Histamine H2 receptor

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External IDsGeneCards: [1]
RefSeq (mRNA)



RefSeq (protein)



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H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A.[1] PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist.


Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons.[1] Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. It is an integral membrane protein and stimulates gastric acid secretion. It also regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation.[2]

Tissue distribution

Histamine H2 receptors are expressed in the following tissues:

Peripheral tissues[1][3]
Central nervous system tissues[3]

Physiological responses

Activation of the H2 receptor results in the following physiological responses:

  • Stimulation of gastric acid secretion (Target of anti-histaminergics (H2 receptors) for peptic ulcer disease and GERD)
  • Smooth muscle relaxation (Experimental histamine H2 receptor agonist used for asthma and COPD)
  • Inhibit antibody synthesis, T-cell proliferation and cytokine production
  • VasodilationPKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in MLC of myosin being dephosphorylated by MLCP and thus inhibiting contraction. The smooth muscle relaxation leads to vasodilation.[4]
  • Inhibition of neutrophil activation and chemotaxis[3]

See also


  1. 1.0 1.1 1.2 Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (Sep 1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253–78. PMID 9311023.
  2. "Entrez Gene: HRH2 histamine receptor H2".
  3. 3.0 3.1 3.2 Maguire JJ, Davenport AP (29 November 2016). "H2 receptor". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 March 2017.
  4. Walter F., PhD. Boron (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 479

Further reading

  • Del Valle J, Gantz I (Nov 1997). "Novel insights into histamine H2 receptor biology". The American Journal of Physiology. 273 (5 Pt 1): G987–96. PMID 9374694.
  • Gantz I, Munzert G, Tashiro T, Schäffer M, Wang L, DelValle J, Yamada T (Aug 1991). "Molecular cloning of the human histamine H2 receptor". Biochemical and Biophysical Research Communications. 178 (3): 1386–92. doi:10.1016/0006-291X(91)91047-G. PMID 1714721.
  • Vannier E, Dinarello CA (Apr 1994). "Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells". The Journal of Biological Chemistry. 269 (13): 9952–6. PMID 7511596.
  • Smit MJ, Timmerman H, Alewijnse AE, Punin M, van den Nieuwenhof I, Blauw J, van Minnen J, Leurs R (Sep 1995). "Visualization of agonist-induced internalization of histamine H2 receptors". Biochemical and Biophysical Research Communications. 214 (3): 1138–45. doi:10.1006/bbrc.1995.2404. PMID 7575521.
  • Nishi T, Koike T, Oka T, Maeda M, Futai M (May 1995). "Identification of the promoter region of the human histamine H2-receptor gene". Biochemical and Biophysical Research Communications. 210 (2): 616–23. doi:10.1006/bbrc.1995.1703. PMID 7755641.
  • Traiffort E, Vizuete ML, Tardivel-Lacombe J, Souil E, Schwartz JC, Ruat M (Jun 1995). "The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart". Biochemical and Biophysical Research Communications. 211 (2): 570–7. doi:10.1006/bbrc.1995.1851. PMID 7794271.
  • Orange PR, Heath PR, Wright SR, Pearson RC (May 1996). "Allelic variations of the human histamine H2 receptor gene". NeuroReport. 7 (7): 1293–6. doi:10.1097/00001756-199605170-00015. PMID 8817552.
  • Elenkov IJ, Webster E, Papanicolaou DA, Fleisher TA, Chrousos GP, Wilder RL (Sep 1998). "Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors". Journal of Immunology. 161 (5): 2586–93. PMID 9725260.
  • Murakami H, Sun-Wada GH, Matsumoto M, Nishi T, Wada Y, Futai M (May 1999). "Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression". FEBS Letters. 451 (3): 327–31. doi:10.1016/S0014-5793(99)00618-3. PMID 10371214.
  • Wang LD, Wang M, Todisco A, Grand E, del Valle J (Jun 2000). "The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner". American Journal of Physiology. Cell Physiology. 278 (6): C1246–55. doi:10.1152/ajpcell.2000.278.6.c1246. PMID 10837353.
  • Suh BC, Lee H, Jun DJ, Chun JS, Lee JH, Kim KT (Aug 2001). "Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells". Journal of Immunology. 167 (3): 1663–71. doi:10.4049/jimmunol.167.3.1663. PMID 11466390.
  • Brew OB, Sullivan MH (Sep 2001). "Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy". Inflammation Research. 50 (9): 449–52. doi:10.1007/PL00000269. PMID 11603849.
  • Shayo C, Fernandez N, Legnazzi BL, Monczor F, Mladovan A, Baldi A, Davio C (Nov 2001). "Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases". Molecular Pharmacology. 60 (5): 1049–56. PMID 11641433.
  • Tanimoto A, Murata Y, Nomaguchi M, Kimura S, Arima N, Xu H, Hamada T, Sasaguri Y (Nov 2001). "Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells". FEBS Letters. 508 (3): 345–9. doi:10.1016/S0014-5793(01)03073-3. PMID 11728449.
  • Gutzmer R, Langer K, Lisewski M, Mommert S, Rieckborn D, Kapp A, Werfel T (Mar 2002). "Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells". The Journal of Allergy and Clinical Immunology. 109 (3): 524–31. doi:10.1067/mai.2002.121944. PMID 11898002.
  • Esbenshade TA, Kang CH, Krueger KM, Miller TR, Witte DG, Roch JM, Masters JN, Hancock AA (Feb 2003). "Differential activation of dual signaling responses by human H1 and H2 histamine receptors". Journal of Receptor and Signal Transduction Research. 23 (1): 17–31. doi:10.1081/RRS-120018758. PMID 12680587.

External links

This article incorporates text from the United States National Library of Medicine, which is in the public domain.