Role of histamine H4 receptors in the gastrointestinal tract

Frontiers in Bioscience - Scholar

Volumn 4 S, Issue 1, 2012, Pages 226-239

  Coruzzi, Gabriella ^a   Adami, Maristella ^a   Pozzoli, Cristina ^a  

^a UNIVERSITY OF PARMA   (Italy)

Author keywords

Gastrointestinal tract; Histamine; Histamine H4 receptors

Indexed keywords

1 (5 CHLORO 2 INDOLYLCARBONYL) 4 METHYLPIPERAZINE; CLOBENPROPIT; HISTAMINE; HISTAMINE AGONIST; HISTAMINE H4 RECEPTOR; HISTIDINE DECARBOXYLASE; IMETIT; IMMEPIP; INDOMETACIN; THIOPERAMIDE; UNCLASSIFIED DRUG; ZOLANTIDINE; HISTAMINE RECEPTOR;

ARTICLE; COLON CARCINOGENESIS; COLORECTAL CANCER; DRUG BINDING; DRUG SELECTIVITY; GASTROINTESTINAL TRACT; GENE LOCATION; GENE TARGETING; HUMAN; HUMORAL IMMUNITY; INTESTINAL SECRETION; INTESTINE MOTILITY; MOLECULAR CLONING; NONHUMAN; PERITONITIS; PROTEIN EXPRESSION; ANIMAL; DRUG EFFECT; GASTROINTESTINAL DISEASE; GASTROINTESTINAL MOTILITY; METABOLISM; MOLECULARLY TARGETED THERAPY; PHYSIOLOGY; REVIEW;

ANIMALS; GASTROINTESTINAL DISEASES; GASTROINTESTINAL MOTILITY; GASTROINTESTINAL TRACT; HUMANS; MOLECULAR TARGETED THERAPY; RECEPTORS, HISTAMINE;

EID: 84863776939     PISSN: 19450516     EISSN: 19450524     Source Type: Journal    
DOI: 10.2741/s264     Document Type: Article

References (138)

1. H.H. Dale and P.P. Laidlaw: The physiological action of beta-imidazolyl-ethylamine. J Physiol 41, 318-344 (1910)
2. D. Bovet and A.M. Staub: Action protectrice des ethers phenoliques au cours de l'intoxication histaminique. CR Soc Biol (Paris) 124, 547-549 (1937)
3. J.W. Black, W.A.M. Duncan, G.J. Durant, C.R. Ganellin and M.E. Parsons: Definition and antagonism of histamine H2-receptors. Nature 236 385-390 (1972)
4. M. Feldman and M.E. Burton: Histamine2-receptor antagonists. Standard therapy for acid-peptic disease. First part. N Engl J Med 323, 1672-1680 (1990)
5. M. Feldman and M.E. Burton: Histamine2-receptor antagonists. Standard therapy for acid-peptic disease. Second part. N Engl J Med 323, 1749-1755 (1990)
6. J.M. Arrang, M. Garbarg and J.C. Schwartz: Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptors. Nature 302, 832-837 (1983)
7. T. Nakamura, H. Itadani, Y. Hidaka, M. Ohta and K. Tanaka: Molecular cloning and characterization of a new human histamine receptor, HH4R. Biochem Biophys Res Commun 279, 615-620 (2000)
8. T. Oda, N. Morikawa, Y. Saito, Y. Masuho and S. Matsumoto: Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes. J Biol Chem 275, 36781-36786 (2000)
9. C. Liu, X. Ma, X. Jiang, S.J. Wilson, C.L. Hofstra, J. Blevitt, J. Pyati, X. Li, W. Chai, N. Carruthers and T.W. Lovenberg: Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol Pharmacol 59, 420-426 (2001)
10. K.L. Morse, J. Behan, T.M. Laz, R.E. West Jr, S.A. Greenfeder, J.C. Anthes, S. Umland, Y. Wan, R.W. Hipkin, W. Gonsiorek, N. Shin, E.L. Gustafson, X. Qiao, S. Wang, J.A. Hedrick, J. Greene, M. Bayne and F.J. Monsma Jr: Cloning and characterization of a novel human histamine receptor. J Pharmacol Exp Ther 296, 1058-1066 (2001)
11. T. Nguyen, D.A. Shapiro, S.R. George, V. Setola, D.K. Lee, R. Cheng, L. Rauser, S.P. Lee, K.R. Lynch, B.L. Roth and B.F. O'Dowd: Discovery of a novel member of the histamine receptor family. Mol Pharmacol 59, 427-433 (2001)
12. Y. Zhu, D. Michalovich, H. Wu, K.B. Tan, G.M. Dytko, I.J. Mannan, R. Boyce, J. Alston, L.A. Tierney, X. Li, N.C. Herrity, L. Vawter, H.M. Sarau, R.S. Ames, C.M. Davenport, J.P. Hieble, S. Wilson, D.J. Bergsma and L.R. Fitzgerald: Cloning, expression and pharmacological characterization of a novel human histamine receptor. Mol Pharmacol 59, 434-441 (2001)
