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International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

Panula, P.; Chazot, P.; Cowart, M.; Gutzmer, R.; Leurs, R.; Liu, W.L.; Stark, H.; Thurmond, R.L.; Haas, H.L.

Authors

P. Panula

M. Cowart

R. Gutzmer

R. Leurs

W.L. Liu

H. Stark

R.L. Thurmond

H.L. Haas



Abstract

Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues. Its physiological functions are mediated by four 7-transmembrane G protein–coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R was identified in the 1970s and led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The crystal structure of ligand-bound H1R has rendered it possible to design new ligands with novel properties. The H3R is an autoreceptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. A block of these actions promotes waking. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.

Citation

Panula, P., Chazot, P., Cowart, M., Gutzmer, R., Leurs, R., Liu, W., …Haas, H. (2015). International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors. Pharmacological Reviews, 67(3), 601-655. https://doi.org/10.1124/pr.114.010249

Journal Article Type Article
Publication Date Jul 1, 2015
Deposit Date Feb 2, 2016
Publicly Available Date Mar 28, 2024
Journal Pharmacological Reviews
Print ISSN 0031-6997
Electronic ISSN 1521-0081
Publisher American Society for Pharmacology and Experimental Therapeutics (ASPET)
Peer Reviewed Peer Reviewed
Volume 67
Issue 3
Pages 601-655
DOI https://doi.org/10.1124/pr.114.010249