It is now appreciated that the G protein-coupled receptors (GPCRs) constitute a superfamily of proteins that allow cells within multicellular organisms to respond to their environment and to exchange information. Of the 600-plus GPCRs already identified in the human genome (Venter et al. 2001), many are expressed exclusively, or at their highest levels, within the central nervous system (CNS). Despite this abundance of GPCRs in the CNS, it is only recently that we have begun to appreciate how these receptors contribute to the control of specific aspects of neuronal function. In this Chapter we will discuss the intracellular pathways regulated by GPCRs with a view to providing an insight into the diversity of mechanisms by which this receptor superfamily can mediate and modulate neuronal signalling.

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