Histamine H1 Receptors

Supporting information

Histamine H1 receptors are Gαq/11-protein-coupled receptors that mediate allergic responses. These receptors are expressed in a wide variety of tissues including the gastrointestinal tract, CNS, airway and vascular smooth muscle cells and endothelial cells.

H1 receptors are also expressed in chondrocytes, monocytes, neutrophils, dendritic cells, T and B lymphocytes, adrenal medulla, and the cardiovascular and genitourinary systems.

H1 receptor activation induces a wide range of biological responses due to their widespread distribution. In smooth muscle, H1 activation increases tension and the contractile response, and in vascular endothelial cells receptor activation increases cell permeability. In the adrenal medulla, histamine acting at H1 receptors stimulates both adrenalin and noradrenalin release. Furthermore, H1 activation induces prostacyclin and platelet-activating factor synthesis, promotes von Willebrand factor and nitric oxide release, liberates arachidonic acid from phospholipids, and causes vasodilation of capillaries and arterioles.

At a physiological level, H1 receptors are involved in a wide array of processes including thermal regulation, memory and learning, and control of the sleep-wake cycle, food intake, and emotional and aggressive behavior.

Histamine acting through the H1 receptor has proinflammatory effects, and is involved in the development of various aspects of the antigen-specific immune response. Activation of these receptors triggers maturation of dendritic cells and modulates the balance of Th1 and Th2 cells. H1 receptors are involved in the pathological process of allergy, including allergic rhinits, atopic dermatitis, anaphylaxis and asthma, and also have a role in autoimmune diseases and malignancy.

The human gene encoding this receptor has been localized to chromosome 3p14-21.

To view external sources of pharmacological information for Histamine H1 Receptors, please click here: IUPHAR Receptor Code and BJP Guide

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Species Gene Symbol Gene Accession No. Protein Accession No.
Human HRH1 NM_001098211 P35367
Mouse Hrh1 NM_008285 P70174
Rat Hrh1 NM_017018 P31390

Literature for Histamine H1 Receptors

GPCR Product Listing

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

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GPCR Product Listing
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This review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them. Compounds available from Tocris are listed.

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Histamine Receptors Scientific Review
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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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