The therapeutic potential of histamine receptor ligands in inflammatory bowel disease

Biochem Pharmacol. 2014 Sep 1;91(1):12-7. doi: 10.1016/j.bcp.2014.06.004. Epub 2014 Jun 11.

Abstract

In the intestine of patients suffering from inflammatory bowel disease concentrations of histamine are increased compared to healthy controls. Genetic ablation of histamine production in mice ameliorates the course of experimentally induced colitis. These observations and first pharmacological studies indicate a function of histamine in the pathogenesis of inflammatory bowel disease. However, a closer examination reveals that available data are highly heterogeneous, limiting the rational design of strategies addressing specific histamine receptor subtypes as possible target for pharmacological interaction. However, very recently first clinical data indicate that antagonism at the histamine receptor subtype H4 provides a beneficial effect in at least the skin. Here, we discuss the available data on histamine effects and histamine receptor subtype functions in inflammatory bowel disease with a special emphasis on the histamine H4-receptor.

Keywords: Animal model; Histamine; Inflammatory bowel disease; Mouse.

MeSH terms

  • Animals
  • Colitis / metabolism
  • Colitis / pathology
  • Disease Models, Animal
  • Histamine / metabolism*
  • Humans
  • Immune System / metabolism
  • Inflammatory Bowel Diseases / drug therapy*
  • Inflammatory Bowel Diseases / metabolism
  • Inflammatory Bowel Diseases / physiopathology*
  • Ligands
  • Mast Cells / drug effects
  • Mice
  • Rats
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Histamine / metabolism
  • Receptors, Histamine / physiology*
  • Receptors, Histamine H4

Substances

  • HRH4 protein, human
  • Ligands
  • Receptors, G-Protein-Coupled
  • Receptors, Histamine
  • Receptors, Histamine H4
  • Histamine