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Histamine H1 receptor

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The correct title of this article is Histamine H1 receptor. It appears incorrectly here because of technical restrictions.
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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.

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) that activates phospholipase C and the phosphatidylinositol (PIP2) signaling pathway.

Role in inflammationEdit

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

NeurophysiologyEdit

Histamine H1 receptors are activated by endogenous histamine, which is released by neurons that 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 2 Hz; during slow wave sleep; this firing rate drops to approximately 0.5 Hz. Finally, during REM sleep, histaminergic neurons stop firing altogether. It has been reported that histaminergic neurons have the most wake-selective firing pattern of all known neuronal types.[1]

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]

See also Edit

ReferencesEdit

  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 readingEdit


  • 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.
  • Braman SS (1987). Histamine receptors in the lung.. N Engl Reg Allergy Proc 8 (2): 116–20.
  • Hill SJ, Ganellin CR, Timmerman H, et al. (1997). International Union of Pharmacology. XIII. Classification of histamine receptors.. Pharmacol. Rev. 49 (3): 253–78.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.




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External linksEdit

  • Histamine Receptors: H1. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.




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