2005
DOI: 10.1124/jpet.105.087965
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Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist

Abstract: The histamine H 4 receptor (H 4 R) is involved in the chemotaxis of leukocytes and mast cells to sites of inflammation and is suggested to be a potential drug target for asthma and allergy. So far, selective H 4 R agonists have not been identified. In the present study, we therefore evaluated the human H 4 R (hH 4 R) for its interaction with various known histaminergic ligands. Almost all of the tested H 1 R and H 2 R antagonists, including several important therapeutics, displaced less than 30% of specific [3… Show more

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Cited by 270 publications
(413 citation statements)
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“…Moreover, during receptor. [19,37] Moreover, at least some antagonism by thioperamide, JNJ7777120 and MMPCI would have been expected at the H 4 receptor [19,35] even though histamine was used with a much higher concentration than its affinity for the H 4 receptor subtype [19]. In previous studies evaluating the H 4 receptor-mediated effects of histamine on eosinophils, the A c c e p t e d m a n u s c r i p t effects of similar histamine concentrations were antagonized with similar thioperamide and JNJ7777120 concentrations and agonized with similar clobenpropit concentrations as used in the present study.…”
Section: Discussionmentioning
confidence: 99%
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“…Moreover, during receptor. [19,37] Moreover, at least some antagonism by thioperamide, JNJ7777120 and MMPCI would have been expected at the H 4 receptor [19,35] even though histamine was used with a much higher concentration than its affinity for the H 4 receptor subtype [19]. In previous studies evaluating the H 4 receptor-mediated effects of histamine on eosinophils, the A c c e p t e d m a n u s c r i p t effects of similar histamine concentrations were antagonized with similar thioperamide and JNJ7777120 concentrations and agonized with similar clobenpropit concentrations as used in the present study.…”
Section: Discussionmentioning
confidence: 99%
“…[19] However, evidence suggesting the existence of the histamine H 3 receptors on human eosinophils is now known to be incorrect. [1,45,46] Indeed, the novel histamine receptor discovered in eosinophils by Raible and co-workers in the 1990s [45,46] has now been identified as the H 4…”
Section: Discussionmentioning
confidence: 99%
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