Histamine H2 receptor

Histamine H2 receptor

H2 receptors positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production. It increases the intracellular Ca2+ concentrations and release Ca2+ from intracellular stores. 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. 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.cite web | title = Entrez Gene: HRH2 histamine receptor H2| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3274| accessdate = ]

Tissue distribution

*Gastric parietal cells (oxyntic cells)
*Vascular smooth muscle
*Central nervous system

Physiological responses

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

* Stimulation of gastric acid secretion
* Smooth muscle relaxation
* Inhibit antibody synthesis, T-cell proliferation and cytokine production
* VasodilationPKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in dephosphorylation of MLC of myosin. The smooth muscle relaxation leads to vasodilation. cite book |author=Walter F., PhD. Boron|title=Medical Physiology: A Cellular And Molecular Approaoch|publisher=Elsevier/Saunders|location=|year= |pages= |isbn=1-4160-2328-3 |oclc= |doi= Page 479 ]

See also

* H2-receptor antagonist


Further reading

citations =
*cite journal | author=Hill SJ, Ganellin CR, Timmerman H, "et al." |title=International Union of Pharmacology. XIII. Classification of histamine receptors. |journal=Pharmacol. Rev. |volume=49 |issue= 3 |pages= 253–78 |year= 1997 |pmid= 9311023 |doi=
*cite journal | author=Del Valle J, Gantz I |title=Novel insights into histamine H2 receptor biology. |journal=Am. J. Physiol. |volume=273 |issue= 5 Pt 1 |pages= G987–96 |year= 1997 |pmid= 9374694 |doi=
*cite journal | author=Gantz I, Munzert G, Tashiro T, "et al." |title=Molecular cloning of the human histamine H2 receptor. |journal=Biochem. Biophys. Res. Commun. |volume=178 |issue= 3 |pages= 1386–92 |year= 1991 |pmid= 1714721 |doi=
*cite journal | author=Vannier E, Dinarello CA |title=Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells. |journal=J. Biol. Chem. |volume=269 |issue= 13 |pages= 9952–6 |year= 1994 |pmid= 7511596 |doi=
*cite journal | author=Smit MJ, Timmerman H, Alewijnse AE, "et al." |title=Visualization of agonist-induced internalization of histamine H2 receptors. |journal=Biochem. Biophys. Res. Commun. |volume=214 |issue= 3 |pages= 1138–45 |year= 1995 |pmid= 7575521 |doi=
*cite journal | author=Nishi T, Koike T, Oka T, "et al." |title=Identification of the promoter region of the human histamine H2-receptor gene. |journal=Biochem. Biophys. Res. Commun. |volume=210 |issue= 2 |pages= 616–23 |year= 1995 |pmid= 7755641 |doi= 10.1006/bbrc.1995.1703
*cite journal | author=Traiffort E, Vizuete ML, Tardivel-Lacombe J, "et al." |title=The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart. |journal=Biochem. Biophys. Res. Commun. |volume=211 |issue= 2 |pages= 570–7 |year= 1995 |pmid= 7794271 |doi=
*cite journal | author=Orange PR, Heath PR, Wright SR, Pearson RC |title=Allelic variations of the human histamine H2 receptor gene. |journal=Neuroreport |volume=7 |issue= 7 |pages= 1293–6 |year= 1996 |pmid= 8817552 |doi=
*cite journal | author=Elenkov IJ, Webster E, Papanicolaou DA, "et al." |title=Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors. |journal=J. Immunol. |volume=161 |issue= 5 |pages= 2586–93 |year= 1998 |pmid= 9725260 |doi=
*cite journal | author=Murakami H, Sun-Wada GH, Matsumoto M, "et al." |title=Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression. |journal=FEBS Lett. |volume=451 |issue= 3 |pages= 327–31 |year= 1999 |pmid= 10371214 |doi=
*cite journal | author=Wang LD, Wang M, Todisco A, "et al." |title=The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner. |journal=Am. J. Physiol., Cell Physiol. |volume=278 |issue= 6 |pages= C1246–55 |year= 2000 |pmid= 10837353 |doi=
*cite journal | author=Suh BC, Lee H, Jun DJ, "et al." |title=Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells. |journal=J. Immunol. |volume=167 |issue= 3 |pages= 1663–71 |year= 2001 |pmid= 11466390 |doi=
*cite journal | author=Brew OB, Sullivan MH |title=Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy. |journal=Inflamm. Res. |volume=50 |issue= 9 |pages= 449–52 |year= 2002 |pmid= 11603849 |doi=
*cite journal | author=Shayo C, Fernandez N, Legnazzi BL, "et al." |title=Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases. |journal=Mol. Pharmacol. |volume=60 |issue= 5 |pages= 1049–56 |year= 2001 |pmid= 11641433 |doi=
*cite journal | author=Tanimoto A, Murata Y, Nomaguchi M, "et al." |title=Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells. |journal=FEBS Lett. |volume=508 |issue= 3 |pages= 345–9 |year= 2001 |pmid= 11728449 |doi=
*cite journal | author=Gutzmer R, Langer K, Lisewski M, "et al." |title=Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells. |journal=J. Allergy Clin. Immunol. |volume=109 |issue= 3 |pages= 524–31 |year= 2002 |pmid= 11898002 |doi=
*cite journal | author=Strausberg RL, Feingold EA, Grouse LH, "et al." |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899–903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899
*cite journal | author=Esbenshade TA, Kang CH, Krueger KM, "et al." |title=Differential activation of dual signaling responses by human H1 and H2 histamine receptors. |journal=J. Recept. Signal Transduct. Res. |volume=23 |issue= 1 |pages= 17–31 |year= 2003 |pmid= 12680587 |doi=

External links

* [http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2305 IUPHAR GPCR Database - H2 Histamine Receptor]

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