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Encyclopedia > Histamine H1 receptor

Histamine receptor H1
Identifiers
Symbol(s) HRH1; H1-R; hisH1
External IDs OMIM: 600167 MGI: 107619 Homologene: 668
RNA expression pattern

Look up Hugo in Wiktionary, the free dictionary. ... The Mouse Genome Informatics (MGI) website is run by The Jackson Laboratory. ... HomoloGene[1], a tool of the National Center for Biotechnology Information (NCBI)[2], is a system for automated detection of homologs (similarity attributable to descent from a common ancestor) among the annotated genes of several completely sequenced eukaryotic genomes. ... The Gene Ontology, or GO, project can be broadly split into two parts. ...



More reference expression data
Orthologs
Human Mouse
Entrez 3269 15465
Ensembl ENSG00000196639 ENSMUSG00000053004
Uniprot P35367 P70174
Refseq NM_000861 (mRNA)
NP_000852 (protein)		 NM_008285 (mRNA)
NP_032311 (protein)
Location Chr 3: 11.28 - 11.28 Mb Chr 6: 114.36 - 114.45 Mb
Pubmed search [1] [2]


The H1 receptor is a histamine receptor, and thus an important target for clinically important drugs, and is likely one of the most important receptors for modulating mammalian circadian cycles. The Entrez logo The Entrez Global Query Cross-Database Search System allows access to databases at the National Center for Biotechnology Information (NCBI) website. ... Ensembl is a bioinformatics research project aiming to develop a software system which produces and maintains automatic annotation on selected eukaryotic genomes. It is run in a collaboration between the Wellcome Trust Sanger Institute and the European Bioinformatics Institute, an outstation of the European Molecular Biology Laboratory. ... UniProt is the universal protein database, a central repository of protein data created by combining Swiss-Prot, TrEMBL and PIR. This makes it the worlds most comprehensive resource on protein information. ... Medline is a comprehensive literature database of life sciences and biomedical information. ... The histamine receptors are a class of G-protein coupled receptors with histamine as their endogenous ligand. ... The circadian rhythm is a name given to the internal body clock that regulates the (roughly) 24 hour cycle of biological processes in animals and plants. ...


Histamine H1 receptor are metabotropic G-protein-coupled receptors expressed throughout the body, specifically in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. The H1 receptor is linked to an intracellular G-protein (Gq) which activates phospholipase C and the phosphatidylinositol (PIP2) signalling pathway. This article or section does not cite any references or sources. ... Metabotropic receptor is a subtype of membrane receptors at the surface or in vesicles of eukaryotic cells. ... The seven transmembrane α-helix structure of a G-protein-coupled receptor. ... Smooth muscle is a type of non-striated muscle, found within the walls of hollow organs; such as blood vessels, bladders, uteri. ... The endothelium is the layer of thin, flat cells that lines the interior surface of blood vessels, forming an interface between circulating blood in the lumen and the rest of the vessel wall. ... A diagram showing the CNS: 1. ... G-proteins, short for guanine nucleotide binding proteins, are a family of proteins involved in second messenger cascades. ... Phospholipase C is a key enzyme in phosphatidylinositol (PIP2) metabolism and lipid signaling pathways. ... Chemical structure of sn-1-stearoyl-2-arachidonoyl phosphatidylinositol Phosphatidylinositol (abbreviated PtdIns, or PI) is a minor phospholipid component of eukaryotic cell membranes. ...

Contents

H1 receptor and inflammation

The production of prostaglandin E2 synthase induces the release of histamine from neurons, consequentially causing systemic vasodilation, along with increased cell permeability due to the its action on H1 receptors.


Neurophysiology

Histamine H1 receptors are activated by endogenous histamine, which is released by neurons which have their cell bodies in the tuberomamillary nucleus of the hypothalamus. The histaminergic neurons of the tuberomammillary nucleus become active during the 'wake' cycle, firing at approximately 2Hz; during slow wave sleep this firing rate drops to approximately 0.5Hz. Finally during REM sleep, histaminergic neurons stop firing all together. It has been reported that histaminergic neurons have the most wake-selective firing pattern of all known neuronal types.[1] The hypothalamus links the nervous system to the endocrine system via the pituitary gland (hypophysis). ... Rapid eye movement (REM) sleep is the normal stage of sleep characterized by rapid movements of the eyes. ...


