Application of a molecular genetic techniques has allowed the isolation and identification of more than 50 members of the G protein-coupled receptor family. Their specificities range from sensory receptors such as the opsins and odorant receptors through those for the amines, peptides and other small molecules to those for glycoprotein hormones. These studies make it clear that traditional pharmacological methods, often underestimate receptor diversity. G protein-coupled receptors share a common structure consisting of 7 transmembrane alpha helical segments. Receptor structure-function relationships are discussed in the light of results obtained by site-directed mutagenesis and the construction of chimeric receptors. Studies which have allowed the identification of ligand-binding domains, and of sequences defining G protein specificity as well as those involved in receptor desensitization and downregulation are also discussed.