Histaminski H1 receptor

H₁ receptor je histaminski receptor iz familije rodopsinu sličnih G protein spregnutih receptora. Ovaj receptor, koji aktivira biogeni amin histamin, je izražen širom tela, u glatkim mišićima, vaskularnim endotelnim ćelijama, u srcu, i u centralnom nervnom sistemu. H₁ receptor je spregnut sa intracelularnim G proteinom (G_q) koji aktivira signalni put fosfolipaze C i fosfatidilinozitola (PIP2). Antihistamini koji deluju na ovaj receptor se koriste kao lekovi protiv alergije. Kristalna struktura receptora je određena.^[1]

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Histamine receptor H1
Histaminski H1 receptor u kompleksu sa doksepinom (3RZE)
Dostupne strukture
3RZE
Identifikatori
Simboli	HRH1; H1-R; hisH1
Vanjski ID	OMIM: 600167 MGI: 107619 HomoloGene: 668 IUPHAR: H1 GeneCards: HRH1 Gene
Ontologija gena Molekularna funkcija • aktivnost prenosa signala • receptorska aktivnost • aktivnost G-protein spregnutog receptora • aktivnost histaminskog receptora • vezivanje histamina Celularna komponenta • membranska frakcija • nukleus • nukleolus • citoplazma • ćelijska membrana • integralno sa ćelijskom membranom Biološki proces • inflamatorni respons • signalni put G-protein spregnutog receptora • aktivacija fosfolipaze C signalnim putom G-protein spregnutog receptora posredstvom IP3 sekundarnog glasnika • sinaptička transmisija • respons na gravitaciju • negativna regulacija steroidnog biosintetičkog procesa • positivna regulacija biosintetičkog procesa azot oksida • positivna regulacija vazokonstrikcije
Pregled RNK izražavanja
podaci
Ortolozi
Vrsta	Čovek	Miš
Entrez	3269	15465
Ensembl	ENSG00000196639	ENSMUSG00000053004
UniProt	P35367	P70174
RefSeq (mRNA)	NM_000861.3	NM_001252642.1
RefSeq (protein)	NP_000852.1	NP_001239571.1
Lokacija (UCSC)	Chr 3: 11.18 - 11.31 Mb	Chr 6: 114.35 - 114.43 Mb
PubMed pretraga

Reference

1. Tatsuro Shimamura, Mitsunori Shiroishi, Simone Weyand, Hirokazu Tsujimoto, Graeme Winter, Vsevolod Katritch, Ruben Abagyan, Vadim Cherezov, Wei Liu, Gye Won Han, Takuya Kobayashi, Raymond C. Stevens & So Iwata (July 2011). „Structure of the human histamine H1 receptor complex with doxepin”. Nature 475 (7354): 65–70. DOI:10.1038/nature10236. PMID 21697825.

Literatura

• Mitsuchashi M, Payan DG (1989). „Molecular and cellular analysis of histamine H1 receptors on cultured smooth muscle cells.”. J. Cell. Biochem. 40 (2): 183–92. DOI:10.1002/jcb.240400207. PMID 2670975.
• Braman SS (1987). „Histamine receptors in the lung.”. N Engl Reg Allergy Proc 8 (2): 116–20. DOI:10.2500/108854187778994446. PMID 2886904.
• 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.
• Holden CA, Chan SC, Norris S, Hanifin JM (1988). „Histamine induced elevation of cyclic AMP phosphodiesterase activity in human monocytes.”. Agents Actions 22 (1–2): 36–42. DOI:10.1007/BF01968814. PMID 2891264.
• Moguilevsky N, Varsalona F, Noyer M, et al. (1994). „Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene”. Eur. J. Biochem. 224 (2): 489–95. DOI:10.1111/j.1432-1033.1994.00489.x. PMID 7925364.
• Fukui H, Fujimoto K, Mizuguchi H, et al. (1994). „Molecular cloning of the human histamine H1 receptor gene”. Biochem. Biophys. Res. Commun. 201 (2): 894–901. DOI:10.1006/bbrc.1994.1786. PMID 8003029.
• Le Coniat M, Traiffort E, Ruat M, et al. (1994). „Chromosomal localization of the human histamine H1-receptor gene”. Hum. Genet. 94 (2): 186–8. PMID 8045566.
• De Backer MD, Gommeren W, Moereels H, et al. (1994). „Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor”. Biochem. Biophys. Res. Commun. 197 (3): 1601–8. DOI:10.1006/bbrc.1993.2662. PMID 8280179.
• Hishinuma S, Young JM (1996). „Characteristics of the binding of [3H-mepyramine to intact human U373 MG astrocytoma cells: evidence for histamine-induced H1-receptor internalisation”]. Br. J. Pharmacol. 116 (6): 2715–23. PMC 1909113. PMID 8590995.
• Max SI, Chowdhury BA, Fraser CM (1996). „Sequence analysis of the 5'-untranslated region of the human H1 histamine receptor-encoding gene”. Gene 171 (2): 309–10. DOI:10.1016/0378-1119(96)00036-4. PMID 8666296.
• De Backer MD, Loonen I, Verhasselt P, et al. (1998). „Structure of the human histamine H1 receptor gene”. Biochem. J. 335 (3): 663–70. PMC 1219830. PMID 9794809.
• Horváth BV, Szalai C, Mándi Y, et al. (1999). „Histamine and histamine-receptor antagonists modify gene expression and biosynthesis of interferon gamma in peripheral human blood mononuclear cells and in CD19-depleted cell subsets”. Immunol. Lett. 70 (2): 95–9. DOI:10.1016/S0165-2478(99)00126-1. PMID 10569698.
• Wang KY, Arima N, Higuchi S, et al. (2000). „Switch of histamine receptor expression from H2 to H1 during differentiation of monocytes into macrophages”. FEBS Lett. 473 (3): 345–8. DOI:10.1016/S0014-5793(00)01560-X. PMID 10818238.
• Oda T, Morikawa N, Saito Y, et al. (2001). „Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes”. J. Biol. Chem. 275 (47): 36781–6. DOI:10.1074/jbc.M006480200. PMID 10973974.
• 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.
• 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.
• Idzko M, la Sala A, Ferrari D, et al. (2002). „Expression and function of histamine receptors in human monocyte-derived dendritic cells”. J. Allergy Clin. Immunol. 109 (5): 839–46. DOI:10.1067/mai.2002.124044. PMID 11994709.

Povezano

• Antihistaminik – antagonist H₁ receptora

Spoljašnje veze

• „Histamine Receptors: H₁”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-03-03.