International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors
- 11 June 2015
- journal article
- review article
- Published by American Society for Pharmacology & Experimental Therapeutics (ASPET) in Pharmacological Reviews
- Vol. 67 (3), 601-655
- https://doi.org/10.1124/pr.114.010249
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.Keywords
This publication has 171 references indexed in Scilit:
- Antagonism of the histamine H4 receptor reduces LPS-induced TNF production in vivoInflammation Research, 2013
- Combinatorial roles for histamine H1‐H2 and H3‐H4 receptors in autoimmune inflammatory disease of the central nervous systemEuropean Journal of Immunology, 2012
- The waking brain: an updateCellular and Molecular Life Sciences, 2011
- Transporter‐Mediated Efflux Influences CNS Side Effects: ABCB1, from Antitarget to TargetMolecular Informatics, 2010
- The 7 TM G‐Protein‐Coupled Receptor Target FamilyChemMedChem, 2006
- The Rat H3 Receptor: Gene Organization and Multiple IsoformsBiochemical and Biophysical Research Communications, 2001
- Lysine200 Located in the Fifth Transmembrane Domain of the Histamine H1 Receptor Interacts with Histamine but Not with All H1 AgonistsBiochemical and Biophysical Research Communications, 1995
- The Guinea Pig Histamine H2 Receptor: Gene Cloning, Tissue Expression and Chromosomal Localization of Its Human CounterpartBiochemical and Biophysical Research Communications, 1995
- Histamine inhibits dopamine release in the mouse striatum via presynaptic H3 receptorsJournal of Neural Transmission, 1993
- (+)- and (-)-3-Methoxycyproheptadine. A comparative evaluation of the antiserotonin, antihistaminic, anticholinergic, and orexigenic properties with cyproheptadineJournal of Medicinal Chemistry, 1977