The synthesis and the identification of histamine marked a milestone in both pharmacological and immunological research. Since Sir Henry Dale and Patrick Laidlaw described some of its physiological effects in vivo in 1910, histamine has been shown to play a key role in the control of gastric acid secretion and in allergic disorders. Using selective agonists and antagonists, as well as molecular biology tools, four histamine receptors (H 1 R, H 2 R, H 3 R and H 4 R) have been identified. The Nobel Prize in Physiology and Medicine was awarded to Daniel Bovet in 1957 for the discovery of antihistamines (anti-H 1 R) and to Sir James Black in 1988 for the identification of anti-H 2 R antagonists. Anti-H 1 R and anti- H 2 R histamine receptor antagonists have revolutionized the treatment of certain allergic disorders and gastric acid-related conditions, respectively. More recently, anti-H 3 R antagonists have entered early-phase clinical trials for possible application in obesity and a variety of neurologic disorders. The preferential expression of H 4 R by several immune cells and its involvement in the development of allergic inflammation provide the rationale for the use of anti-H 4 R antagonists in allergic and in other immune-related disorders.
ASJC Scopus subject areas
- Immunology and Microbiology(all)