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Gene Review

HRH2  -  histamine receptor H2

Homo sapiens

Synonyms: Gastric receptor I, H2R, HH2R, Histamine H2 receptor
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Disease relevance of HRH2


Psychiatry related information on HRH2


High impact information on HRH2


Chemical compound and disease context of HRH2


Biological context of HRH2


Anatomical context of HRH2


Associations of HRH2 with chemical compounds

  • Denatured AT-III did not bind HRH2, indicating that its heparin recognition site may depend on conformation [24].
  • Stimulation of dendritic cells with histamine resulted in F-actin polymerization and cyclic adenosine monophosphate production through H2R [25].
  • H2r desensitization was not affected by protein kinases A and C (PKA and PKC) inhibitors but was remarkably reduced by Zn(2+), an inhibitor of G protein-coupled receptor kinases (GRKs) [19].
  • Histamine-induced increase of cAMP was inhibited by the H2 receptor antagonist famotidine, whereas induction of IP3 was not observed, making signaling via the H1 receptor unlikely [26].
  • The binding affinity of [3H]tiotidine was not significantly different between H2R-GFP- and wild-type H2R-expressing HEK-293 cells, both of which had constitutive activity of adenylate cyclase [22].

Physical interactions of HRH2


Regulatory relationships of HRH2


Other interactions of HRH2


Analytical, diagnostic and therapeutic context of HRH2


  1. The role of histamine in allergic diseases. White, M.V. J. Allergy Clin. Immunol. (1990) [Pubmed]
  2. Histamine elevates the expression of Ets-1, a protooncogen in human melanoma cell lines through H2 receptor. Hegyesi, H., Horváth, B., Pállinger, E., Pós, Z., Molnár, V., Falus, A. FEBS Lett. (2005) [Pubmed]
  3. Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression. Murakami, H., Sun-Wada, G.H., Matsumoto, M., Nishi, T., Wada, Y., Futai, M. FEBS Lett. (1999) [Pubmed]
  4. Immune responses and immunoregulation in relation to human schistosomiasis in Egypt. II. Cimetidine reversal of histamine-mediated suppression of antigen-induced blastogenesis. Barsoum, I.S., Dahawi, H.S., Gamil, F.M., Habib, M., El Alamy, M.A., Colley, D.G. J. Immunol. (1984) [Pubmed]
  5. Comparative effects of H2-receptor antagonists on subjective and objective assessments of sleep. Orr, W.C., Duke, J.C., Imes, N.K., Mellow, M.H. Aliment. Pharmacol. Ther. (1994) [Pubmed]
  6. Alzheimer's disease and angiogenesis. Vagnucci, A.H., Li, W.W. Lancet (2003) [Pubmed]
  7. The medical management of reflux esophagitis. Role of antacids and acid inhibition. Sontag, S.J. Gastroenterol. Clin. North Am. (1990) [Pubmed]
  8. Actions of histamine in the suprachiasmatic nucleus of the Syrian hamster. Scott, G., Piggins, H.D., Semba, K., Rusak, B. Brain Res. (1998) [Pubmed]
  9. Loss of striatal histamine H2 receptors in Huntington's chorea but not in Parkinson's disease: comparison with animal models. Martínez-Mir, M.I., Pollard, H., Moreau, J., Traiffort, E., Ruat, M., Schwartz, J.C., Palacios, J.M. Synapse (1993) [Pubmed]
  10. A comparison of sucralfate and ranitidine for the prevention of upper gastrointestinal bleeding in patients requiring mechanical ventilation. Canadian Critical Care Trials Group. Cook, D., Guyatt, G., Marshall, J., Leasa, D., Fuller, H., Hall, R., Peters, S., Rutledge, F., Griffith, L., McLellan, A., Wood, G., Kirby, A. N. Engl. J. Med. (1998) [Pubmed]
  11. High-dose pancreatic-enzyme supplements and fibrosing colonopathy in children with cystic fibrosis. FitzSimmons, S.C., Burkhart, G.A., Borowitz, D., Grand, R.J., Hammerstrom, T., Durie, P.R., Lloyd-Still, J.D., Lowenfels, A.B. N. Engl. J. Med. (1997) [Pubmed]
  12. Famotidine for the prevention of gastric and duodenal ulcers caused by nonsteroidal antiinflammatory drugs. Taha, A.S., Hudson, N., Hawkey, C.J., Swannell, A.J., Trye, P.N., Cottrell, J., Mann, S.G., Simon, T.J., Sturrock, R.D., Russell, R.I. N. Engl. J. Med. (1996) [Pubmed]
  13. A controlled study of ranitidine for the prevention of recurrent hemorrhage from duodenal ulcer. Jensen, D.M., Cheng, S., Kovacs, T.O., Randall, G., Jensen, M.E., Reedy, T., Frankl, H., Machicado, G., Smith, J., Silpa, M. N. Engl. J. Med. (1994) [Pubmed]
  14. H2 receptor blockade and bronchial hyperreactivity to histamine in asthma. Nogrady, S.G., Bevan, C. Thorax (1981) [Pubmed]
  15. Analysis of histamine receptors in the central thermoregulatory mechanism of Mastomys natalensis. Dhawan, B.N., Shukla, R., Srimal, R.C. Br. J. Pharmacol. (1982) [Pubmed]
  16. H2-receptor-mediated vasodilation contributes to postexercise hypotension. McCord, J.L., Beasley, J.M., Halliwill, J.R. J. Appl. Physiol. (2006) [Pubmed]
  17. Histamine antagonists in the treatment of acute allergic reactions. Runge, J.W., Martinez, J.C., Caravati, E.M., Williamson, S.G., Hartsell, S.C. Annals of emergency medicine. (1992) [Pubmed]