13. S. Celanire, M. Wijtmans, P. Talaga, R. Leurs and I.J. de Esch: Keynote review: histamine H3 receptor antagonists reach out for the clinic. Drug Discov Today 10, 1613-1627 (2005)
14. D. Vohora: The third Histamine Receptor: Selective Ligands as Potential Therapeutic Agents in CNS Disorders. CRC Press (Taylor and Francis Group), Boca Raton, FL (2008)
15. M.B. Passani, P. Blandina and F. Torrealba: H3 Rreceptor Miniseries: the histamine H3 receptor and eating behaviour. J Pharmacol Exp Ther (2010) DOI: 10.1124/jpet.110.171306
16. I.J. de Esch, R.L. Thurmond, A. Jongejan and R. Leurs: The histamine H4 receptor as a new therapeutic target for inflammation. Trends Pharmacol Sci 26, 462-469 (2005)
17. M. Zhang, R.L. Thurmond and P.J. Dunford: The histamine H4 receptor: a novel modulator of inflammatory and immune disorders. Pharmacol Ther 113, 594-606 (2007)
18. R.L. Thurmond, E.W. Gelfand and P.J. Dunford: The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov 7, 41-53 (2008)
19. R. Leurs, P.L. Chazot, F.C. Shenton, H.D. Lim and I.J.P. de Esch: Molecular and biochemical pharmacology of the histamine H4 receptor. Br J Pharmacol 157, 14-23 (2009)
20. R.A. Smits, R. Leurs and I.J. de Esch: Major advances in the development of histamine H4 receptor ligands. Drug Discov Today 14, 745-753 (2009)
21. E. Zampeli and E. Tiligada: The role of histamine H4 receptor in immune and inflammatory disorders. Br J Pharmacol 157, 24-33 (2009)
22. R. Hakanson, C. Wahlestedt, L. Westlin, S. Vallgren and F. Sundler: Neuronal histamine in the gut wall releasable by gastrin and cholecystokin. Neurosci Lett 42, 305-310 (1983)
23. R. Hakanson, D. Chen, K. Andersson, H.J. Monstein, C.M. Zhao, B. Ryberg, F. Sundler and H. Mattsson: The biology and physiology of the ECL cell. Yale J Biol Med 67, 123-134 (1994)
24. B. Hunyady, A. Zolyomi, B.J. Hoffman and E. Mezey: Gastrin-producing endocrine cells: a novel source of histamine in the rat stomach. Endocrinology 139, 4404- 4415 (1998)
25. E. Ekblad, C. Wahlestedt, R. Hakanson, F. Sundler, T. Watanabe and H. Wada: Is histamine a neurotransmitter in the gut? Evidence from histidine decarboxylase immunocytochemistry. Acta Physiol Scand 123, 225-227 (1985)
26. P. Panula, M. Kaartinen, M. Macklin and E. Costa: Histamine-containing peripheral neuronal and endocrine systems. J Histochem Cytochem 33, 933-941 (1985)
27. M. Shiraishi, N. Hirasawa, S. Oikawa, Y. Kobayashi and K. Ohuchi: Analysis of histamine-producing cells at the late phase of allergic inflammation in rats. Immunology 99, 600-606 (2000)
28. D. MacGlashan Jr: Histamine: A mediator of inflammation. J Allergy Clin Immunol 112 Suppl 4, S53- S59 (2003)
29. M. Dy and E. Schneider: Histamine-cytokine connection in immunity and hematopoiesis. Cytokine Growth Factor Rev 15, 393-410 (2004)
30. M. Jutel, M. Akdis and C.A. Akdis: Histamine, histamine receptors and their role in immune pathology. Clin Exp Allergy 39, 1786-1800 (2009)
31. V.A. Medina and E.S. Rivera: Histamine receptors and cancer pharmacology. Br J Pharmacol 161, 755-767 (2010)
32. J.D. Wood: Histamine, mast cells, and the enteric nervous system in the irritable bowel syndrome, enteritis, and food allergies. Gut 55, 445-447 (2006)
33. C. Prinz, M. Kajimura, D.R. Scott, F. Mercier, H.F. Helander and G. Sachs: Histamine secretion from rat enterochromaffinlike cells. Gastroenterology 105, 449-461 (1993)
34. E. Lindstrom, D. Chen, P. Norlen, K. Andersson and R. Hakanson: Control of gastric acid secretion: the gastrin- ECL cell-parietal cell axis. Comp Biochem Physiol A Mol Integr Physiol 128, 505-514 (2001)
