RT Journal Article
SR Electronic
T1 International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors
JF Pharmacological Reviews
JO Pharmacol Rev
FD American Society for Pharmacology and Experimental Therapeutics
SP 601
OP 655
DO 10.1124/pr.114.010249
VO 67
IS 3
A1 Pertti Panula
A1 Paul L. Chazot
A1 Marlon Cowart
A1 Ralf Gutzmer
A1 Rob Leurs
A1 Wai L. S. Liu
A1 Holger Stark
A1 Robin L. Thurmond
A1 Helmut L. Haas
A2 Eliot H. Ohlstein
YR 2015
UL http://pharmrev.aspetjournals.org/content/67/3/601.abstract
AB 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.