Histamine H2 Receptors
Histamine H2 receptors are Gαs-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 and endothelial cells.
Histamine H2 Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 0668 | Amthamine dihydrobromide |
| Highly selective standard H2 agonist | |
| 3545 | Histamine dihydrochloride |
| Endogenous histamine receptor agonist | |
| 0646 | HTMT dimaleate |
| H2/ H1 agonist | |
Histamine H2 Receptor Inverse Agonists |
|
| Cat. No. | Product Name / Activity |
| 7290 | Famotidine |
| Potent and high affinity H2 biased inverse agonist | |
Histamine H2 Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 0902 | Cimetidine |
| H2 antagonist, I1 agonist | |
| 0826 | Tiotidine |
| Potent and selective H2 antagonist | |
| 1070 | Zolantidine dimaleate |
| Potent, centrally active H2 antagonist | |
Histamine H2 receptors are Gαs-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 immune system, H2 activation negatively regulates basophils and mast cells, and inhibits antibody synthesis, T cell production, cell-mediated cytolysis and cytokine production. H2 receptors are present on Th2 cells and activation increases the synthesis of cytokines such as IL-4, IL-5, IL-10 and IL-13. Furthermore, histamine-induced T cell suppressor activity is mediated through H2 receptors.
Due to their role in gastric acid secretion, H2 receptor overactivity is a cause of gastric ulcers, and pharmacological inhibition of these receptors is an effective treatment for this condition.
The human gene encoding the H2 receptor is localized to chromosome 5q35.3.
External sources of pharmacological information for Histamine H2 Receptors :
Literature for Histamine H2 Receptors
Tocris offers the following scientific literature for Histamine H2 Receptors to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.
Our Histamine review gives an overview of the different histamine receptor subtypes, as well as highlighting pharmacological ligands for their study.
Request copyRequest PDF