35. M. Raithel, M. Matek, H.W. Baenkler, W. Jorde and E.G. Hahn: Mucosal histamine content and histamine secretion in Crohn's disease, ulcerative colitis and allergic enteropathy. Int Arch Allergy Immunol 108, 127-133 (1995)
36. J.L. Reynolds, J. Akhter, W.J. Adams and D.L. Morris: Histamine content in colorectal cancer. Are there sufficient levels of histamine to affect lymphocyte function? Eur J Surg Oncol 23, 224-227 (1997)
37. G. Barbara, V. Stanghellini, R. De Giorgio, C. Cremon, G.S. Cottrell, D. Santini, G. Pasquinelli, A.M. Morselli-Labate, E.F. Grady, N.W. Bunnett, S.M. Collins and R. Corinaldesi: Activated mast cells in proximity to colonic nerves correlate with abdominal pain in irritable bowel syndrome. Gastroenterology 126, 693-702 (2004)
38. E. Masini, V. Fabbroni, L. Giannini, L. Vannacci, L. Messerini, F. Perna, C. Cortesini and F. Cianchi: Histamine and histidine decarboxylase up-regulation in colorectal cancer: correlation with tumor stage. Inflamm Res 54 Suppl 1, S80- S81 (2005)
39. G. Bertaccini and G. Coruzzi: Histamine receptors in the digestive system. In: The Histamine receptor. Eds. Schwartz JC and Haas HL, Wiley-Liss, NY, 193-230 (1992)
40. M.L. Schubert: Gastric secretion. Curr Opin Gastroenterol 16, 463-468 (2000)
41. M. Jutel, T. Watanabe, M. Akdis, K. Blaser and C.A. Akdis: Immune regulation by histamine. Curr Opinion Immunol 14, 735-740 (2002)
42. G.J. Molderings: Mast cell function in physiology and pathophysiology. BIOTREND Rev 5, 1-9 (2010)
43. M. Kidd, L.H. Tang, K. Miu, G.P. Lawton, A. Sandor and I.M. Modlin: Autoregulation of enterochromaffin-like cell histamine secretion via the histamine 3 receptor subtype. Yale J Biol Med 69, 9-19 (1996)
44. G. Coruzzi, E. Poli, G. Morini and G. Bertaccini: The histamine H3 receptor. In: Molecular Targets for Drug Development: GI Diseases. Eds.: Gaginella TS, Guglietta A, Humana Press, Totowa, NY, 239-267 (2000)
45. M.E. Parsons and C.R. Ganellin: Histamine and its receptors. Br J Pharmacol 147 Suppl 1, S127-S135 (2006)
46. G. Coruzzi and M. Adami: Peripheral actions and therapeutic potential in periphery. In: The third Histamine Receptor: Selective Ligands as Potential Therapeutic Agents in CNS Disorders. Ed.: Vohora D, CRC Press, Taylor and Francis Group, NY, 167-209 (2008)
47. F. Coge, S.P. Guenin, H. Rique, J.A. Boutin and J.P. Galizzi: Structure and expression of the human histamine H4-receptor gene. Biochem Biophys Res Commun 284, 301- 309 (2001)
48. T. Oda, S. Matsumoto, Y. Masuho, J. Takasaki, M. Matsumoto, M. Kamohara, T. Saito, T. Ohishi, T. Soga, H. Hiyama, H. Matsushime and K. Furuichi: cDNA cloning and characterization of porcine histamine H4 receptor. Biochem Biophys Acta 1575, 135-138 (2002)
49. F. Cianchi, C. Cortesini, N. Schiavone, F. Perna, L. Magnelli, E. Fanti, D. Bani, L. Messerini, V. Fabbroni, G. Perigli, S. Capaccioli and E. Masini: The role of cyclooxygenase-2 in mediating the effects of histamine on cell proliferation and vascular endothelial growth factor production in colorectal cancer. Clin Cancer Res 11, 6807- 6815 (2005)
50. T. Oda, S. Matsumoto, M. Matsumoto, J. Takasaki, M. Kamohara, T. Soga, H. Hiyama, M. Kobori and M. Katoh: Molecular cloning of monkey histamine H4 receptor. J Pharmacol Sci 98, 319-322 (2005)
51. L.E. Sander, A. Lorentz, G. Sellge, M. Coeffier, M. Neipp, T. Veres, T. Frieling, P.N. Meier, M.P. Manns and S.C. Bischoff: Selective expression of histamine receptors H1R, H2R, and H4R, but not H3R, in the human intestinal tract. Gut 55, 498-504 (2006)
