G protein-coupled receptors (GPCRs) are widely expressed in the central nervous system (CNS), where they mediate and modulate synaptic transmission in the brain and spinal cord. A large percentage of CNS drugs target GPCRs, and these compounds have been exploited scientifically to further explore the molecular natures and physiological functions of these target proteins. Large GPCR groups such as the dopamine, serotonin, and opioid receptor families show indications of both redundancy and exquisite receptor subtype selectivity of biological responses. Structural studies are now adding to our understanding of GPCR activation at the molecular level, although the influences of the neuronal cell environment and synaptic architecture remain key determinants in the functioning of GPCRs in the CNS. This chapter provides an overview of the roles of neuronal GPCRs in normal and disease states in the areas of psychiatry, pain, neurodegeneration, and neuroendocrine function.

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