Histamine H2 receptor: Difference between revisions

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Latest revision as of 20:21, 13 January 2018

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.^[1] 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.^[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

Histamine H₂ receptors are expressed in the following tissues:

Peripheral tissues^[1]^[3]

Central nervous system tissues^[3]

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.^[4]
Inhibition of neutrophil activation and chemotaxis^[3]

References

↑ ^1.0 ^1.1 ^1.2 Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (Sep 1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253–78. PMID 9311023.
↑ "Entrez Gene: HRH2 histamine receptor H2".
↑ ^3.0 ^3.1 ^3.2 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.
↑ Walter F., PhD. Boron (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 479

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". Biochemical and Biophysical Research Communications. 178 (3): 1386–92. doi:10.1016/0006-291X(91)91047-G. 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. doi:10.1006/bbrc.1995.2404. 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. doi:10.1006/bbrc.1995.1703. 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. doi:10.1006/bbrc.1995.1851. 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. doi:10.1097/00001756-199605170-00015. 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. PMID 9725260.
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. doi:10.1016/S0014-5793(99)00618-3. PMID 10371214.
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. doi:10.1152/ajpcell.2000.278.6.c1246. 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. doi:10.4049/jimmunol.167.3.1663. 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. doi:10.1007/PL00000269. PMID 11603849.
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. PMID 11641433.
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. doi:10.1016/S0014-5793(01)03073-3. PMID 11728449.
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. doi:10.1067/mai.2002.121944. 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. 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.

[PR1997-1] 1.0 ^1.1 ^1.2 Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL (Sep 1997). "International Union of Pharmacology. XIII. Classification of histamine receptors". Pharmacological Reviews. 49 (3): 253–78. PMID 9311023.

[entrez-2] "Entrez Gene: HRH2 histamine receptor H2".

[IUPHAR_HRH2-3] 3.0 ^3.1 ^3.2 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.

[boron-4] Walter F., PhD. Boron (2005). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 479

[1]

[2]

[3]

[4]

