The effects of beta-1-adrenergic blockade (100 mg metoprolol) on metabolism in exercise was examined in 14 healthy males who worked for 50 min on a treadmill at 65% of their maximal exercise capacity. The tests were carried out in a double blind fashion. Glucose and lactate were determined in arterialized capillary blood, free fatty acids, glycerol, growth hormone, cortisol, glucagon, insulin, testosterone, and estradiol in serum, and adrenaline and noradrenaline in plasma. Lactate and glucose were not significantly affected by beta-1-adrenergic blockade, free fatty acids and glycerol were reduced by 50% and 30% respectively as compared with the unmedicated condition. Adrenaline and noradrenaline levels were increased by 104% and 54% respectively, growth hormone by 60%, cortisol by 72%, and glucagon by 36% when compared with the control experiments. Insulin and estradiol were unaffected, testosterone was depressed by 21% under medication. The results demonstrate that during prolonged exercise beta-1-adrenergic blockade depresses lipolysis. Energetic deficiency is prevented by counter-regulatory increases of various hormones. Consequently, from the metabolic point of view there is no indication of impairment of prolonged exercise capacity under beta-1-adrenergic blockade.