IMR Press / FBL / Volume 17 / Issue 6 / DOI: 10.2741/4039

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Article
Molecular pharmacology of histamine H4 receptors
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1 VU University Amsterdam, Leiden-Amsterdam Center for Drug Research, Amsterdam, The Netherlands

Academic Editor: Ekaterini Tiligada

Front. Biosci. (Landmark Ed) 2012, 17(6), 2089–2106;
Published: 1 June 2012
(This article belongs to the Special Issue Histamine revisited: the H4 receptor in health and disease)

The histamine H4 receptor (H4R) is the youngest member of the histamine receptor family. Based on its predominant expression pattern in hematopoietic cells, the H4R is considered to be an interesting drug target for inflammatory disorders such as allergy and asthma. Since the identification and cloning of the H4R in 2000, drug discovery programs boosted the development of various H4R (specific) ligands. Differences between H4R orthologs in combination with available three-dimensional G protein-coupled receptor (GPCR) models have guided site-directed mutagenesis studies to gain insight in ligand binding and receptor activation. In addition, ongoing characterization of H4R-mediated signaling in transfected and native cells contributes to further unravel the (patho-) physiological functions of H4Rs.

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