histamine H2 receptor

ヒスタミンH2受容体、ヒスタミンH2レセプター

関

H2 receptor

WordNet

1. the 8th letter of the Roman alphabet (同)h
2. amine formed from histidine that stimulates gastric secretions and dilates blood vessels; released by the human immune system during allergic reactions
3. a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

1. hydrogenの化学記号
2. 鉛筆の硬度 / 《俗》heroin
3. ヒスタミン(子宮収縮・血圧降下の薬)
4. =sense organ / 受信装置

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/18 02:01:31」(JST)

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Histamine receptor H2
Identifiers
Symbols	HRH2 ; H2R
External IDs	OMIM: 142703 MGI: 108482 HomoloGene: 40613 IUPHAR: 263 ChEMBL: 1941 GeneCards: HRH2 Gene
Gene ontology Molecular function • histamine receptor activity Cellular component • plasma membrane • integral component of plasma membrane Biological process • histamine-induced gastric acid secretion • gastrin-induced gastric acid secretion • epithelial cell morphogenesis • immune response • G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger • memory • visual learning • positive regulation of vasoconstriction • regulation of synaptic plasticity • digestive tract development • gland development Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	3274	15466
Ensembl	ENSG00000113749	ENSMUSG00000034987
UniProt	P25021	P97292
RefSeq (mRNA)	NM_001131055	NM_001010973
RefSeq (protein)	NP_001124527	NP_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 G_s. 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

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.

Tissue distribution

It is found here:

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

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
• 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.

See also

• H2-receptor antagonist

References

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. doi:10.1016/0006-291X(91)91047-G. 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. doi:10.1006/bbrc.1995.2404. 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. doi:10.1006/bbrc.1995.1851. 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. doi:10.1097/00001756-199605170-00015. 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. doi:10.1016/S0014-5793(99)00618-3. 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. doi:10.4049/jimmunol.167.3.1663. 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. doi:10.1007/PL00000269. 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. doi:10.1016/S0014-5793(01)03073-3. 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. doi:10.1067/mai.2002.121944. 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. PMC 139241. 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. doi:10.1081/RRS-120018758. PMID 12680587. 

External links

• "Histamine Receptors: H₂". 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)

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

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 胃酸分泌の生理学 physiology of gastric acid secretion
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English Journal

• Influence of nitric oxide agents in the dorsal hippocampus of mice on anxiogenic-like effect induced by histamine.

• Piri M, Nasehi M, Asgariyan M, Zarrindast MR.SourceDepartment of Biology, Faculty of Basic Sciences, Islamic Azad University, Ardabil Branch, Ardabil, Iran.
• Pharmacology, biochemistry, and behavior.Pharmacol Biochem Behav.2012 Sep;102(3):391-9. Epub 2012 Jun 9.
• Histaminergic receptors and neuronal nitric oxide synthase (nNOS) are co-expressed at high levels in the hippocampal neurons and alter anxiety-like behaviors in rodents. Since the dorsal hippocampus may be involved in modulation of anxiety-like behaviors, the aim of the present study was to assess w
• PMID 22687724

• Histaminergic pharmacology of homo-oligomeric β3 γ-aminobutyric acid type A receptors characterized by surface plasmon resonance biosensor technology.

• Seeger C, Christopeit T, Fuchs K, Grote K, Sieghart W, Danielson UH.SourceBeactica AB, Uppsala, Sweden; Department of Chemistry - BMC, Uppsala, Sweden.
• Biochemical pharmacology.Biochem Pharmacol.2012 Aug 1;84(3):341-51. Epub 2012 Apr 15.
• A surface plasmon resonance biosensor assay was established for studying the interactions of 51 histaminergic and 15 GABAergic ligands with homo-oligomeric β3 GABA(A) receptors. Detergent solubilized receptors were successfully immobilized via affinity-capture on biosensor surfaces. The interaction
• PMID 22531219

Japanese Journal

• I-1．急性膵炎の薬物療法

• 膵臓 30(6), 733-740, 2015
• NAID 130005126563

• CCL22/Macrophage-derived Chemokine Expression in Apolipoprotein E-deficient Mice and Effects of Histamine in the Setting of Atherosclerosis

• Journal of Atherosclerosis and Thrombosis 22(6), 599-609, 2015
• NAID 130005078025

• CCL22/Macrophage-derived Chemokine Expression in Apolipoprotein E-deficient Mice and Effects of Histamine in the Setting of Atherosclerosis

• Journal of Atherosclerosis and Thrombosis advpub(0), 2015
• NAID 130004713049

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★リンクテーブル★

リンク元	「H2受容体」
関連記事	「H」

「H2受容体」

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英

H2 receptor

同

ヒスタミンH2受容体 histamine H2 receptor、H2レセプター

関

ヒスタミン、ヒスタミン受容体

• 胃酸分泌に関与するヒスタミン受容体サブタイプ

「H」

　　[★]

• 食道裂孔
• ヒスチジン
• 水素