Histamine H2 Receptor Antagonists: Small Molecules and Peptides

Histamine H₂ receptors are G_αs-protein-coupled receptors involved in the suppressive activities of histamine. H₂ receptors exhibit a widespread distribution and are found in the gastrointestinal tract, the central nervous system, smooth muscle cells, endothelial cells, cardiomyocytes and immune cells amongst others.

H₂ receptors regulate various functions of histamine, including heart contraction, gastric acid secretion, cell proliferation and differentiation, and immune responses. In the ...