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 (1)
Gene Data

Histamine H4 Receptor Agonists

Cat. No. Product Name / Activity
0752 Clobenpropit dihydrobromide
H4 partial agonist and H3 antagonist
3545 Histamine dihydrochloride
Endogenous histamine 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

Histamine H4 Receptor Inverse Agonists

Cat. No. Product Name / Activity
0644 Thioperamide
H4 inverse agonist; also H3 antagonist

Histamine H4 Receptor Antagonists

Cat. No. Product Name / Activity
2441 JNJ 10191584 maleate
Selective H4 antagonist; orally active
6279 JNJ 39758979 dihydrochloride
High affinity and selective histamine H4 antagonist; orally bioavailable
4021 JNJ 7777120
Selective H4 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

Tocris offers the following scientific literature for Histamine H4 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

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.

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