Keul J, Lehmann M, Wybitul K
Arzneimittelforschung. 1981;31(11):1948-53.
Plasma catecholamines, glucose, lactate, free fatty acids, and glycerol in the blood, as well as heart rate, oxygen intake, and work capacity have been examined in 9 healthy subjects (28.5 +/- 2 years) at rest, during submaximum and maximum ergometric exercise, after oral administration of a placebo and of 10 mg O-[3-(tert.-butylamino)-2-hydroxypropoxy]-benzonitril (bunitrolol, Stresson), respectively. The results are as follows: 1. As caused by the intrinsic activity of bunitrolol, the heart rate does not show nearly any reduction at rest and during submaximum physical exercise. At maximum exercise level the heart rate is 37 beats/min lower with bunitrolol. The limitation of heart function leads to a work capacity reduction of approx. 14%. 2. After administration of bunitrolol, adrenaline level is significantly lower at rest and during submaximum exercise than with placebo. At a 200 W level, the concentration is higher with bunitrolol, but the maximum results are not attained with placebo. In relation to the percentile of the maximum work capacity, plasma catecholamine level shows no differences with placebo and with bunitrolol, respectively, except that it is lower during maximum exercise and the recovery phase. 3. Glucose, free fatty acids, and glycerol levels show no significant changes with bunitrolol. Lactate decreases significantly after bunitrolol at submaximal exercise levels and during the recovery stage, which can be looked upon as an indication of a glycolysis restriction.
对9名健康受试者(28.5±2岁)在静息状态、次极量和极量测力计运动期间、口服安慰剂以及分别口服10毫克O-[3-(叔丁氨基)-2-羟基丙氧基]-苄腈(布尼洛尔,Stresson)后,检测了血浆儿茶酚胺、葡萄糖、乳酸、游离脂肪酸和甘油水平,以及心率、摄氧量和工作能力。结果如下:1. 由于布尼洛尔的内在活性,静息和次极量体育锻炼期间心率几乎没有降低。在极量运动水平时,服用布尼洛尔时心率降低37次/分钟。心脏功能受限导致工作能力降低约14%。2. 服用布尼洛尔后,静息和次极量运动期间肾上腺素水平显著低于服用安慰剂时。在200瓦水平时,布尼洛尔组的浓度较高,但服用安慰剂时未达到最大值。相对于最大工作能力的百分位数,血浆儿茶酚胺水平在服用安慰剂和布尼洛尔时分别无差异,只是在极量运动和恢复阶段较低。3. 布尼洛尔对葡萄糖、游离脂肪酸和甘油水平无显著影响。在次极量运动水平和恢复阶段,布尼洛尔使乳酸显著降低,这可视为糖酵解受限的一个指标。