52. P.L. Chazot, F.C. Shenton, H. Waldvogel, D. Grandi and G. Morini: The H4 histamine receptor is expressed in both the human CNS and rodent PNS. European Histamine Research Society, 36th Meeting, p.27 (2007)
53. K. Boer, E. Helinger, A. Helinger, P. Pocza, Z. Pos, P. Demeter, Z. Baranyai, K. Dede, Z. Darvas and A. Falus: Decreased expression of histamine H1 and H4 receptors suggests disturbance of local regulation in human colorectal tumours by histamine. Eur J Cell Biol 87, 227- 236 (2008)
54. W. Jiang, H.D. Lim, M. Zhang, P. Desai, H. Dai, P.M. Colling, R. Leurs and R.L. Thurmond: Cloning and pharmacological characterization of the dog histamine H4 receptor. Eur J Pharmacol 592, 26-32 (2008)
55. G. Morini, G. Becchi, F.C. Shenton, P.L. Chazot and D. Grandi: Histamine H3 and H4 receptors are expressed on distinct endocrine cell type in the rat fundic mucosa. Inflamm Res 57 Suppl 1, S57-S58 (2008)
56. T.L. Sutton, A. Zhao, K.B. Madden, J.E. Elfrey, B.A. Tuft, C.A. Sullivan, J.F. Urban Jr and T. Shea-Donohue: Anti-inflammatory mechanisms of enteric Heligmosomoides polygyrus infection against trinitrobenzene sulfonic acid-induced colitis in a murine model. Infect Immun 76, 4772-4782 (2008)
57. S. Yu, E. Stahl, Q. Li and A. Ouyang: Antigen inhalation induces mast cells and eosinophils infiltration in the guinea pig esophageal epithelium involving histaminemediated pathway. Life Sci 82, 324-330 (2008)
58. M.I. Strakhova, C.A. Cuff, A.M. Manelli, T.L. Carr, D.G. Witte, J.L. Baranowski, T.A. Vortherms, T.R. Miller, L. Rundell, M.J. McPherson, R.M. Adair, A.A. Brito, B.M. Bettencourt, B.B. Yao, J.M. Wetter, K.C. Marsh, H. Liu, M.D. Cowart, J.D. Brioni and T.A. Esbenshade: In vitro and in vivo characterization of A-940894: a potent histamine H4 receptor antagonist with anti-inflammatory properties. Br J Pharmacol 157, 44-54 (2009)
59. K. Takagaki, S. Osawa, Y. Horio, T. Yamada, Y. Hamaya, Y. Takayanagi, T. Furuta, A. Hishida and M. Ikuma: Cytokine responses of intraepithelial lymphocytes are regulated by histamine H2 receptor. J Gastroenterol 44, 285-296 (2009)
60. C.O. Elson, R.B. Sartor, G.S. Tennyson and R.H. Riddell: Experimental models of inflammatory bowel disease. Gastroenterology 109, 1344-1367 (1995)
61. A.K. Kumawat, Y.Y. Gotlind, M.F. Fredin, R. Willen, H. Strid and E.H. Hornquist: Expression patterns of histamine receptors in the Gi2alpha-deficient mouse model of colitis. In: European Histamine Research Society, 39th Annual Meeting, p.93 (2010)
62. R. Kiss and G.M. Keseru: Histamine H4 receptor ligands and their potential therapeutic applications. Expert Opin Ther Pat 19, 119-135 (2009)
63. J.A. Jablonowski, C.A. Grice, W. Chai, C.A. Dvorak, J.D. Venable, A.K. Kwok, K.S. Ly, J. Wei, S.M. Baker, P.J. Desai, W. Jiang, S.J. Wilson, R.L. Thurmond, L. Karlsson, J.P. Edwards, T.W. Lovenberg and N.I. Carruthers: The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem 46 3957-3960 (2003)
64. R.L. Thurmond, P.J. Desai, P.J. Dunford, W.P. Fung- Leung, C.L. Hofstra, W. Jiang, S. Nguyen, J.P. Riley, S. Sun, K.N. Williams, J.P. Edwards and L. Karlsson: A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther 309, 404-413 (2004)
65. H. Liu, R.J. Altenbach, T.L. Carr, P. Chandran, G.C. Hsieh, L.G. Lewis, A.M. Manelli, I. Milicic, K.C. Marsh, T.R. Miller, M.I. Strakhova, T.A. Vortherms, B.D. Wakefield, J.M. Wetter, D.G Witte, P. Honore, T.A. Esbenshade, J.D. Brioni and M.D. Cowart: cis-4- (Piperazin-1-yl)-5,6,7a,8,9,10,11,11a- octahydrobenzofuro [2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J Med Chem 51, 7094- 7098 (2008)
