Zaroslinski J, Borgman R J, O'Donnell J P, Anderson W G, Erhardt P W, Kam S T, Reynolds R D, Lee R J, Gorczynski R J
Life Sci. 1982 Aug 30;31(9):899-907. doi: 10.1016/0024-3205(82)90547-1.
Beta-blockade is of proven value in the therapy of acute myocardial infarction but, unfortunately, may produce cardiac failure by removal of needed sympathetic support. The long duration of action of available blockers (hours) makes reversal of failure a complicated problem and precludes rapid modification of therapy to match changing autonomic conditions. To improve the safety and efficacy of beta-blockade in this setting we have developed the concept of ultra-short beta-blockade and have identified a novel beta-blocker (ASL-8052) which possesses a duration of action less than 15 minutes. This compound is cardioselective and possesses efficacy in an animal model of acute myocardial infarction. It, therefore, appears to be suitable for rapid attainment of controlled levels of beta-blockade via intravenous infusion and rapid recovery from beta-blockade if required by the clinical situation. The compound should, therefore, be useful for safe therapy in critically ill cardiac patients.
β受体阻滞剂在急性心肌梗死治疗中的价值已得到证实，但不幸的是，它可能通过去除所需的交感神经支持而导致心力衰竭。现有阻滞剂的作用时间较长（数小时），这使得心力衰竭的逆转成为一个复杂的问题，并且排除了根据自主神经状态变化快速调整治疗方案的可能性。为了提高β受体阻滞剂在这种情况下的安全性和有效性，我们提出了超短效β受体阻滞的概念，并确定了一种新型β受体阻滞剂（ASL-8052），其作用时间小于15分钟。该化合物具有心脏选择性，在急性心肌梗死动物模型中具有疗效。因此，它似乎适合通过静脉输注快速达到可控的β受体阻滞水平，并在临床情况需要时快速从β受体阻滞中恢复。因此，该化合物对于危重心脏病患者的安全治疗应该是有用的。
