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Adrenoceptors have been at the forefront of physiological and pharmacological research for a century. They served as prototypes for rationale drug design as recognized by a Nobel Prize to Sir James Black and for the molecular understanding and structure of G protein-coupled receptors as recognized by a Nobel Prize to Brian Kobilka and Robert J. Lefkowitz. Drugs directly or indirectly targeting adrenoceptors have become guideline-recommended treatments for more than 30 human and various animal diseases. This volume assembles leading experts on various types of adrenoceptor research to provide concise insight into the current standing and future direction of uses of adrenoceptor-targeted drugs and research in this field.