Engel B, Einstein R, Goodman A H
Eur J Pharmacol. 1985 Oct 8;116(1-2):97-104. doi: 10.1016/0014-2999(85)90189-x.
The cardiovascular effects of the selective beta 2-adrenoceptor agonists salbutamol and terbutaline have been evaluated in anaesthetised, areflexic dogs. The preparation was designed to reduce the effects of changes in cardiac function mediated via reflex responses to changes in blood pressure. The effects of the selective beta 2-adrenoceptor agonists on heart rate, hindlimb blood flow, left ventricular pressure, max dP/dt and (dP/dt)/IIT (integrated isometric tension) were compared to those of isoprenaline, while blood pressure was held constant. All three drugs produced dose-dependent increases in heart rate, myocardial contractility and iliac blood flow. When equiactive inotropic doses of isoprenaline and salbutamol were compared, salbutamol produced a significantly lower chronotropic effect. A similar inotropic selectivity was found when terbutaline was compared to isoprenaline. beta 2-Adrenoceptor blockade abolished this selectivity. It is concluded that, in the absence of autonomic reflex activity, the beta 2-selective adrenoceptor agonists are relatively selective inotropic stimulants.
在麻醉的、无反射的犬中评估了选择性β2肾上腺素能受体激动剂沙丁胺醇和特布他林的心血管效应。该实验设计旨在减少因血压变化的反射反应介导的心脏功能改变的影响。在血压保持恒定的情况下,将选择性β2肾上腺素能受体激动剂对心率、后肢血流量、左心室压力、最大dP/dt以及(dP/dt)/IIT(等长张力积分)的影响与异丙肾上腺素的影响进行了比较。所有三种药物均使心率、心肌收缩力和髂血流量呈剂量依赖性增加。当比较等活性变力剂量的异丙肾上腺素和沙丁胺醇时,沙丁胺醇产生的变时效应明显较低。当比较特布他林与异丙肾上腺素时,发现了类似的变力选择性。β2肾上腺素能受体阻断消除了这种选择性。得出的结论是,在没有自主反射活动的情况下,β2选择性肾上腺素能受体激动剂是相对选择性的变力刺激剂。