In the cortex, activation of H1 receptors leads to inhibition of cell membrane potassium channels. This depolarizes the neurons and increases the resistance of the neuronal cell membrane, bringing the cell closer to its firing threshold and increasing the excitatory voltage produced by a given excitatory current. H1 receptor antagonists, or antihistamines, produce drowsiness because they oppose this action, reducing neuronal excitation.[2] For other uses, see Cortex. ... In cell biology, potassium channels are the most common type of ion channel. ... An antihistamine is a drug which serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions, through action at the histamine receptor. ...


H1-receptor antagonists

see Antihistamine - H1-receptor antagonists An H1 antihistamine is a histamine antagonist which serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions, through action at the H1 receptor. ...


References

  1. ^ Passani, M. B., Lin, J. S., Hancock, A., Crochet, S., Blandina, P., 2004. The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders. Trends Pharmacol Sci 25, 618-625.
  2. ^ Reiner P. B., Kamondi A., 1994. Mechanisms of antihistamine-induced sedation in the human brain: H1 receptor activation reduces a background leakage potassium current. Neuroscience 59(3), 579-88.

Further reading

  • 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. 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. 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. 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. 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. 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. 
  • De Backer MD, Loonen I, Verhasselt P, et al. (1998). "Structure of the human histamine H1 receptor gene.". Biochem. J. 335 ( Pt 3): 663-70. 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. 
  • 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. 
  • 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. 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. 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. PMID 11994709. 

A digital object identifier (or DOI) is a standard for persistently identifying a piece of intellectual property on a digital network and associating it with related data, the metadata, in a structured extensible way. ... A digital object identifier (or DOI) is a standard for persistently identifying a piece of intellectual property on a digital network and associating it with related data, the metadata, in a structured extensible way. ... A digital object identifier (or DOI) is a standard for persistently identifying a piece of intellectual property on a digital network and associating it with related data, the metadata, in a structured extensible way. ...

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Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1A, α1B, α1D, α2A, α2B, α2C, β1, β2, β3) - 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 (LTB4, LTB4R2, Prostaglandin) - Endothelin (A, B) - Estrogen - Formyl peptide - Free fatty acid - FSH - Galanin - Ghrelin - Gonadotropin-releasing hormone - Histamine (H1, H2, H3, H4) - Kisspeptin - LHRH - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 8) - MAS1 - Melanocortin (1, 2, 3, 4, 5) - MCHR - Melatonin - Motilin - Neuromedin (B, U) - Neuropeptide (B/W, FF, S, Y) - Neurotensin - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory (TAAR) - Opsin (1SW) - Orexin - Oxytocin - PAF - Prokineticin - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, P2Y12) - Relaxin - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (2A, 2B, 2C), 4, 5A, 6, 7) - SREB - Tachykinin (TACR1) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like Brain-specific angiogenesis inhibitor (1, 2, 3) - Calcitonin - CD97 - Corticotropin-releasing hormone (1, 2) - EMR - Glucagon (GR, GIPR, GLP1R, GLP2R) - Growth hormone releasing hormone - PACAPR1 - Parathyroid hormone (1, 2) - Secretin - Vasoactive intestinal peptide
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  Results from FactBites:
 
Histamine - Wikipedia, the free encyclopedia (499 words)
Histamine is a biogenic amine chemical involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
Histamine is synthesized by the decarboxylation of the amino acid histidine, a reaction catalyzed by the enzyme L-histidine decarboxylase.
Histamine is broken down by histamine-N-methyltransferase and diamine oxidase, and is also possibly taken up by a transporter.
HRH2 - Histamine H2 receptor (1001 words)
The effect of histamine, prometasin (the blocker of histamine H-1 receptor) and cimetidin (the blocker of histamine H-2 receptor) on the frequency of the isolated right atrium of rat was studied.
For this study, we investigated the effects of histamine on NADPH oxidase activity in human neutrophil granulocytes triggered by a lipoxin A4 receptor agonist [the hexapeptide Trp-Lys-Tyr-Met-Val-Met (WKYMVM), a formyl peptide receptor (FPR) agonist (the chemotactic tripeptide formylmethionyl-leucyl-phenylalanine (fMLF)) and an activator of protein kinase C (phorbol myristate acetate (PMA)].
HRH2 is a homologue of 5-HT7 (5-hydroxytryptamine receptor 1) from Drosophila melanogaster.
  More results at FactBites »

 

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