Histamine H2 receptor

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The correct title of this article is Histamine H2 receptor. It appears incorrectly here because of technical restrictions.
Histamine receptor H2
Identifiers
Symbol(s) HRH2; H2R
External IDs OMIM: 142703 MGI: 108482 HomoloGene: 40613
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 3274 15466
Ensembl ENSG00000113749 ENSMUSG00000034987
Uniprot P25021 Q3ZB30
Refseq NM_022304 (mRNA)
NP_071640 (protein)		 NM_001010973 (mRNA)
NP_001010973 (protein)
Location Chr 5: 175.02 - 175.05 Mb Chr 13: 54.2 - 54.23 Mb
Pubmed search [1] [2]

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. 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.[1]

Contents

[edit] Location

[edit] Response

[edit] 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.[2]

[edit] H2-receptor agonists and antagonists

see H2-receptor agonist and H2-receptor antagonist

[edit] References

  1. ^ Entrez Gene: HRH2 histamine receptor H2.
  2. ^ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3.  Page 479

[edit] 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 
  • 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. 

[edit] External links

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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1 (A, B, D), α2 (A, B, C), β1, β2, β3) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - Eicosanoid (CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin ((DP (1, 2), EP (1, 2, 3, 4), PGF, Prostacyclin, Thromboxane) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - neuromedin (B, U (1, 2)) - Neuropeptide (B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like
Class C: Metabotropic
glutamate / pheromone
Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened