Abstract
Since identification and cloning of the histamine H4 receptor (H4R) in 2000 by several groups, the development of H4R ligands has been boosted by different drug development programmes. The newest member of the histamine receptor family is considered a promising drug target (as described in this book in different chapters). Highly potent and selective H4R agonists and antagonists have been ...
Abstract
Since identification and cloning of the histamine H4 receptor (H4R) in 2000 by several groups, the development of H4R ligands has been boosted by different drug development programmes. The newest member of the histamine receptor family is considered a promising drug target (as described in this book in different chapters). Highly potent and selective H4R agonists and antagonists have been published by several groups. The effort to improve the pharmacokinetic properties of the currently available H4R ligands is reflected in a steadily growing number of scientific publications and patent applications. Preclinical data strongly confirms the need for novel potent H4R ligands to explore their potential therapeutic value in allergy, inflammation, autoimmune disorders and, possibly, cancer. The main structural classes of H4R ligands are (benz)imidazoles and six-membered nitrogen-containing heterocycles with numerous variations. The objective of this review is to compile currently available H4R ligands and to present noticeable structure-activity and structure-selectivity relationships as well as some selected functional and (pre)clinical data.