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International union of basic and clinical pharmacology. XCVIII. Histamine receptors.

Panula, P. and Chazot, P. and Cowart, M. and Gutzmer, R. and Leurs, R. and Liu, W.L. and Stark, H. and Thurmond, R.L. and Haas, H.L. (2015) 'International union of basic and clinical pharmacology. XCVIII. Histamine receptors.', Pharmacological reviews., 67 (3). pp. 601-655.


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.

Item Type:Article
Full text:Publisher-imposed embargo
(AM) Accepted Manuscript
File format - PDF (Copyright agreement prohibits open access to the full-text)
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Date accepted:No date available
Date deposited:06 May 2016
Date of first online publication:July 2015
Date first made open access:No date available

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