Histamine H2 receptor
|Histamine receptor H2|
|External IDs||IUPHAR: ChEMBL: GeneCards:|
|RNA expression pattern|
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. PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a Histamine H2 receptor agonist.
- Function 1
- Tissue distribution 2
- Physiological responses 3
- See also 4
- References 5
- Further reading 6
- External links 7
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.
It is found here:
- Gastric parietal cells (oxyntic cells)
- Vascular smooth muscle
- Central nervous system
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
- Vasodilation – PKA 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.
- Hill SJ, Ganellin CR, Timmerman H, et al. (1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Review 49 (3): 253–78.
- "Entrez Gene: HRH2 histamine receptor H2".
- Walter F., PhD. Boron (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. Page 479
- Del Valle J, Gantz I (1997). "Novel insights into histamine H2 receptor biology". Am. J. Physiol. 273 (5 Pt 1): G987–96.
- 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.
- 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.
- 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.
- 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.
- 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.
- Orange PR, Heath PR, Wright SR, Pearson RC (1996). "Allelic variations of the human histamine H2 receptor gene". Neuroreport 7 (7): 1293–6.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- "2"Histamine Receptors: H. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- H2 receptors at the US National Library of Medicine Medical Subject Headings (MeSH)