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Profiling of histamine H 4 receptor agonists in native human monocytes
Author(s) -
Gschwandtner M,
Koether B,
Werfel T,
Stark H,
Gutzmer R
Publication year - 2013
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12237
Subject(s) - receptor , histamine , agonist , histamine h4 receptor , histamine receptor , histamine h2 receptor , pharmacology , chemistry , monocyte , radioligand assay , histamine h1 receptor , receptor antagonist , antagonist , biochemistry , biology , immunology
Since the identification of the histamine H₄ receptor, several ligands activating this receptor have been described and more compounds are in development. These ligands are well characterized in pharmacological assays, including radioligand competition binding studies, GTPγS and GTPase assays. In most cases, these experiments are performed in transfected cell lines, expressing unnaturally high levels of target receptors and G-protein signalling components. In this study we investigated the specific properties of H₄ receptor ligands in native cells.