Histamine H2 Receptors

Supporting information

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.

To view external sources of pharmacological information for Histamine H2 Receptors, please click here: IUPHAR Receptor Code and BJP Guide

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

Literature for Histamine H2 Receptors

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Asthma Life Science Poster

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GPCR Product Listing

GPCR Product Listing

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Histamine Review

Written by I. de Esch & R. Leurs

Histamine Receptors Scientific Review

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New Therapies and Challenges in Asthma

Written by Peter J. Barnes

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Our Asthma poster highlights key pathways and new therapies used to treat asthma, including those currently in clinical development. Request copy today.

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