Histaminski H1 receptor

Histamine receptor H1
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
Entrez	3269
Ensembl	ENSG00000196639
UniProt	P35367
RefSeq (mRNA)	NM_000861.3
RefSeq (protein)	NP_000852.1
Lokacija (UCSC)	Chr 3:; 11.18 - 11.31 Mb
PubMed pretraga	[1]

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]

Reference

^ 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 (2011). „Structure of the human histamine H1 receptor complex with doxepin”. Nature. 475 (7354): 65—70. PMID 21697825. doi:10.1038/nature10236.

Literatura

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SS, Braman (1987). „Histamine receptors in the lung.”. N Engl Reg Allergy Proc. 8 (2): 116—20. PMID 2886904. doi:10.2500/108854187778994446.
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. PMID 2891264. doi:10.1007/BF01968814.
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. PMID 7925364. doi:10.1111/j.1432-1033.1994.00489.x.
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. PMID 8003029. doi:10.1006/bbrc.1994.1786.
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. PMID 8280179. doi:10.1006/bbrc.1993.2662.
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. PMID 8666296. doi:10.1016/0378-1119(96)00036-4.
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. PMID 10569698. doi:10.1016/S0165-2478(99)00126-1.
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. PMID 10818238. doi:10.1016/S0014-5793(00)01560-X.
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. PMID 10973974. doi:10.1074/jbc.M006480200.
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. doi:10.1007/PL00000269.
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. doi:10.1067/mai.2002.121944.
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. PMID 11994709. doi:10.1067/mai.2002.124044.

Vidi još

Antihistaminik – antagonist H₁ receptora

Spoljašnje veze

„Histamine Receptors: H₁”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 03. 03. 2016. г.

[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 (2011). „Structure of the human histamine H1 receptor complex with doxepin”. Nature. 475 (7354): 65—70. PMID 21697825. doi:10.1038/nature10236.

[1]