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Histamine H? receptors in the gastrointestinal tract.


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-H?). The histamine H? receptor 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-selective H? receptor ligands have rapidly increased our knowledge of H? receptor involvement in gastrointestinal processes both under physiological conditions and in models of disease. Strong evidence points towards a role for H? receptors 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 implicating H? receptors in gastrointestinal cancerogenesis, sensory signalling, and visceral pain as well as in gastric ulceration. These studies highlight the potential of H? receptor targeted therapy in the treatment of various gastrointestinal disorders such as inflammatory bowel disease, irritable bowel syndrome and cancer.

SUBMITTER: Deiteren A 

PROVIDER: S-EPMC4337694 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature

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Histamine H₄ receptors in the gastrointestinal tract.

Deiteren A A   De Man J G JG   Pelckmans P A PA   De Winter B Y BY  

British journal of pharmacology 20150112 5


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 histamine H₄ receptor 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-selective H₄ receptor ligands have rapidly increased our know  ...[more]

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