  18. A double blind trial of H1 and H2 receptor antagonists in the treatment of atopic dermatitis. Frosch, P.J., Schwanitz, H.J., Macher, E. Arch. Dermatol. Res. (1984) [Pubmed]
  19. Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases. Shayo, C., Fernandez, N., Legnazzi, B.L., Monczor, F., Mladovan, A., Baldi, A., Davio, C. Mol. Pharmacol. (2001) [Pubmed]
  20. Nitric oxide mediates histamine induced down-regulation of H2 receptor mRNA and internalization of the receptor protein (R1). Schaefer, U., Schneider, A., Rudroff, C., Neugebauer, E. Cell. Mol. Life Sci. (2003) [Pubmed]
  21. The human histamine H2-receptor couples more efficiently to Sf9 insect cell Gs-proteins than to insect cell Gq-proteins: limitations of Sf9 cells for the analysis of receptor/Gq-protein coupling. Houston, C., Wenzel-Seifert, K., Bürckstümmer, T., Seifert, R. J. Neurochem. (2002) [Pubmed]
  22. Alteration of intracellular histamine H2 receptor cycling precedes antagonist-induced upregulation. Osawa, S., Kajimura, M., Yamamoto, S., Ikuma, M., Mochizuki, C., Iwasaki, H., Hishida, A., Terakawa, S. Am. J. Physiol. Gastrointest. Liver Physiol. (2005) [Pubmed]
  23. Histamine H4 receptor stimulation suppresses IL-12p70 production and mediates chemotaxis in human monocyte-derived dendritic cells. Gutzmer, R., Diestel, C., Mommert, S., Köther, B., Stark, H., Wittmann, M., Werfel, T. J. Immunol. (2005) [Pubmed]
  24. Reactivity of heparin with the human plasma heparin-binding proteins thrombin, antithrombin III, and apolipoproteins E and B-100. Cardin, A.D., Barnhart, R.L., Witt, K.R., Jackson, R.L. Thromb. Res. (1984) [Pubmed]
  25. Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells. Gutzmer, R., Langer, K., Lisewski, M., Mommert, S., Rieckborn, D., Kapp, A., Werfel, T. J. Allergy Clin. Immunol. (2002) [Pubmed]
  26. Human skin mast cells express H2 and H4, but not H3 receptors. Lippert, U., Artuc, M., Grützkau, A., Babina, M., Guhl, S., Haase, I., Blaschke, V., Zachmann, K., Knosalla, M., Middel, P., Krüger-Krasagakis, S., Henz, B.M. J. Invest. Dermatol. (2004) [Pubmed]
  27. Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor. Seifert, R., Wenzel-Seifert, K., Burckstummer, T., Pertz, H.H., Schunack, W., Dove, S., Buschauer, A., Elz, S. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  28. Regulation of antibody-dependent cellular cytotoxicity in multiple sclerosis by central nervous system hormones. Merrill, J.E., Mohlstrom, C. Int. Arch. Allergy Appl. Immunol. (1987) [Pubmed]
  29. Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model. Monczor, F., Fernandez, N., Legnazzi, B.L., Riveiro, M.E., Baldi, A., Shayo, C., Davio, C. Mol. Pharmacol. (2003) [Pubmed]
  30. A new model for the agonistic binding site on the histamine H2-receptor: the catalytic triad in serine proteases as a model for the binding site of histamine H2-receptor agonists. Nederkoorn, P.H., Vernooijs, P., Donné-Op den Kelder, G.M., Baerends, E.J., Timmerman, H. Journal of molecular graphics. (1994) [Pubmed]
  31. Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells. Tanimoto, A., Murata, Y., Nomaguchi, M., Kimura, S., Arima, N., Xu, H., Hamada, T., Sasaguri, Y. FEBS Lett. (2001) [Pubmed]
  32. Histamine receptors on lymphocytes: distribution and functional significance. Sachs, B., Hertl, M., Merk, H.F. Skin Pharmacol. Appl. Skin Physiol. (2000) [Pubmed]
  33. Recent advances in molecular pharmacology of the histamine systems: immune regulatory roles of histamine produced by leukocytes. Tanaka, S., Ichikawa, A. J. Pharmacol. Sci. (2006) [Pubmed]
  34. Histaminergic regulation of prolactin secretion: dose-response relationship and possible involvement of the dopaminergic system. Knigge, U., Thuesen, B., Christiansen, P.M. J. Clin. Endocrinol. Metab. (1986) [Pubmed]
  35. Effect of histamine H2-receptor stimulation on bombesin- and peptone-stimulated gastrin release in man. Kleibeuker, J.H., Kooi, H., Lamers, C.B. Dig. Dis. Sci. (1986) [Pubmed]
  36. Histamine influences the expression of the interleukin-6 receptor on human lymphoid, monocytoid and hepatoma cell lines. Merétey, K., Falus, A., Taga, T., Kishimoto, T. Agents Actions (1991) [Pubmed]
  37. Allelic variations of the human histamine H2 receptor gene. Orange, P.R., Heath, P.R., Wright, S.R., Pearson, R.C. Neuroreport (1996) [Pubmed]
  38. Molecular cloning of the human histamine H2 receptor. Gantz, I., Munzert, G., Tashiro, T., Schäffer, M., Wang, L., DelValle, J., Yamada, T. Biochem. Biophys. Res. Commun. (1991) [Pubmed]
  39. The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart. Traiffort, E., Vizuete, M.L., Tardivel-Lacombe, J., Souil, E., Schwartz, J.C., Ruat, M. Biochem. Biophys. Res. Commun. (1995) [Pubmed]
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