Histamine H₁ Receptors

Histamine H₁ receptors are G_αq/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.

External sources of pharmacological information for Histamine H₁ Receptors :

• IUPHAR Receptor Code

• BJP Guide

Literature for Histamine H₁ Receptors

Tocris offers the following scientific literature for Histamine H₁ 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.

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Histamine H₁ Receptor Gene Data