Histamine H₄ Receptors in the Gastrointestinal Tract

Overview

Journal Br J Pharmacol

Publisher Wiley

Specialty Pharmacology

Date 2014 Nov 4

PMID 25363289

Citations 31

Authors

A Deiteren

J G DE Man

P A Pelckmans

B Y DE Winter

Affiliations

Soon will be listed here.

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 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 knowledge of H₄ receptor involvement in gastrointestinal processes both under physiological conditions and in models of disease. Strong evidence points towards a role for H₄ 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 H₄ receptors in gastrointestinal cancerogenesis, sensory signalling, and visceral pain as well as in gastric ulceration. These studies highlight the potential of H₄ receptor targeted therapy in the treatment of various gastrointestinal disorders such as inflammatory bowel disease, irritable bowel syndrome and cancer.

Citing Articles

Chronic Visceral Pain: New Peripheral Mechanistic Insights and Resulting Treatments.

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Histamine H4 Receptor Agonist, 4-Methylhistamine, Aggravates Disease Progression and Promotes Pro-Inflammatory Signaling in B Cells in an Experimental Autoimmune Encephalomyelitis Mouse Model.

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Digestibility and Palatability of the Diet and Intestinal Functionality of Dogs Fed a Blend of Yeast Cell Wall and Oregano Essential Oil.

Soares N, Bastos T, Kaelle G, de Souza R, de Oliveira S, Felix A Animals (Basel). 2023; 13(15).

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Inflammatory Bowel Disease: Crosstalk between Histamine, Immunity, and Disease.

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References

Alexander S, Benson H, Faccenda E, Pawson A, Sharman J, Spedding M . The Concise Guide to PHARMACOLOGY 2013/14: enzymes. Br J Pharmacol. 2014; 170(8):1797-867. PMC: 3892293. DOI: 10.1111/bph.12451. View

Heron A, Rouleau A, Cochois V, Pillot C, Schwartz J, Arrang J . Expression analysis of the histamine H(3) receptor in developing rat tissues. Mech Dev. 2001; 105(1-2):167-73. DOI: 10.1016/s0925-4773(01)00389-6. View

Wood J . Enteric neuroimmunophysiology and pathophysiology. Gastroenterology. 2004; 127(2):635-57. DOI: 10.1053/j.gastro.2004.02.017. View

Andaloussi M, Lim H, van der Meer T, Sijm M, Poulie C, de Esch I . A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787. Bioorg Med Chem Lett. 2013; 23(9):2663-70. DOI: 10.1016/j.bmcl.2013.02.091. View

Leurs R, Chazot P, Shenton F, Lim H, de Esch I . Molecular and biochemical pharmacology of the histamine H4 receptor. Br J Pharmacol. 2009; 157(1):14-23. PMC: 2697796. DOI: 10.1111/j.1476-5381.2009.00250.x. View

Zimmermann A, Burhenne H, Kaever V, Seifert R, Neumann D . Systematic analysis of histamine and N-methylhistamine concentrations in organs from two common laboratory mouse strains: C57Bl/6 and Balb/c. Inflamm Res. 2011; 60(12):1153-9. DOI: 10.1007/s00011-011-0379-5. View

Brunsden A, Grundy D . Sensitization of visceral afferents to bradykinin in rat jejunum in vitro. J Physiol. 1999; 521 Pt 2:517-27. PMC: 2269676. DOI: 10.1111/j.1469-7793.1999.00517.x. View

Kim B, Kwon Y, Kim E, So I . Effects of histamine on cultured interstitial cells of cajal in murine small intestine. Korean J Physiol Pharmacol. 2013; 17(2):149-56. PMC: 3634092. DOI: 10.4196/kjpp.2013.17.2.149. View

Deiteren A, De Man J, Ruyssers N, Moreels T, Pelckmans P, De Winter B . Histamine H4 and H1 receptors contribute to postinflammatory visceral hypersensitivity. Gut. 2014; 63(12):1873-82. DOI: 10.1136/gutjnl-2013-305870. View

10.

Coge F, Guenin S, Rique H, Boutin J, Galizzi J . Structure and expression of the human histamine H4-receptor gene. Biochem Biophys Res Commun. 2001; 284(2):301-9. DOI: 10.1006/bbrc.2001.4976. View

11.

Fukushima Y, Ohmachi Y, Asano T, Nawano M, Funaki M, Anai M . Localization of the histamine H(2) receptor, a target for antiulcer drugs, in gastric parietal cells. Digestion. 1999; 60(6):522-7. DOI: 10.1159/000007701. View

12.

Oda T, Matsumoto S, Matsumoto M, Takasaki J, Kamohara M, Soga T . Molecular cloning of monkey histamine H4 receptor. J Pharmacol Sci. 2005; 98(3):319-22. DOI: 10.1254/jphs.sc0050033. View

13.

Oda T, Morikawa N, Saito Y, Masuho Y, Matsumoto S . Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes. J Biol Chem. 2000; 275(47):36781-6. DOI: 10.1074/jbc.M006480200. View

14.

Coruzzi G, Adami M, Guaita E, de Esch I, Leurs R . Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation. Eur J Pharmacol. 2007; 563(1-3):240-4. DOI: 10.1016/j.ejphar.2007.02.026. View

15.

Sokol H, Georgin-Lavialle S, Grandpeix-Guyodo C, Canioni D, Barete S, Dubreuil P . Gastrointestinal involvement and manifestations in systemic mastocytosis. Inflamm Bowel Dis. 2010; 16(7):1247-53. DOI: 10.1002/ibd.21218. View

16.

Pozzoli C, Adami M, Smits R, Coruzzi G . Effect of histamine H4 receptor ligands on cholinergic neurotransmission of the rat duodenum. Inflamm Res. 2009; 58 Suppl 1:59-60. DOI: 10.1007/s00011-009-2012-4. View

17.

van Diest S, Stanisor O, Boeckxstaens G, de Jonge W, van den Wijngaard R . Relevance of mast cell-nerve interactions in intestinal nociception. Biochim Biophys Acta. 2011; 1822(1):74-84. DOI: 10.1016/j.bbadis.2011.03.019. View

18.

Adachi N, Liu K, Motoki A, Nishibori M, Arai T . Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats. Eur J Pharmacol. 2006; 544(1-3):181-7. DOI: 10.1016/j.ejphar.2006.06.053. View

19.

Snyder S, Epps L . Regulation of histidine decarboxylase in rat stomach by gastrin: the effect of inhibitors of protein synthesis. Mol Pharmacol. 1968; 4(2):187-95. View

20.

Buhner S, Li Q, Vignali S, Barbara G, De Giorgio R, Stanghellini V . Activation of human enteric neurons by supernatants of colonic biopsy specimens from patients with irritable bowel syndrome. Gastroenterology. 2009; 137(4):1425-34. DOI: 10.1053/j.gastro.2009.07.005. View