The biological effects of epinephrine and norepinephrine are mediated via 9 different adrenergic receptor subtypes, which all belong to the superfamily of G protein-coupled receptors. Although pharmacological ligands for adrenergic receptors have an important place in medical therapy, the full therapeutic potential of the 9 adrenergic receptor subtypes has not been explored yet. To dissect the physiological relevance of adrenergic receptor subtype diversity, gene-targeted mouse models carrying deletions in these receptor genes ("knockout mice") have been generated. This review gives an overview of the phenotypes observed in mice deficient in adrenergic receptors and discusses the therapeutic relevance of subtype-specific drug therapy.