H2 Histamine Receptor Antibodies
The classical antihistamines reduce the effects of histamine on many tissues, however, the effects of histamine on stimulation of gastric acid secretion were resistant to antagonism by these compounds suggesting the presence of at least two histamine receptors. This was confirmed by the development of selective antagonists for the H2 receptor by Sir James Black and colleagues. Burimamide was the first compound to be described with selectivity for the H2 receptor, and a large number of more potent and selective H2 receptor antagonists have since been developed - including cimetidine, ranitidine and tiotidine. H2 receptor knockout mice develop normally with normal basal gastric acid levels. However they exhibit hypertrophy of gastric mucosa and an increase in the number of parietal and enterochromaffin-like (ECL) cells. The H2 receptor primarily couples to Gs proteins to stimulate adenylyl cyclase. The H2 receptor is phosphorylated at Serine319/Ser322 (pS319/pS322-H2) in an agonist dependent manner.
For more information on histamine receptor pharmacology please refer to the IUPHAR database. For further reading refer to:
Chazot P, Cowart M, Fukui H, Ganellin CR, Gutzmer R, Haas HL, Hill SJ, Hills R, Leurs R, Levi R, Liu S, Panula P, Schunack W, Schwartz JC, Seifert R, Shankley NP, Stark H, Thurmond R, Timmerman H, Young JM. Histamine receptors in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F33/2023.1.