Cellular analysis of the histamine H4 receptor in human myeloid cells

Biochemical Pharmacology
Ricardo CapeloAstrid S Kahnt

Abstract

The human histamine H4 receptor (H4R) is a Gαi/o-coupled receptor which is mainly expressed on hematopoietic cells. Accordingly, the receptor is implicated in the pathology of various diseases such as autoimmune disorders, bronchial asthma and pruritus. Due to complicated receptor pharmacology, the lack of a reliable antibody and limited availability of primary cells expressing the receptor the physiology of this receptor is still poorly understood. Therefore, we aimed to assess absolute receptor mRNA expression and functionality (intracellular Ca(2+) release) in various human myeloid cell types such as granulocytes, monocytes, macrophages and dendritic cells (DCs). This was put into context with the expression of the H1R and H2R. In addition, the influence of various inflammatory stimuli on H4R expression was investigated in macrophages and monocyte-derived DCs. We found that classically activated macrophages treated with pro-inflammatory stimuli down-regulated histamine receptor mRNA expression as did LPS and zymosan A matured monocyte-derived DCs. In contrast, alternatively activated macrophages (IL-4 or IL-13) upregulated H2R and H4R expression compared to controls. Consistent with existing literature, we found eosinophils ...Continue Reading

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Citations

Jan 9, 2018·Oncoimmunology·Gilda VarricchiGiovanna Schiavoni
Mar 31, 2018·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·Susanne MommertThomas Werfel
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May 19, 2020·Journal of Medicinal Chemistry·Edith BartoleGünther Bernhardt
Oct 6, 2021·Pharmacology Research & Perspectives·María de la Paz SarasolaVanina A Medina

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