Abstract
The G‐protein‐coupled receptor (GPCR) family represents the largest and most versatile group of cell surface receptors. Drugs active at these receptors have therapeutic actions across a wide range of human diseases ranging from allergic rhinitis to pain, hypertension and schizophrenia. This review provides a brief historical overview of the properties and signalling characteristics of this important family of receptors.British Journal of Pharmacology (2006) 147, S27–S37. doi:10.1038/sj.bjp.0706455