Historical Perspectives -- Adrenergic Receptors -- Structure-Function -- Ligand Binding, Activation, and Agonist Trafficking -- New Signal Transduction Paradigms -- Regulation of the Cellular Localization and Trafficking of the Adrenergic Receptors -- Adrenergic Receptors in Clinical Medicine -- Imaging Adrenergic Receptors and Their Function -- Use of Fluorescent Ligands and Receptors to Visualize Adrenergic Receptors -- Localization of Adrenergic Receptor Subtypes and Transgenic Expression of Fluorescent-Tagged Receptors -- Genetically Altered Mouse Models -- The ?1-Adrenergic Receptors -- The ?2-Adrenergic Receptors -- The ?-Adrenergic Receptors -- Lessons From Overexpressed Mouse Models -- Adrenergic Receptor Signaling Components in Gene Therapy -- Pharmacogenomics -- Genetic, Molecular, and Clinical Characterization of Adrenergic Receptor Polymorphisms -- Microarray Analysis of Novel Adrenergic Receptor Functions -- Summary and Future Endeavors -- Summary and Future Endeavors. The adrenergic receptors control many critical functions of the heart, kidney, brain, and all organs under autonomic control. Today significant opportunities exist for molecular and genetic analysis of their function and signaling pathways. In The Adrenergic Receptors: In the 21st Century, senior scientists who have developed novel molecular approaches describe the state-of-the-art understanding of the structure and function of the adrenergic receptor subtypes, as well as the role played by these receptors in physiological and pathophysiological settings. Topics range from structure-function studies and the imaging of adrenergic receptors to the use of genetically altered mouse models and pharmacogenomics. Many of the methods described can be applied to characterize any receptor of interest. Highlights include a survey of the knockout and overexpressed mouse models, a review of the new ways that adrenergic receptors can signal, and the effects of polymorphisms on both clinical outcomes and potential gene therapy applications. Additional chapters address modern techniques for assessing adrenergic function, such as fluorescent labeling and microarrays, and offer an insightful historical survey of the extraordinary progress made in our understanding of these receptors in the twentieth century. Comprehensive and authoritative, The Adrenergic Receptors: In the 21st Century provides researchers-through its side-by-side comparison of all the adrenergic receptors (a1, a2, and b) and their subtypes-with an excellent survey of the field, including the rationale for how best to design better drugs for control of the heart, blood pressure, and related pathophysiological systems.