Histamine H2 receptor
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| Location (UCSC) | Chr 5: 175.66 – 175.71 Mb | Chr 13: 54.35 – 54.39 Mb | |||||||
| PubMed search | [3] | [4] | |||||||
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H2 receptors are positively coupled to
cAMP production, which leads to activation of protein kinase A.[5] PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine
H2 receptor agonist.
Function
enterochromaffin-like cells, and neurons.[5] 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.[6] Histamine may play a role in penile erection.[7]
Tissue distribution
Histamine H2 receptors are expressed in the following tissues:
- Gastric parietal cells (oxyntic cells)
- Vascular smooth muscle
- Neutrophils
- Mast cells
- Heart
- Genitourinary system[9] (uterus, bladder)
- Central nervous system tissues[8]
- Caudate–putamen
- Cerebral cortex (external layers)
- Hippocampal formation
- Dentate nucleus of the cerebellum
Physiological responses
Activation of the H2 receptor results in the following physiological responses:
- Stimulation of GERD)
- Smooth muscle relaxation (Experimental histamine H2 receptor agonist used for asthma and COPD)
- Inhibit T-cell proliferation and cytokineproduction
- Inhibition of neutrophil activation and chemotaxis[8]
See also
- H2-receptor antagonist
- Histamine H1-receptor
- Histamine H3-receptor
- Histamine H4-receptor
References
- ^ a b c GRCh38: Ensembl release 89: ENSG00000113749 - Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000034987 - Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ PMID 9311023.
- ^ "Entrez Gene: HRH2 histamine receptor H2".
- PMID 7850330.
- ^ a b c 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.
- S2CID 24764785.
- 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" (PDF). Biochemical and Biophysical Research Communications. 178 (3): 1386–92. 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. 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. 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. 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. 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. S2CID 6034918.
- 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. S2CID 33650873.
- 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. 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. 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. S2CID 28710647.
- 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. S2CID 24358588.
- 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. S2CID 7257298.
- 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. 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. S2CID 24392073.
External links
- "Histamine Receptors: H2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- H2+receptors at the U.S. 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.