Eight healthy untrained male volunteers pedalled a cycle ergometer according to two exercise protocols: the first involved step-wise increasing physical exercise to maximal (MPE); the second involved prolonged (35 min) submaximal physical exercise (PPE) at 70% of the individual's maximal oxygen uptake. Each volunteer performed these exercise twice, following either an intravenous injection of phosphocreatine (PCr) or a placebo of an isotonic NaCl solution. Anaerobic threshold (AT) was determined from the point of departure of the ventilatory response from linearity and from the sudden increase in venous blood lactate concentrations during MPE. After exercise following placebo administration we observed increases in concentrations of blood substrates, plasma adrenocorticotropin (ACTH), growth hormone and cortisol and in the number of glucocorticoid receptors in lymphocytes without changes in the dissociation constant. Intravenous administration of PCr (starting 1 day before exercise) led to an increase in the total workload (on average by 5.8%) and in AT (on average by 6.8%) during MPE and to a better tolerance of exercise during PPE. Following PCr administration we observed lower blood lactate concentrations and different patterns of some enzyme activities, less pronounced changes in plasma ACTH and cortisol concentrations and in glucocorticoid binding in lymphocytes, but no changes in plasma growth hormone concentrations compared to the placebo. The results showed that intense physical exercise led not only to increases in blood hormone concentrations but also to an increase in the density of glucocorticoid receptors in lymphocytes. Intravenous PCr injection led to smaller changes in ACTH and cortisol concentrations as well as to a lower activation of glucocorticoid binding in lymphocytes.