拮抗作用;该浓度的醋丁洛尔也能抑制持续性再灌注室性心律失常,但出乎意料的是增加了NE3H的释放。另一种心脏选择性药物阿替洛尔,即使在40mg/L(1.5×10(-4)M)的高浓度下也不能预防再灌注室性心律失常。普萘洛尔的d-异构体,其β-拮抗特性比l-异构体差,在1.3×10(-5)M的浓度下就能预防此类室性心律失常,与阿替洛尔相比该浓度较低。有人提出,所测试化合物的β-拮抗活性无法解释对再灌注室性心律失常的抑制作用,可能涉及另一种性质,如膜稳定活性。