British Journal of Pharmacology (2006) 147, S127–S135 & 2006 Nature Publishing Group All rights reserved 0007–1188/06 $
Histamine and its receptors
*,1Mike E. Parsons & 2C. Robin Ganellin
1Department of Life Sciences, University of Hertfordshire, Hatfield, Hertfordshire AL10 9AB and 2Department of Chemistry,
Christopher Ingold Laboratories, University College London, London WC1H OAJ
This article reviews the development of our knowledge of the actions of histamine which have taken
place duringthe course of the 20th century. Histamine has been shown to have a key physiologicalrole
in the control of gastric acid secretion and a pathophysiological role in a range of allergic disorders.
The synthesis of, and pharmacological studies on, selective agonists and antagonists has established
the existence of four types of histamine receptor and histamine receptor antagonists have found very
important therapeutic applications. Thus, in the 1940s, H1-receptor antagonists (‘the antihistamines’)
yielded and still provide valuable treatment for allergic conditions such as hay fever and rhinitis. In
the late 1970s and 1980s, H2-receptor antagonists (in the discovery of which the two authors were
personally involved) revolutionised the treatment of peptic ulcer and other gastric acid-related
diseases. The H3-receptor antagonists, although available since 1987, hav
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