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