This study was intended to investigate the effects of energy restriction on the acute responses of platelet alpha 2- and lymphocyte beta 2-adrenoceptors to exercise in obese female subjects. Seven obese females were restricted to a low-energy formula diet (2.0 MJ/day) for 4 wk. As result of the diet, there was a 7.8-kg weight loss. No significant changes could be detected in sleeping and resting metabolic rate expressed per kilogram fat-free mass. Basal venous glucose, insulin, and norepinephrine levels decreased as a result of the diet, whereas free fatty acid values increased. Before the diet, 60 min of exercise (45% peak mechanical power) caused no alteration in the density of lymphocyte beta 2-adrenoceptors. At the end of 4 wk of dieting, the density was significantly increased in response to exercise, together with a higher thermogenic and lipolytic response and decreased venous insulin levels. Energy restriction resulted in an increased basal platelet alpha 2-adrenoceptor density, whereas exercise did not modify density and affinity of platelet alpha 2-adrenoceptors. The results indicate that adrenoceptor numbers can be modulated by energy restriction in obesity. Modulation of adrenoceptor density may play a role in increased exercise-induced lipolysis during energy restriction.