Pharmacological and molecular cloning studies have shown that the superfamily of G-protein coupled receptors (GPCRs) forms one of the largest and most diverse protein families in nature. They are involved in the modulation of almost all our bodily functions and are pivotal in the regulation and control of central nervous system function. As such, pharmacological manipulation of GPCRs has been demonstrated to be valuable in the treatment of diseases of the central nervous system, ranging from Alzhmeimer's disease to schizophrenia and continues to be a key area of investigation in the search for tomorrow's medicines. The aim of this book is to bring together, for the first time in one volume, all aspects of GPCR structure and function, with an emphasis on receptors expressed in the central nervous system. The book comprises two major parts: part one provides a detailed overview of GPCR superfamily structure and function, including reviews of the mechanisms of ligand activation and inactivation, signalling through G-proteins and downstream signal transduction pathways and effector systems. Part two focuses on individual members of each of the three subfamilies of the GPCR superfamily, providing specific information about their localization, pharmacology, physiology and disease relevance. GPCRs in the CNS is essential reading for neuroscientists, pharmacologists, biochemists, molecular biologists, physiologists and all those involved in the process of drug discovery.