@@ Line 1: / Line 1: @@
-{{Wrongtitle|title=Histamine H<sub>2</sub> receptor}}
+{{DISPLAYTITLE:Histamine H<sub>2</sub> receptor}}
- <!-- The PBB_Controls template provides controls for Protein Box Bot, please see Template:PBB_Controls for details. -->
+{{Infobox_gene}}
-{{PBB_Controls
+'''H<sub>2</sub> receptors''' are positively coupled to [[adenylate cyclase]] via [[Gs subunit|G<sub>s</sub>]]. It is a potent stimulant of [[Cyclic AMP|cAMP]] production, which leads to activation of [[protein kinase A]].<ref name = PR1997/> PKA functions to phosphorylate certain proteins, affecting their activity. The drug [[betazole]] is an example of a [[histamine]] H<sub>2</sub> receptor agonist.
-| update_page = yes
-| require_manual_inspection = no
-| update_protein_box = yes
-| update_summary = yes
-| update_citations = yes
-}}
-<!-- The GNF_Protein_box is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
+== Function ==
-{{GNF_Protein_box
+[[Histamine]] is a ubiquitous messenger molecule released from [[mast cell]]s, [[enterochromaffin-like cells]], and [[neuron]]s.<ref name = PR1997/> Its various actions are mediated by histamine receptors H<sub>1</sub>, H<sub>2</sub>, H<sub>3</sub> and H<sub>4</sub>. The histamine receptor H<sub>2</sub> belongs to the [[rhodopsin]]-like family of [[G protein-coupled receptor]]s. 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.<ref name="entrez">{{cite web | title = Entrez Gene: HRH2 histamine receptor H2| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3274| accessdate = }}</ref>
- | image =
- | image_source =
- | PDB =
- | Name = Histamine receptor H2
- | HGNCid = 5183
- | Symbol = HRH2
- | AltSymbols =; H2R
- | OMIM = 142703
- | ECnumber =
- | Homologene = 40613
- | MGIid = 108482
- | GeneAtlas_image1 = PBB_GE_HRH2_220805_at_tn.png
- | Function = {{GNF_GO|id=GO:0001584 |text = rhodopsin-like receptor activity}} {{GNF_GO|id=GO:0004872 |text = receptor activity}} {{GNF_GO|id=GO:0004969 |text = histamine receptor activity}}
- | Component = {{GNF_GO|id=GO:0005887 |text = integral to plasma membrane}} {{GNF_GO|id=GO:0016020 |text = membrane}} {{GNF_GO|id=GO:0016021 |text = integral to membrane}}
- | Process = {{GNF_GO|id=GO:0006955 |text = immune response}} {{GNF_GO|id=GO:0007165 |text = signal transduction}} {{GNF_GO|id=GO:0007186 |text = G-protein coupled receptor protein signaling pathway}} {{GNF_GO|id=GO:0007187 |text = G-protein signaling, coupled to cyclic nucleotide second messenger}}
- | Orthologs = {{GNF_Ortholog_box
-    | Hs_EntrezGene = 3274
-    | Hs_Ensembl = ENSG00000113749
-    | Hs_RefseqProtein = NP_071640
-    | Hs_RefseqmRNA = NM_022304
-    | Hs_GenLoc_db =
-    | Hs_GenLoc_chr = 5
-    | Hs_GenLoc_start = 175017637
-    | Hs_GenLoc_end = 175045847
-    | Hs_Uniprot = P25021
-    | Mm_EntrezGene = 15466
-    | Mm_Ensembl = ENSMUSG00000034987
-    | Mm_RefseqmRNA = NM_001010973
-    | Mm_RefseqProtein = NP_001010973
-    | Mm_GenLoc_db =
-    | Mm_GenLoc_chr = 13
-    | Mm_GenLoc_start = 54201750
-    | Mm_GenLoc_end = 54232053
-    | Mm_Uniprot = Q3ZB30
-  }}
-}}
-'''H<sub>2</sub> receptors''' positively coupled to [[adenylate cyclase]] via [[Gs subunit|G<sub>s</sub>]]. It is a potent stimulant of [[Cyclic_AMP|cAMP]] production. It increases the intracellular [[Ca2+|Ca<sup>2+</sup>]] concentrations and release Ca<sup>2+</sup> from intracellular stores.
-The drug [[Betazole]] is an example of a [[Histamine]] H2 receptor agonist.
+==Tissue distribution==
+Histamine H<sub>2</sub> receptors are expressed in the following tissues:
-<!-- The PBB_Summary template is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
+;Peripheral tissues<ref name = PR1997>{{cite journal | vauthors = Hill SJ, Ganellin CR, Timmerman H, Schwartz JC, Shankley NP, Young JM, Schunack W, Levi R, Haas HL | title = International Union of Pharmacology. XIII. Classification of histamine receptors | journal = Pharmacological Reviews | volume = 49 | issue = 3 | pages = 253–78 | date = Sep 1997 | pmid = 9311023 | doi =  | url = http://pharmrev.aspetjournals.org/content/49/3/253.long }}</ref><ref name="IUPHAR HRH2">{{cite web | title=H<sub>2</sub> receptor|url=http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=263 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | accessdate= 20 March 2017 |vauthors=Maguire JJ, Davenport AP | date=29 November 2016 | quote = }}</ref>
-{{PBB_Summary
-| section_title =