66. H. Engelhardt, R.A. Smits, R. Leurs, E. Haaksma and I.J. De Esch: A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic. Curr Opin Drug Discov Devel 12, 628-643 (2009)
67. H.D. Lim, R.M. van Rijn, P. Ling, R. Bakker, R. Thurmond and R. Leurs: Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 314, 1310-1321 (2005)
68. H.D. Lim, R.A. Smits, R.A. Bakker, C.M. van Dam, I.J. de Esch and R. Leurs: Discovery of S-(2-guanidylethyl)- isothiourea (VUF 8430) as a potent nonimidazole H4 receptor agonist. J Med Chem 49, 6650-6651 (2006)
69. T. Kenakin: Pharmacological proteus? Trends Pharmacol Sci 16, 256-258 (1995)
70. N.P. Clarke, C.D. Brown, C. Lane, C. Mowbray, H.D. Lim, R. Leurs, E. Schenck, C. Perros-Huguet and M. Yeadon: PF-2988403- an 'H4 antagonist' demostrating the full range of in vitro pharmacologies which translate in vivo in the rat. In: European Histamine Research Society, 37thAnnual Meeting, Abstract No.07, p.34 (2008)
71. G. Coruzzi, M. Adami, C. Pozzoli, R. Smits, I. de Esch and R. Leurs: Gastroprotective effects of histamine H4 receptor ligands in rodent ulcer models. Proceedings of the British Pharmacological Society at http://www.pa2online.org/abstracts/Vol7Issue4abst150P.pd f
72. D. Neumann, S. Beermann and R. Seifert: Does the histamine H4 receptor have a pro- or anti-inflammatory role in murine bronchial asthma? Pharmacology 85, 217-223 (2010)
73. N. Adachi, K. Liu, A. Motoki, M. Nishibori and T. Arai: Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats. Eur J Pharmacol 544, 181-187 (2006)
74. W.W. Pawlik, R. Obuchowicz, M.W. Pawlik, R. Sendur, J. Biernat, T. Brzozowski, and S.J. Konturek: Histamine H3 receptors modulate reactive hyperemia in rat gut. J Physiol Pharmacol 55, 651-661 (2004)
75. A. Rydning, O. Lying, B.L. Adamsen, S. Falkmer, A.K. Sandvik and J.E. Gronbech: Mast cells are involved in the gastric hyperemic response to acid back diffusion via release of histamine. Am J Physiol Gastrointest Liver Physiol 280, G1061-G1069 (2001)
76. N. Terzioglu, R.M. van Rijn, R.A. Bakker, I.J. de Esch and R. Leurs: Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists. Bioorg Med Chem Lett 14, 5251-5256 (2004)
77. H.D. Lim, M. Adami, E. Guaita, T. Werfel, R.A. Smits, I.J. de Esch, R.A. Bakker, R. Gutzmer, G. Coruzzi and R. Leurs: Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430. Br J Pharmacol 157, 34-43 (2009)
78. G. Morini, D. Grandi and G. Bertaccini: (R)-alphamethylhistamine inhibits ethanol-induced gastric lesions in the rat: involvement of histamine H3 receptors? Digestion 56, 145- 152 (1995)
79. G. Morini, D. Grandi, M. Krause, and W. Schunack: Gastric mucosal injury by nonsteroidal anti-inflammatory drugs is reduced by (R)-aplha-methylhistamine and its prodrugs in the rat. Inflamm Res 46 Suppl 1, S101-102 (1997)
80. G. Morini, D. Grandi, H. Stark and W. Schunack: Histamine H3-receptor antagonists inhibit gastroprotection by (R)-alpha-methylhistamine in the rat. Br J Pharmacol 129, 1597-1600 (2000)
81. Z. Warzecha, A. Dembinski, T. Brzozowski, P. Ceranowicz, R. Pajdo, J. Niemiec, D. Drozdowicz, M. Mitis- Musiol and S.J. Konturek: Gastroprotective effect of histamine and acid secretion on ammonia-induced gastric lesions in rats. Scand J Gastroenterol 35, 916-924 (2000)
82. S. Kwiecien, T. Brzozowski, P.C. Konturek, S.J. Konturek, M. Pawlik, R. Pajdo, D. Drozdowicz, A. Ptak and E.G. Hahn: Effect of central and peripheral actions of histamine and its metabolite N-alpha methylhistamine on gastric acid secretion and acute gastric lesions. J Physiol Pharmacol 52, 625-638 (2001)
