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.
Histamine H4 Receptor Agonists |
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|---|---|
| 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 |
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| Cat. No. | Product Name / Activity |
| 0644 | Thioperamide |
| H4 inverse agonist; also H3 antagonist | |
Histamine H4 Receptor Antagonists |
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| 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
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.
Our Histamine review gives an overview of the different histamine receptor subtypes, as well as highlighting pharmacological ligands for their study.
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