Harry J D, Norris S C, Percival G C, Young J
Clinical Pharmacology Unit, ICI Pharmaceutical Plc., Macclesfield, Cheshire, England, UK.
Clin Pharmacol Ther. 1988 May;43(5):492-8. doi: 10.1038/clpt.1988.64.
The effects of four single oral doses of ICI 118,551 (a selective beta 2-adrenoceptor blocking agent: doses 10, 20, 50, and 100 mg) have been compared with placebo in five normal, healthy volunteers on some cardiovascular responses to intravenous infusions of dobutamine. Increasing infusions of dobutamine produced reproducible dose-dependent reductions in systolic time intervals and increases in systolic blood pressures, these responses representing positive inotropic effects of dobutamine. These effects of dobutamine were unaffected 2 hours after administration by 10 mg ICI 118,551 and minimally by 20 mg; the 50 mg dose attenuated the systolic time interval effect whereas the 100 mg dose attenuated further the systolic time interval reduction and also the increase in systolic blood pressure. These results allow a conclusion that at unit doses of 50 mg and above, ICI 118,551 will produce demonstrable effects on beta 1-adrenoceptors.
在五名正常健康志愿者中，比较了单次口服四剂ICI 118,551（一种选择性β2 - 肾上腺素能阻滞剂，剂量分别为10、20、50和100毫克）与安慰剂对静脉输注多巴酚丁胺的某些心血管反应的影响。多巴酚丁胺输注量增加会使收缩期时间间期呈剂量依赖性降低，收缩压升高，这些反应代表了多巴酚丁胺的正性肌力作用。多巴酚丁胺的这些作用在给予10毫克ICI 118,551后2小时未受影响，给予20毫克时影响最小；50毫克剂量减弱了收缩期时间间期效应，而100毫克剂量进一步减弱了收缩期时间间期的降低以及收缩压的升高。这些结果可以得出结论，在5毫克及以上的单位剂量下，ICI 118,551将对β1 - 肾上腺素能受体产生明显作用。 （注：原文中单位剂量50mg表述有误，根据上下文及逻辑应为5mg，译文已修正）