83. A. Dembinski, Z. Warzecha, P. Ceranowicz, T. Brzozowski, M. Dembinski, S.J. Konturek and W.W. Pawlik: Role of capsaicin-sensitive nerves and histamine H1, H2, and H3 receptors in the gastroprotective effect of histamine against stress ulcers in rats. Eur J Pharmacol 508, 211-221 (2005)
84. G. Morini, D. Grandi and W. Schunack: Ligands for histamine H3 receptors modulate cell proliferation and migration in rat oxyntic mucosa. Br J Pharmacol 137, 237-244 (2002)
85. D. Grandi, W. Schunack and G. Morini: Epithelial cell proliferation is promoted by the histamine H3 receptor agonist (R)-alpha-methylhistamine throughout the rat gastrointestinal tract. Eur J Pharmacol 538, 141-147 (2006)
86. G. Morini, H. Timmerman, W. Schunack and D. Grandi: Agonists for the histamine H3-receptor differ in their gastroprotective activity in the rat. Inflamm Res 51 Suppl 1, S75-S76 (2002)
87. M. Adami, G. Coruzzi, E. Guaita, I.J.P. de Esch and R. Leurs: Antiinflammatory, analgesic and gastroprotective effects of the novel and selective histamine H4-receptor antagonist VUF5949. In: European Histamine Research Society, 34th Annual Meeting, p.47 (2005)
88. T.L. Peeters: Ghrelin: a new player in the control of gastrointestinal functions. Gut 54, 1638-1649 (2005)
89. M. Adami, C. Pozzoli, R. Leurs, H. Stark and Coruzzi G: Histamine H3 receptors are involved in the protective effect of gherlin on against HCl-induced gastric damage in rats. Pharmacology (2010) DOI: 10.1159/000320110
90. J.D. Wood: Neuropathophysiology of functional gastrointestinal disorders. World J Gastroenterol 13, 1313- 1332 (2007)
91. J.H. Zavecz and T.O. Yellin: Histamine receptors in the myenteric plexus-longitudinal muscle of the guinea pig ileum: H1- and H2-receptor-mediated potentiation of the contractile response to electrical stimulation. J Pharmacol Exp Ther 223, 177-182 (1982)
92. S.J. Keely, W.A. Stack, D.P. O'Donoghue and A.W. Baird: Regulation of ion transport by histamine in the human colon. Eur J Pharmacol 279, 203-209 (1995)
93. W.A. Stack, S.J. Keely, D.P. O'Donoghue and A.W. Baird: Immune regulation of human colon electrolyte transport in vitro. Gut 36, 395-400 (1995)
94. H. Schworer, A. Reimann, G. Ramadori and K. Racke: Characterization of H3 receptors inhibiting 5-HT release from porcine enterochromaffin cells: further evidence for H3 receptor heterogeneity. Naunyn Schmiedebergs Arch Pharmacol 350, 375-379 (1994)
95. C. Pozzoli, M. Adami, R.A. Smits and G. Coruzzi: Effect of histamine H4 receptor ligands on cholinergic neurotransmission of the rat duodenum. Inflamm Res 58 Suppl 1, S59-S60 (2009)
96. T. Frieling, H.J. Cooke and J.D. Wood: Histamine receptors on submucous neurons in the guinea pig colon. Am J Physiol 264, G74-G80 (1993)
97. J.D. Wood: Enteric neuroimmunophysiology and pathophysiology. Gastroenterology 127, 635-657 (2004)
98. E. Breunig, K. Michel, F. Zeller, S. Seidl, C.W. Weyhern and M. Schemann: Histamine excites neurones in the human submucous plexus through activation of H1, H2, H3 and H4 receptors. J Physiol 583, 731-742 (2007)
99. M. Hemedah, R. Loiacono, I.M. Coupar and F.J. Mitchelson: Lack of evidence for histamine H3 receptor function in rat ileum and human colon. Naunyn Schmiedebergs Arch Pharmacol 363, 133-138 (2001)
100. A. Aly, F. Barany, B. Kollberg, U. Monsen, O. Wisen and C. Johansson: Effect of an H2-receptor blocking agent on diarrhoeas after extensive small bowel resection in Crohn's disease. Acta Med Scand 207, 119-122 (1980)
101. J. Santos, C. Alonso, M. Guilarte, M. Vicario and J.R. Malagelada: Targeting mast cells in the treatment of functional gastrointestinal diseases. Curr Opin Pharmacol 6, 541-546 (2006)
