The Histamine H4 Receptor: A Novel Target for Safe Anti-inflammatory Drugs?
After the discovery of histamine H2 receptors and their revolutionary role in the therapy of gastroduodenal ulcer,1-3 the research on Gastrointestinal histamine was considered
to be settled.
However, renewed interested in the amine emerged in the ‘90s with the discovery
of the histamine H3 receptor (H3 R), and subsequently, in the early 2000 when the H4
receptor (H4 R) was detected from the human genome database by several independent groups.
As a consequence, novel therapeutic fields have been unravelled for antihistamine drugs: whereas histamine H3 R antagonists may represent new therapeutic options for cognitive, sleep and
memory disorders and for obesity,H4 R antagonists are currently the object of intensive
research, as potential candidates in the therapy of allergy, inflammatory disorders, neurophatic
pain and pruritus.
The present review will focus on the location and functional role of H4
Rs in the GI tract and the potential clinical implications for human diseases.
Beneficial effects of H4 R blockers at GI level would be of particular interest, when considering that the available Nonsteroidal Anti-inflammatory Drugs are still endowed with significant gastric and intestinal toxicity.
This is particularly true for the still unrecognized NSAID-induced enteropathy,
which occurs frequently and still awaits for medical treatment.
The H4 R is a G-protein coupled receptor which has been primarily detected outside the Central Nervous System, and, in particular, in immune and inflammatory cells, including
mast cells, eosinophils, basophils, dendritic cells and T cellsigration.
Gastro Open J. 2014; 1(1): 7-12. doi: 10.17140/GOJ-1-103
