Differential effects of functionally different histamine H4 receptor ligands on acute irritant dermatitis in mice

Naunyn-Schmiedeberg's Archives of Pharmacology
Maristella AdamiHolger Stark

Abstract

The anti-inflammatory effects of histamine H4 receptor (H4R) antagonists opened new therapeutic options for the treatment of inflammatory/allergic diseases, but the role of H4R in inflammation is far from being solved. Aim of the present study was to investigate the role of structurally related H4R ligands of the aminopyrimidine class with different efficacies and functionalities (neutral antagonist ST-994, partial agonist ST-1006, inverse agonist ST-1012, and partial inverse agonist ST-1124) on croton oil-induced ear edema and pruritus in mice. The H4R ligands were administered subcutaneously before topical application of croton oil. While ST-1006 and ST-1124 were ineffective at any dose tested (10-100 mg/kg), both ST-994 and ST-1012 (30 and 100 mg/kg) significantly reduced croton oil-induced ear edema. Moreover, ST-994, ST-1006, and ST-1124, but not ST-1012, significantly inhibited croton oil-induced ear pruritus at 30 mg/kg. In accordance with results obtained with the reference H4R antagonist JNJ7777120 (100 mg/kg), histological examination of inflamed ear tissue indicated that treatment with ST-994 (30 mg/kg) led to a significant reduction in the inflammatory severity score and in the number of eosinophils infiltrating the...Continue Reading

References

Jan 1, 1987·International Archives of Allergy and Applied Immunology·S J GalliY A Mekori
Jan 1, 1986·Agents and Actions·A TubaroR Della Loggia
Aug 1, 1994·Agents and Actions·G Blazsó, M Gábor
Apr 24, 2001·Skin Pharmacology and Applied Skin Physiology·N InagakiH Nagai
Feb 14, 2003·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Cuiping ChenJae S Lee
Sep 10, 2003·Proceedings of the National Academy of Sciences of the United States of America·Florence GbahouJean-Michel Arrang
Oct 8, 2003·British Journal of Pharmacology·Karen F BucklandDolores M Conroy
Jan 15, 2004·The Journal of Pharmacology and Experimental Therapeutics·Robin L ThurmondLars Karlsson
May 8, 2004·British Journal of Pharmacology·Ping LingWai-Ping Fung-Leung
Dec 21, 2006·Pharmaceutical Research·Tanja ObradovicIsmael J Hidalgo
Jan 9, 2007·The Journal of Allergy and Clinical Immunology·Paul J DunfordRobin L Thurmond
May 17, 2008·Nature Reviews. Immunology·Stephen J GalliMindy Tsai
Jul 24, 2008·Experimental Dermatology·Kristine RossbachWolfgang Bäumer
Oct 22, 2008·Nature Immunology·Janet Kalesnikoff, Stephen J Galli
Nov 13, 2009·The Journal of Investigative Dermatology·Jeffery M CowdenRobin L Thurmond
Jun 16, 2010·Archives of Dermatological Research·Yasutomo FujiiShoji Takakura
Jul 24, 2010·British Journal of Pharmacology·J C McGrathC L Wainwright
Jul 24, 2010·British Journal of Pharmacology·Carol KilkennyUNKNOWN NC3Rs Reporting Guidelines Working Group
Nov 26, 2010·Current Allergy and Asthma Reports·Susanne MommertThomas Werfel
Dec 8, 2010·Molecular Pharmacology·Elizabeth M Rosethorne, Steven J Charlton
Jan 18, 2011·European Journal of Pharmacology·Tim KottkeHolger Stark
Mar 2, 2011·Naunyn-Schmiedeberg's Archives of Pharmacology·David SchnellRoland Seifert
May 4, 2013·British Journal of Pharmacology·M GschwandtnerR Gutzmer
Nov 26, 2014·Naunyn-Schmiedeberg's Archives of Pharmacology·Erich H SchneiderRoland Seifert
Apr 16, 2015·Frontiers in Pharmacology·Robin L Thurmond
Nov 20, 2015·Neuropharmacology·Bassem Sadek, Holger Stark
Aug 1, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Laura LucariniEmanuela Masini
Feb 25, 2017·Handbook of Experimental Pharmacology·Robin L ThurmondJames P Edwards

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BETA
light microscopy

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NIS
GraphPad
Prism GraphPad
ARRIVE
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