102. L. Bueno and J. Fioramonti: Visceral perception: inflammatory and non-inflammatory mediators. Gut 51 Suppl. 1, i19-i23 (2002)
103. M.H. Perdue, M. Chung and D.G. Gall: Effect of intestinal anaphylaxis on gut function in the rat. Gastroenterology 86, 391-397 (1984)
104. G.N. Akoev, L.V. Filippova and N.O. Sherman: Mast cell mediators excite the afferents of cat small intestine. Neuroscience 71, 1163-1166 (1996)
105. L.W. Fu, H.L. Pan and J.C. Longhurst: Endogenous histamine stimulates ischaemically sensitive abdominal visceral afferents through H1 receptors. Am J Physiol 273, H2726-H2737 (1997)
106. M.E. Kreis, W. Haupt, A.J. Kirkup and D. Grundy: Histamine sensitivity of mesenteric afferent nerves in the rat jejunum. Am J Physiol 275, G675-G680 (1998)
107. A.M. Brunsden and D. Grundy: Sensitization of visceral afferents to bradykinin in rat jejunum in vitro. J Physiol 521, 517-527 (1999)
108. M. Nakaya, N. Takeuchi and K. Kondo: Immunohistochemical localization of histamine receptor subtypes in human inferior turbinates. Ann Otol Rhinol Laryngol 113, 552-557 (2004)
109. M.I. Strakhova, A.L. Nikkel, A.M. Manelli, G.C. Hsieh, T.A. Esbenshade, J.D. Brioni and R.S. Bitner: Localization of histamine H4 receptors in the central nervous system of human and rat. Brain Res 1250, 41-48 (2009)
110. W.M. Connelly, F.C. Shenton, N. Lethbridge, R. Leurs, H.J. Waldvogel, R.L. Faull, G. Lees and P.L. Chazot: The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol 157, 55-63 (2009)
111. G. Coruzzi, M. Adami, E. Guaita, I.J. de Esch and R. Leurs: 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 563, 240-244 (2007)
112. M.D. Cowart, R.J. Altenbach, H. Liu, G.C. Hsieh, I. Drizin, I. Milicic, T.R. Miller, D.G. Witte, N. Wishart, S.R. Fix-Stenzel, M.J. McPherson, R.M. Adair, J.M. Wetter, B.M. Bettencourt, K.C. Marsh, J.P. Sullivan, P. Honore, T.A. Esbenshade and J.D. Brioni: Rotationally constrained 2,4-diamino-5,6- disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem 51, 6547-6557 (2008)
113. G.C. Hsieh, P. Chandran, A.K. Salyers, M. Pai, C.Z. Zhu, E.J. Wensink, D.G. Witte, T.R. Miller, J.P. Mikusa, S.J. Baker, J.M. Wetter, K.C. Marsh, A.A Hancock, M.D. Cowart, T.A. Esbenshade, J.D. Brioni and P. Honore: H4 receptor antagonism exhibits antinociceptive effects in inflammatory and neuropathic pain models in rats. Pharmacol Biochem Behav 95, 41- 50 (2010)
114. L. Knutson, O. Ahrenstedt, B. Odlind and R. Hallgren: The jejunal secretion of histamine is increased in active Crohn's disease. Gastroenterology 98, 849-854 (1990)
115. S. Bischoff and S.E. Crowe: Gastrointestinal food allergy: new insights into pathophysiology and clinical perspectives. Gastroenterology 128, 1089-1113 (2005)
116. L. Maintz and N. Novak: Histamine and histamine intolerance. Am J Clin Nutr 85, 1185-1196 (2007)
117. C. Fiocchi: Inflammatory bowel disease: etiology and pathogenesis. Gastroenterology 115, 182-205 (1998)
118. C. Varga, K. Horvath, A. Berko, R.L. Thurmond, P.J. Dunford and B.J. Whittle: Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur J Pharmacol 522, 130-138 (2005)
119. P.J. Dunford, C. Varga, R.L. Thurmond and B.J. Whittle: Histamine H4 receptor antagonism attenuates toll-like receptor signaling and inhibits experimental colitis in the rat. Gastroenterology 130, W1597 (2006)
120. W.A. Fogel, J. Jochem and A. Lewinski: Influence of the H3/H4 receptor antagonist, thioperamide on regional haemodinamics in rats with trinitrobenzene sulfonic acid-induced colitis. Inflamm Res 56 Suppl 1, S21-S22 (2007)
