Histamine H4 Receptors

Histamine H4 receptors are Gαi/o-protein-coupled receptors, first cloned in 2000. H4 receptors are expressed at high levels in the gastrointestinal tract, spleen, thymus, medullary cells, bone marrow and peripheral hematopoietic cells, including eosinophils and T lymphocytes.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
0752 Clobenpropit dihydrobromide
H4 partial agonist and H3 antagonist
3545 Histamine dihydrochloride
Endogenous histamine receptor agonist
0729 Imetit dihydrobromide
Standard H3 and H4 agonist
0932 Immepip dihydrobromide
H4 and H3 agonist
2342 4-Methylhistamine dihydrochloride
Selective, high affinity H4 agonist
4769 VUF 10460
Selective H4 agonist
2494 VUF 8430 dihydrobromide
Potent, high affinity H4 agonist

Antagonists

Cat No Product Name / Activity
3753 A 943931 dihydrochloride
Potent and selective H4 antagonist
3640 A 987306
Potent and selective H4 receptor antagonist
2441 JNJ 10191584 maleate
Selective H4 receptor antagonist; orally active
4021 JNJ 7777120
Selective H4 receptor antagonist
0644 Thioperamide
H4 inverse agonist and H3 antagonist

Histamine H4 receptors are Gαi/o-protein-coupled receptors that were initially cloned in 2000. H4 receptors are expressed at high levels in the gastrointestinal tract, spleen, thymus, medullary cells, bone marrow and peripheral hematopoietic cells, including eosinophils, basophils, mast cells, T lymphocytes, leukocytes and dendritic cells. Moderate expression levels are detected in the brain, heart, liver and lung.

H4 receptors have an important role in inflammation, hematopoiesis and immunity and their expression is regulated by stimuli such as IFN, TNF-α and IL-6. Activation of this receptor mediates chemotaxis of mast cells and eosinophils and also controls cytokine release from dendritic and T cells. Furthermore, H4 receptors have a role in the differentiation of myeloblasts and promyelocytes.

The human gene encoding the H4 receptor is localized to chromosome 18q11.2

External sources of pharmacological information for Histamine H4 Receptors :

Literature for Histamine H4 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 H4 Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human HRH4 NM_021624 Q9H3N8
Mouse Hrh4 NM_153087 Q91ZY2
Rat Hrh4 NM_131909 Q91ZY1