Histamine H2 receptor

Histamine receptor H2
Identifiers
Symbols	HRH2 ; H2R
External IDs	Template:OMIM5 Template:MGI HomoloGene: 40613
Gene ontology Molecular function Template:GNF GO Template:GNF GO Template:GNF GO Cellular component Template:GNF GO Template:GNF GO Template:GNF GO Biological process Template:GNF GO Template:GNF GO Template:GNF GO Template:GNF GO
RNA expression pattern
More reference expression data
Orthologs
Template:GNF Ortholog box
Species	Human	Mouse
Entrez	n/a	n/a
Ensembl	n/a	n/a
UniProt	n/a	n/a
RefSeq (mRNA)	n/a	n/a
RefSeq (protein)	n/a	n/a
Location (UCSC)	n/a	n/a
PubMed search	n/a	n/a

H₂ receptors positively coupled to adenylate cyclase via G_s. 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. Histamine receptor H2 belongs to the family 1 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.

Location

• Gastric parietal cells (oxyntic cells)
• Vascular smooth muscle
• Neutrophils
• Central nervous system
• Heart
• Uterus

Response

• Stimulation of gastric acid secretion
• Smooth muscle relaxation
  • Vasodilation
• Inhibit antibody synthesis, T-cell proliferation and cytokine production

Vasodilation

In vasodilation, PKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in dephosphorylation of MLC of myosin. The smooth muscle relaxation leads to vasodilation.

H₂-receptor agonists and antagonists

see H2-receptor agonist and H2-receptor antagonist

Further reading

• Hill SJ, Ganellin CR, Timmerman H; et al. (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacol. Rev. 49 (3): 253–78. PMID 9311023.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Del Valle J, Gantz I (1997). "Novel insights into histamine H2 receptor biology". Am. J. Physiol. 273 (5 Pt 1): G987–96. PMID 9374694.
• Gantz I, Munzert G, Tashiro T; et al. (1991). "Molecular cloning of the human histamine H2 receptor". Biochem. Biophys. Res. Commun. 178 (3): 1386–92. PMID 1714721.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Vannier E, Dinarello CA (1994). "Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells". J. Biol. Chem. 269 (13): 9952–6. PMID 7511596.
• Smit MJ, Timmerman H, Alewijnse AE; et al. (1995). "Visualization of agonist-induced internalization of histamine H2 receptors". Biochem. Biophys. Res. Commun. 214 (3): 1138–45. PMID 7575521.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Nishi T, Koike T, Oka T; et al. (1995). "Identification of the promoter region of the human histamine H2-receptor gene". Biochem. Biophys. Res. Commun. 210 (2): 616–23. doi:10.1006/bbrc.1995.1703. PMID 7755641.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Traiffort E, Vizuete ML, Tardivel-Lacombe J; et al. (1995). "The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart". Biochem. Biophys. Res. Commun. 211 (2): 570–7. PMID 7794271.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Orange PR, Heath PR, Wright SR, Pearson RC (1996). "Allelic variations of the human histamine H2 receptor gene". Neuroreport. 7 (7): 1293–6. PMID 8817552.CS1 maint: Multiple names: authors list (link)
• Elenkov IJ, Webster E, Papanicolaou DA; et al. (1998). "Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors". J. Immunol. 161 (5): 2586–93. PMID 9725260.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Murakami H, Sun-Wada GH, Matsumoto M; et al. (1999). "Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression". FEBS Lett. 451 (3): 327–31. PMID 10371214.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Wang LD, Wang M, Todisco A; et al. (2000). "The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner". Am. J. Physiol., Cell Physiol. 278 (6): C1246–55. PMID 10837353.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Suh BC, Lee H, Jun DJ; et al. (2001). "Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells". J. Immunol. 167 (3): 1663–71. PMID 11466390.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Brew OB, Sullivan MH (2002). "Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy". Inflamm. Res. 50 (9): 449–52. PMID 11603849.
• Shayo C, Fernandez N, Legnazzi BL; et al. (2001). "Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases". Mol. Pharmacol. 60 (5): 1049–56. PMID 11641433.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Tanimoto A, Murata Y, Nomaguchi M; et al. (2001). "Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells". FEBS Lett. 508 (3): 345–9. PMID 11728449.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Gutzmer R, Langer K, Lisewski M; et al. (2002). "Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells". J. Allergy Clin. Immunol. 109 (3): 524–31. PMID 11898002.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMID 12477932.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Esbenshade TA, Kang CH, Krueger KM; et al. (2003). "Differential activation of dual signaling responses by human H1 and H2 histamine receptors". J. Recept. Signal Transduct. Res. 23 (1): 17–31. PMID 12680587.CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)

External links

• IUPHAR GPCR Database - H₂ Histamine Receptor
• H2+receptors at the US National Library of Medicine Medical Subject Headings (MeSH)

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