-| summary_text = 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.<ref name="entrez">{{cite web | title = Entrez Gene: HRH2 histamine receptor H2| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3274| accessdate = }}</ref>
-}}
-==Location==
 *Gastric [[parietal cells|parietal cells (oxyntic cells)]]
 *[[Vascular smooth muscle]]
 *[[Neutrophils]]
-*[[Central nervous system]]
+*[[Mast cells]]
 *[[Heart]]
 *[[Uterus]]
-==Response==
+;[[Central nervous system]] tissues<ref name="IUPHAR HRH2" />
-*Stimulation of [[gastric acid]] secretion
+*[[Caudate nucleus|Caudate]]–[[putamen]]
-*[[Smooth muscle]] relaxation
+*[[Cerebral cortex]] (external layers)
-**Vasodilation
+*[[Hippocampal formation]]
-*Inhibit [[antibody]] synthesis, [[T-cell]] proliferation and [[cytokine]] production
+*[[Dentate nucleus]] of the [[cerebellum]]
-===Vasodilation===
+==Physiological responses==
-In [[vasodilation]], [[protein kinase a|PKA]] activity causes phosphorylation of [[myosin light chain kinase|MLCK]], decreasing its activity, resulting in dephosphorylation of MLC of [[myosin]]. The smooth muscle relaxation leads to vasodilation.<ref name=boron> {{cite book |author=Walter F., PhD. Boron |title=Medical Physiology: A Cellular And Molecular Approaoch |publisher=Elsevier/Saunders |location= |year= |pages= |isbn=1-4160-2328-3 |oclc= |doi=}} Page 479 </ref>
+Activation of the H<sub>2</sub> receptor results in the following physiological responses:
-==H<sub>2</sub>-receptor agonists and antagonists==
+* Stimulation of [[gastric acid]] secretion (Target of anti-histaminergics (H<sub>2</sub> receptors) for [[peptic ulcer disease]] and [[GERD]])
-see H2-receptor agonist and [[H2-receptor antagonist]]
+* [[Smooth muscle]] relaxation (Experimental  histamine H<sub>2</sub> receptor agonist used for asthma and COPD)
+* Inhibit [[antibody]] synthesis, [[T-cell]] proliferation and [[cytokine]] production
+* [[Vasodilation]] – [[protein kinase a|PKA]] activity causes phosphorylation of [[myosin light chain kinase|MLCK]], decreasing its activity, resulting in MLC of [[myosin]] being dephosphorylated by MLCP and thus inhibiting contraction. The smooth muscle relaxation leads to vasodilation.<ref name="boron">{{cite book |author=Walter F., PhD. Boron|title=Medical Physiology: A Cellular And Molecular Approaoch|publisher=Elsevier/Saunders|location=|year= 2005|pages= |isbn=1-4160-2328-3 |oclc= |doi=}} Page 479</ref>
+* Inhibition of neutrophil activation and chemotaxis<ref name="IUPHAR HRH2" />
-==References==
+== See also ==
-{{reflist|2}}
+* [[H2 antagonist|H<sub>2</sub>-receptor antagonist]]
-==Further reading==
+== References ==
+{{reflist}}
+== Further reading ==
 {{refbegin | 2}}
-{{PBB_Further_reading
+* {{cite journal | vauthors = Del Valle J, Gantz I | title = Novel insights into histamine H2 receptor biology | journal = The American Journal of Physiology | volume = 273 | issue = 5 Pt 1 | pages = G987-96 | date = Nov 1997 | pmid = 9374694 | doi =  }}
-| citations =
+* {{cite journal | vauthors = Gantz I, Munzert G, Tashiro T, Schäffer M, Wang L, DelValle J, Yamada T | title = Molecular cloning of the human histamine H2 receptor | journal = Biochemical and Biophysical Research Communications | volume = 178 | issue = 3 | pages = 1386–92 | date = Aug 1991 | pmid = 1714721 | doi = 10.1016/0006-291X(91)91047-G }}
-*{{cite journal  | author=Hill SJ, Ganellin CR, Timmerman H, ''et al.'' |title=International Union of Pharmacology. XIII. Classification of histamine receptors. |journal=Pharmacol. Rev. |volume=49 |issue= 3 |pages= 253-78 |year= 1997 |pmid= 9311023 |doi=  }}
+* {{cite journal | vauthors = Vannier E, Dinarello CA | title = Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells | journal = The Journal of Biological Chemistry | volume = 269 | issue = 13 | pages = 9952–6 | date = Apr 1994 | pmid = 7511596 | doi =  }}
-*{{cite journal  | author=Del Valle J, Gantz I |title=Novel insights into histamine H2 receptor biology. |journal=Am. J. Physiol. |volume=273 |issue= 5 Pt 1 |pages= G987-96 |year= 1997 |pmid= 9374694 |doi=  }}
+* {{cite journal | vauthors = Smit MJ, Timmerman H, Alewijnse AE, Punin M, van den Nieuwenhof I, Blauw J, van Minnen J, Leurs R | title = Visualization of agonist-induced internalization of histamine H2 receptors | journal = Biochemical and Biophysical Research Communications | volume = 214 | issue = 3 | pages = 1138–45 | date = Sep 1995 | pmid = 7575521 | doi = 10.1006/bbrc.1995.2404 }}
-*{{cite journal  | author=Gantz I, Munzert G, Tashiro T, ''et al.'' |title=Molecular cloning of the human histamine H2 receptor. |journal=Biochem. Biophys. Res. Commun. |volume=178 |issue= 3 |pages= 1386-92 |year= 1991 |pmid= 1714721 |doi=  }}
+* {{cite journal | vauthors = Nishi T, Koike T, Oka T, Maeda M, Futai M | title = Identification of the promoter region of the human histamine H2-receptor gene | journal = Biochemical and Biophysical Research Communications | volume = 210 | issue = 2 | pages = 616–23 | date = May 1995 | pmid = 7755641 | doi = 10.1006/bbrc.1995.1703 }}
-*{{cite journal  | author=Vannier E, Dinarello CA |title=Histamine enhances interleukin (IL)-1-induced IL-6 gene expression and protein synthesis via H2 receptors in peripheral blood mononuclear cells. |journal=J. Biol. Chem. |volume=269 |issue= 13 |pages= 9952-6 |year= 1994 |pmid= 7511596 |doi=  }}
+* {{cite journal | vauthors = Traiffort E, Vizuete ML, Tardivel-Lacombe J, Souil E, Schwartz JC, Ruat M | title = The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart | journal = Biochemical and Biophysical Research Communications | volume = 211 | issue = 2 | pages = 570–7 | date = Jun 1995 | pmid = 7794271 | doi = 10.1006/bbrc.1995.1851 }}
-*{{cite journal  | author=Smit MJ, Timmerman H, Alewijnse AE, ''et al.'' |title=Visualization of agonist-induced internalization of histamine H2 receptors. |journal=Biochem. Biophys. Res. Commun. |volume=214 |issue= 3 |pages= 1138-45 |year= 1995 |pmid= 7575521 |doi=  }}
+* {{cite journal | vauthors = Orange PR, Heath PR, Wright SR, Pearson RC | title = Allelic variations of the human histamine H2 receptor gene | journal = NeuroReport | volume = 7 | issue = 7 | pages = 1293–6 | date = May 1996 | pmid = 8817552 | doi = 10.1097/00001756-199605170-00015 }}
-*{{cite journal  | author=Nishi T, Koike T, Oka T, ''et al.'' |title=Identification of the promoter region of the human histamine H2-receptor gene. |journal=Biochem. Biophys. Res. Commun. |volume=210 |issue= 2 |pages= 616-23 |year= 1995 |pmid= 7755641 |doi= 10.1006/bbrc.1995.1703 }}
+* {{cite journal | vauthors = Elenkov IJ, Webster E, Papanicolaou DA, Fleisher TA, Chrousos GP, Wilder RL | title = Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors | journal = Journal of Immunology | volume = 161 | issue = 5 | pages = 2586–93 | date = Sep 1998 | pmid = 9725260 | doi =  }}
-*{{cite journal  | author=Traiffort E, Vizuete ML, Tardivel-Lacombe J, ''et al.'' |title=The guinea pig histamine H2 receptor: gene cloning, tissue expression and chromosomal localization of its human counterpart. |journal=Biochem. Biophys. Res. Commun. |volume=211 |issue= 2 |pages= 570-7 |year= 1995 |pmid= 7794271 |doi=  }}
+* {{cite journal | vauthors = Murakami H, Sun-Wada GH, Matsumoto M, Nishi T, Wada Y, Futai M | title = Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression | journal = FEBS Letters | volume = 451 | issue = 3 | pages = 327–31 | date = May 1999 | pmid = 10371214 | doi = 10.1016/S0014-5793(99)00618-3 }}
-*{{cite journal  | author=Orange PR, Heath PR, Wright SR, Pearson RC |title=Allelic variations of the human histamine H2 receptor gene. |journal=Neuroreport |volume=7 |issue= 7 |pages= 1293-6 |year= 1996 |pmid= 8817552 |doi=  }}
+* {{cite journal | vauthors = Wang LD, Wang M, Todisco A, Grand E, del Valle J | title = The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner | journal = American Journal of Physiology. Cell Physiology | volume = 278 | issue = 6 | pages = C1246-55 | date = Jun 2000 | pmid = 10837353 | doi = 10.1152/ajpcell.2000.278.6.c1246 }}
-*{{cite journal  | author=Elenkov IJ, Webster E, Papanicolaou DA, ''et al.'' |title=Histamine potently suppresses human IL-12 and stimulates IL-10 production via H2 receptors. |journal=J. Immunol. |volume=161 |issue= 5 |pages= 2586-93 |year= 1998 |pmid= 9725260 |doi=  }}
+* {{cite journal | vauthors = Suh BC, Lee H, Jun DJ, Chun JS, Lee JH, Kim KT | title = Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells | journal = Journal of Immunology | volume = 167 | issue = 3 | pages = 1663–71 | date = Aug 2001 | pmid = 11466390 | doi = 10.4049/jimmunol.167.3.1663 }}
-*{{cite journal  | author=Murakami H, Sun-Wada GH, Matsumoto M, ''et al.'' |title=Human histamine H2 receptor gene: multiple transcription initiation and tissue-specific expression. |journal=FEBS Lett. |volume=451 |issue= 3 |pages= 327-31 |year= 1999 |pmid= 10371214 |doi=  }}
