beta-Adrenoceptors of the beta1 and beta2 subtypes classically mediate the effects of catecholamines on the contractility of cardiac muscle and the relaxation of vascular smooth muscle. Since the molecular characterization of the beta3-adrenoceptor in 1989, most studies of this adrenoceptor subtype have focused on its control of lipolysis in adipose tissues. However, more recent studies have investigated the involvement of beta3-adrenoceptors in the physiological control of cardiac and vascular contractility. In this article, the pharmacological and molecular evidence that supports the functional role of beta3-adrenoceptors in cardiovasculartissues of various species, including humans, will be discussed. These data might provide new insights into our understanding of the abnormal responsiveness of the cardiovascular system to catecholamines in heart failure and its treatment with beta3-adrenoceptor antagonists.