The Histamine H4R receptor is the most recently identified G-protein coupled receptor, with little homology to the classical pro-inflammatory histamine H1 or the histamine H2 receptor, and some 35% homology with H3 receptor.
The high expression of the histamine H4 receptor in cells of hemopoietic lineage and immune cells suggests that this new histamine receptor plays a role in inflammatory and immune responses. Activation of the Histamine receptor can mediate calcium mobilization and chemotaxis in mast cells.
Preliminary studies on the H4R and specific antagonist (JNJ 7777120 - Johnson & Johnson, VUF6002-Janssen Pharma.) suggest another rich vein of histamine receptors therapeutics, likely to generate more blockbusters and medical breakthroughs, could be on the horizon.
Ref: Nature Reviews Drug Discovery, 7, 41-53, 2008, Trends Pharmacol. Sci. 26, 462-469, 2005.
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