+* {{cite journal | vauthors = Brew OB, Sullivan MH | title = Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy | journal = Inflammation Research | volume = 50 | issue = 9 | pages = 449–52 | date = Sep 2001 | pmid = 11603849 | doi = 10.1007/PL00000269 }}
-*{{cite journal  | author=Wang LD, Wang M, Todisco A, ''et al.'' |title=The human histamine H(2) receptor regulates c-jun and c-fos in a differential manner. |journal=Am. J. Physiol., Cell Physiol. |volume=278 |issue= 6 |pages= C1246-55 |year= 2000 |pmid= 10837353 |doi=  }}
+* {{cite journal | vauthors = Shayo C, Fernandez N, Legnazzi BL, Monczor F, Mladovan A, Baldi A, Davio C | title = Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases | journal = Molecular Pharmacology | volume = 60 | issue = 5 | pages = 1049–56 | date = Nov 2001 | pmid = 11641433 | doi =  }}
-*{{cite journal  | author=Suh BC, Lee H, Jun DJ, ''et al.'' |title=Inhibition of H2 histamine receptor-mediated cation channel opening by protein kinase C in human promyelocytic cells. |journal=J. Immunol. |volume=167 |issue= 3 |pages= 1663-71 |year= 2001 |pmid= 11466390 |doi=  }}
+* {{cite journal | vauthors = Tanimoto A, Murata Y, Nomaguchi M, Kimura S, Arima N, Xu H, Hamada T, Sasaguri Y | title = Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells | journal = FEBS Letters | volume = 508 | issue = 3 | pages = 345–9 | date = Nov 2001 | pmid = 11728449 | doi = 10.1016/S0014-5793(01)03073-3 }}
-*{{cite journal  | author=Brew OB, Sullivan MH |title=Localisation of mRNAs for diamine oxidase and histamine receptors H1 and H2, at the feto-maternal interface of human pregnancy. |journal=Inflamm. Res. |volume=50 |issue= 9 |pages= 449-52 |year= 2002 |pmid= 11603849 |doi=  }}
+* {{cite journal | vauthors = Gutzmer R, Langer K, Lisewski M, Mommert S, Rieckborn D, Kapp A, Werfel T | title = Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells | journal = The Journal of Allergy and Clinical Immunology | volume = 109 | issue = 3 | pages = 524–31 | date = Mar 2002 | pmid = 11898002 | doi = 10.1067/mai.2002.121944 }}
-*{{cite journal  | author=Shayo C, Fernandez N, Legnazzi BL, ''et al.'' |title=Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases. |journal=Mol. Pharmacol. |volume=60 |issue= 5 |pages= 1049-56 |year= 2001 |pmid= 11641433 |doi=  }}
+* {{cite journal | vauthors = Esbenshade TA, Kang CH, Krueger KM, Miller TR, Witte DG, Roch JM, Masters JN, Hancock AA | title = Differential activation of dual signaling responses by human H1 and H2 histamine receptors | journal = Journal of Receptor and Signal Transduction Research | volume = 23 | issue = 1 | pages = 17–31 | date = Feb 2003 | pmid = 12680587 | doi = 10.1081/RRS-120018758 }}
-*{{cite journal  | author=Tanimoto A, Murata Y, Nomaguchi M, ''et al.'' |title=Histamine increases the expression of LOX-1 via H2 receptor in human monocytic THP-1 cells. |journal=FEBS Lett. |volume=508 |issue= 3 |pages= 345-9 |year= 2001 |pmid= 11728449 |doi=  }}
-*{{cite journal  | author=Gutzmer R, Langer K, Lisewski M, ''et al.'' |title=Expression and function of histamine receptors 1 and 2 on human monocyte-derived dendritic cells. |journal=J. Allergy Clin. Immunol. |volume=109 |issue= 3 |pages= 524-31 |year= 2002 |pmid= 11898002 |doi=  }}
-*{{cite journal  | author=Strausberg RL, Feingold EA, Grouse LH, ''et al.'' |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899-903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899 }}
-*{{cite journal  | author=Esbenshade TA, Kang CH, Krueger KM, ''et al.'' |title=Differential activation of dual signaling responses by human H1 and H2 histamine receptors. |journal=J. Recept. Signal Transduct. Res. |volume=23 |issue= 1 |pages= 17-31 |year= 2003 |pmid= 12680587 |doi=  }}
-}}
 {{refend}}
-==External links==
+== External links ==
-*[http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2305 IUPHAR GPCR Database - H<sub>2</sub> Histamine Receptor]
+* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2305 | title = Histamine Receptors: H<sub>2</sub> | accessdate = | author = | authorlink = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }}
-*{{MeshName|H2+receptors}}
+* {{MeshName|H2+receptors}}
-{{membrane-protein-stub}}
 {{NLM content}}
 {{G protein-coupled receptors}}
-[[Category:G protein coupled receptors]]
+{{Histaminergics}}
-{{WikiDoc Sources}}
+[[Category:Histamine receptors]]