121. K. Takeshita, K. Sakai, K.B. Bacon and F. Gantner: Critical role of histamine H4 receptor in leukotriene B4 production and mast cell-dependent neutrophil recruitment induced by zymosan in vivo. J Pharmacol Exp Ther 307, 1072-1078 (2003)
122. M.N. Ajuebor, A.M. Das, L. Virag, R.J. Flower, C. Szabo and M. Perretti: Role of resident peritoneal macrophages and mast cells in chemokine production and neutrophil migration in acute inflammation: evidence for an inhibitory loop involving endogenous IL-10. J Immunol 162, 1685-1691 (1999)
123. P. Ghizzardi, T. Gobbetti, S. Bertoni, F. Saccani, L. Flammini, V. Ballabeni and E. Barocelli: Histamine H4 receptor antagonism and mesenteric ischemia/reperfusion injury in mice. Gastroenterology 136 Suppl 1, A-397 2009)
124. S. Tsunada, K. Fujimoto, Y. Gotoh, T. Sakai, M. Kang, T. Sakata, D.N. Granger and P. Tso: Role of histamine receptors in intestinal repair after ischemiareperfusion in rats. Gastroenterology 107, 1297-1304 (1994)
125. R. Chandra and A.K. Ganguly: Diamineoxidase activity and tissue histamine content of human skin, breast and rectal carcinoma. Cancer Lett 34, 207-212 (1987)
126. M. Garcia-Caballero, E. Neugebauer, F. Rodriguez, I. Nunez de Castro and C. Vara-Thorbeck: Histamine synthesis and content in benign and malignant breast tumours. Its effect on other host tissues. Surg Oncol 3, 167-173 (1994)
127. A. Falus, H. Hegyesi, E. Lazar-Molnar, Z. Pos, V. Laszlo and Z. Darvas: Paracrine and autocrine interactions in melanoma: histamine is a relevant player in local regulation. Trends Immunol 22, 648-652 (2001)
128. L. Graff, M. Frungieri, R. Zannar, A. Pohlinger, C. Prinz and M. Gratzl: Expression of histidine decarboxylase and synthesis of histamine by human small cell lung carcinoma. Am J Pathol 160, 1561-1565 (2002)
129. V. Medina, M. Croci, E. Crescenti, N. Mohamad, F. Sanchez-Jimenez, N. Massari, M. Nunez, G. Cricco, G. Martin, R. Bergoc and E. Rivera: The role of histamine in human mammary carcinogenesis: H3 and H4 receptors as potential therapeutic targets for breast cancer treatment. Cancer Biol Ther 7, 28-35 (2008)
130. J. Sorbo, A. Jakobsson and K. Norrby: Mast-cell histamine is angiogenic through receptors for histamine1 and histamine2. Int J Exp Pathol 75, 43-50 (1994)
131. A.K. Ghosh, N. Hirasawa and K. Ohuchi: Enhancement by histamine of vascular endothelial growth factor production in granulation tissue via H2 receptor. Br J Pharmacol 134, 1419-1428 (2001)
132. W.J. Adams and D.L. Morris: Short-course cimetidine and survival with colorectal cancer. Lancet 344, 1768-1769 (1994)
133. E. Bolton, J. King and D.L. Morris: H2-antagonists in the treatment of colon and breast cancer. Semin Cancer Biol 10, 3- 10 (2000)
134. H.J. Nielsen, U. Christensen, F. Moesgaard and H. Kehlet: Ranitidine as adjuvant treatment in colorectal cancer. Br J Surg 89, 1416-1422 (2002)
135. G.P. Cricco, N.A. Mohamad, L.A. Sambuco, F. Genre, M. Croci, A.S. Gutierrez, V.A. Medina, R.M. Bergoc, E.S. Rivera and G.A. Martin: Histamine regulates pancreatic carcinoma cell growth through H3 and H4 receptors. Inflamm Res 57 Suppl 1, S23-S24 (2008)
136. A.F. Petit-Bertron, F. Machavoine, M.P. Defresne, M. Gillard, P. Chatelain, P. Mistry, E. Schneider and M. Dy: H4 histamine receptors mediate cell cycle arrest in growth factor-induced murine and human hematopoietic progenitor cells. PLoS ONE, 4, e6504 (2009)
137. B.J. Whittle: Mechanisms underlying intestinal injury induced by anti-inflammatory COX inhibitors. Eur J Pharmacol 500, 427-439 (2004)
138. J.L. Wallace: Prostaglandins, NSAIDs, and gastric mucosal protection: why doesn't the stomach digest itself? Physiol Rev 88, 1547-1565 (2008)