Histamine H1 Receptors

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.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3545 Histamine dihydrochloride
Endogenous histamine receptor agonist
0646 HTMT dimaleate
H1 / H2 agonist
2478 2-Pyridylethylamine dihydrochloride
H1 receptor agonist

Antagonists

Cat No Product Name / Activity
3489 Astemizole
Orally active, potent H1 antagonist. Also KV11.1 (hERG) channel blocker.
2577 Cetirizine dihydrochloride
Selective H1 antagonist
1453 Clemastine fumarate
H1 antagonist
5371 Clemizole hydrochloride
Histamine H1 antagonist; also TRPC5 blocker
5958 Desloratadine
High affinity H1 antagonist; anti-inflammatory.
1425 (S)-(+)-Dimethindene maleate
H1 antagonist. Also M2 muscarinic antagonist
3072 Diphenhydramine hydrochloride
H1 receptor antagonist
0508 Doxepin hydrochloride
Highly potent H1 antagonist. Also binds to H4 receptor
2429 Fexofenadine hydrochloride
H1 receptor antagonist; non-sedating antiallergic agent
0784 Ketotifen fumarate
H1 antagonist
1944 Loratidine
Peripheral H1 antagonist; antiallergic agent
4245 Meclizine dihydrochloride
H1 antagonist; human pregnane X receptor agonist
0660 Mepyramine maleate
Selective H1 inverse agonist
2018 Mirtazapine
Potent H1 antagonist. Also 5-HT2, 5-HT3 and α2-antagonist. Antidepressant
4241 Olopatadine hydrochloride
H1 antagonist; ocular antiallergic agent
3948 Terfenadine
H1 antagonist. Also KV11.1 (hERG) and Kir6 (KATP) channel blocker
0662 trans-Triprolidine hydrochloride
Standard H1 antagonist, highly potent
3996 Zotepine
H1 antagonist. Also 5-HT2A/D2 antagonist. Atypical antipsychotic

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.

External sources of pharmacological information for Histamine H1 Receptors :

Literature for Histamine H1 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 H1 Receptor Gene Data

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