v t e Histamine receptor modulators
H₁	Agonists: 2-Pyridylethylamine Betahistine Histamine HTMT L-Histidine UR-AK49 Antagonists: First-generation: 4-Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine (benztropine) Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorphenamine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cloperastine Cyclizine Cyproheptadine Dacemazine Decloxizine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etodroxizine Etybenzatropine (ethylbenztropine) Etymemazine Fenethazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Medrylamine Mepyramine (pyrilamine) Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Orphenadrine Oxatomide Oxomemazine Perlapine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine Second/third-generation: Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Desloratadine Dorastine Ebastine Efletirizine Emedastine Epinastine Fexofenadine Flezelastine Ketotifen Latrepirdine Levocabastine Levocetirizine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Pibaxizine Piclopastine Quifenadine (phencarol) Rocastine Rupatadine Setastine Sequifenadine (bicarphen) Talastine Temelastine Terfenadine Vapitadine Zepastine Others: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, RP-5063, ziprasidone, zotepine) Phenylpiperazine antidepressants (e.g., hydroxynefazodone, nefazodone, trazodone, triazoledione) Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline) Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine) Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene) Unknown/unsorted: Azanator Belarizine Elbanizine Flotrenizine GSK1004723 Napactadine Tagorizine Trelnarizine Trenizine
H₂	Agonists: Amthamine Betazole Dimaprit Histamine HTMT Impromidine L-Histidine UR-AK49 Antagonists: Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Isolamtidine Lafutidine Lamtidine Lavoltidine (loxtidine) Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine (quisultidine) Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine Zolantidine
H₃	Agonists: α-Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine L-Histidine Methimepip Proxyfan Antagonists: A-349,821 A-423,579 ABT-239 ABT-652 AZD5213 Bavisant Betahistine Burimamide Ciproxifan Clobenpropit Conessine Enerisant GSK-189,254 Impentamine Iodophenpropit Irdabisant JNJ-5207852 MK-0249 NNC 38-1049 PF-03654746 Pitolisant SCH-79687 Thioperamide VUF-5681
H₄	Agonists: 4-Methylhistamine α-Methylhistamine Histamine L-Histidine OUP-16 VUF-8430 Antagonists: JNJ-7777120 Mianserin Seliforant Thioperamide Toreforant VUF-6002
See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake inhibitors

Histamine H2 receptor: Difference between revisions

Latest revision as of 20:21, 13 January 2018

Contents

Function

Tissue distribution

Physiological responses

See also

References

Further reading

External links

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