Background: Beta 2-adrenoceptor agonists have been shown to reduce allergen-induced skin whealing responses via inhibition of mediator release. Objective: To study whether beta 2-adrenoceptor agonists have a direct action against inflammatory mediator-induced skin whealing responses. Methods: We examined the effect of procaterol, a beta 2-adrenoceptor agonist, on skin whealing responses to histamine, platelet-activating factor (PAF), substance P, or bradykinin in eight asthmatic children in a double-blind, randomized, crossover study. Two hours after taking procaterol (50 mu g) or placebo orally, the subjects were given these mediators intradermally at a concentration of 10(-5) M. Results: Procaterol has a small but significant inhibitory effect on wheal formation following the intradermal injection of histamine and PAF by an average of 15% (P < .05) and 18% (P < .05) respectively but not against substance P or bradykinin. Conclusions: Our results suggest that although beta 2-adrenoceptor agonists may have an inhibitory effect against plasma exudation from microvasculature in the human skin, bronchodilatory effects are more prominent.