Open Access Articles- Top Results for Histamine H2 receptor

Histamine H2 receptor

SymbolsHRH2 ; H2R
External IDsOMIM142703 MGI108482 HomoloGene40613 IUPHAR: 263 ChEMBL: 1941 GeneCards: HRH2 Gene
RNA expression pattern
File:PBB GE HRH2 220805 at tn.png
More reference expression data
RefSeq (mRNA)NM_001131055NM_001010973
RefSeq (protein)NP_001124527NP_001010973
Location (UCSC)Chr 5:
175.09 – 175.11 Mb
Chr 13:
54.19 – 54.22 Mb
PubMed search[1][2]

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

It is found here:[1]

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.[3]

See also


  1. ^ a b c Hill SJ; Ganellin CR; Timmerman H et al. (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Review 49 (3): 253–78. PMID 9311023. 
  2. ^ "Entrez Gene: HRH2 histamine receptor H2". 
  3. ^ 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 (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. doi:10.1016/0006-291X(91)91047-G. 
  • 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. doi:10.1006/bbrc.1995.2404. 
  • 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. PMID 7755641. doi:10.1006/bbrc.1995.1703. 
  • 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. doi:10.1006/bbrc.1995.1851. 
  • 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. doi:10.1097/00001756-199605170-00015. 
  • 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. 
  • 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. doi:10.1016/S0014-5793(99)00618-3. 
  • 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. 
  • 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. doi:10.4049/jimmunol.167.3.1663. 
  • 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. doi:10.1007/PL00000269. 
  • 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. 
  • 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. doi:10.1016/S0014-5793(01)03073-3. 
  • 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. doi:10.1067/mai.2002.121944. 
  • 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. PMC 139241. PMID 12477932. doi:10.1073/pnas.242603899. 
  • 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. doi:10.1081/RRS-120018758. 

External links

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