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.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
0668 Amthamine dihydrobromide
Highly selective standard H2 agonist
0506 Dimaprit dihydrochloride
Standard H2 selective agonist
3545 Histamine dihydrochloride
Endogenous histamine receptor agonist
0646 HTMT dimaleate
H2/ H1 agonist

Antagonists

Cat No Product Name / Activity
0721 Aminopotentidine
H2 antagonist
0902 Cimetidine
H2 antagonist, I1 agonist
0833 ICI 162,846
Potent H2 antagonist, active in vivo
1967 Ranitidine hydrochloride
Selective H2 antagonist
0826 Tiotidine
Potent, 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

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Histamine Receptors

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.

Asthma

Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

Histamine H2 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human HRH2 NM_022304 P25021
Mouse Hrh2 NM_001010973 P97292
Rat Hrh2 NM_012965 P25102