journal article Jan 12, 2015

HistamineH4receptors in the gastrointestinal tract

British Journal of Pharmacology Vol. 172 No. 5 pp. 1165-1178 · Wiley
View at Publisher Save 10.1111/bph.12989
Abstract
Histamine is a well‐established mediator involved in a variety of physiological and pathophysiological mechanisms and exerts its effect through activation of four histamine receptors (H1–H4). The histamineH4receptor is the newest member of this histamine receptor family, and is expressed throughout the gastrointestinal tract as well as in the liver, pancreas and bile ducts. Functional studies using a combination of selective and non‐selectiveH4receptor ligands have rapidly increased our knowledge ofH4receptor involvement in gastrointestinal processes both under physiological conditions and in models of disease. Strong evidence points towards a role forH4receptors in the modulation of immune‐mediated responses in gut inflammation such as in colitis, ischaemia/reperfusion injury, radiation‐induced enteropathy and allergic gut reactions. In addition, data have emerged implicatingH4receptors in gastrointestinal cancerogenesis, sensory signalling, and visceral pain as well as in gastric ulceration. These studies highlight the potential ofH4receptor targeted therapy in the treatment of various gastrointestinal disorders such as inflammatory bowel disease, irritable bowel syndrome and cancer.
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