Chapter Ten - H4 Receptor Antagonists and Their Potential Therapeutic Applications

• Autores: David D. Burns, Niu Shin, Ravi Jalluri, Wenqing Yao, Peggy Scherle
• Localización: Annual reports in medicinal chemistry, ISSN 0065-7743, Vol 49, 2014, págs. 135-149
• Idioma: inglés
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• Resumen

  • Abstract The histamine H4 receptor shows generally restricted expression in immune cells and has been shown to mediate histamine induced-chemotaxis, suggesting that it may play a role in inflammation. This has led to the discovery and characterization of histamine H4 receptor antagonists from multiple chemical scaffolds. These antagonists have shown efficacy in numerous preclinical models of inflammation, further supporting the critical role of the histamine H4 receptor in inflammatory diseases, including rheumatoid arthritis, asthma, pruritis and inflammatory pain. The first histamine H4 receptor antagonists have entered into clinical trials and data are expected soon to establish the importance of targeting this receptor as a novel therapeutic in inflammation. This review focuses on the histamine H4 receptor antagonists that have been identified to date.