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Research ArticleJpet Miniseries: H3 Receptors

Histamine H3 Receptors and Sleep-Wake Regulation

Jian-Sheng Lin, Olga A. Sergeeva and Helmut L. Haas
Journal of Pharmacology and Experimental Therapeutics January 2011, 336 (1) 17-23; DOI: https://doi.org/10.1124/jpet.110.170134
Jian-Sheng Lin
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Olga A. Sergeeva
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Helmut L. Haas
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Abstract

The histaminergic system fulfills a major role in the maintenance of waking. Histaminergic neurons are located exclusively in the posterior hypothalamus from where they project to most areas of the central nervous system. The histamine H3 receptors are autoreceptors damping histamine synthesis, the firing frequency of histamine neurons, and the release of histamine from axonal varicosities. It is noteworthy that this action also extends to heteroreceptors on the axons of most other neurotransmitter systems, allowing a powerful control over multiple homeostatic functions. The particular properties and locations of histamine H3 receptors provide quite favorable attributes to make this a most promising target for pharmacological interventions of sleep and waking disorders associated with narcolepsy, Parkinson's disease, and other neuropsychiatric indications.

Footnotes

  • This work was supported by the European Community [Grant QLRT-2001-00826] (to H.L.H and J.-S.L.), the Deutsche Forschungsgemeinschaft [Grants SFB 575/3, SFB 575/8] (to H.L.H. and O.A.S.); and the Institut National de la Santé et Recherche Médicale (to J.-S.L).

  • Article, publication date, and citation information can be found at http://jpet.aspetjournals.org.

    doi:10.1124/jpet.110.170134.

  • ABBREVIATIONS:

    REM
    rapid eye movement
    DREM
    direct transition from wake to REM sleep
    SWS
    slow wave sleep
    CNS
    central nervous system
    SKF91488
    4-(N,N-dimethylamino)butylisothiourea
    BP2-94
    (R)-(−)-2-[[N-[1-(1H-imidazol-4-yl)-2-propyl]imino]phenylmethyl] phenol
    BF2.649
    1-{3-[3-(4-chlorophenyl)propoxy]propyl}piperidine hydrochloride
    GSK-189254
    6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide
    JNJ-5207852
    1-{3-[4-(piperidin-1-ylmethyl)phenoxy]propyl}piperidine
    ABT-239
    4-(2-{2-[(2R)-2-methylpyrrolidin-1-yl]ethyl}-benzofuran-5-yl)benzonitrile
    JNJ-10181457
    4-(3-(4-piperidin-1-ylbut-1-ynyl)benzyl)morpholine)
    PF-03654746
    (1R,3R)-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide.

  • Received May 20, 2010.
  • Accepted August 17, 2010.
  • Copyright © 2011 by The American Society for Pharmacology and Experimental Therapeutics
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In this issue

Journal of Pharmacology and Experimental Therapeutics: 385 (3)
Journal of Pharmacology and Experimental Therapeutics
Vol. 385, Issue 3
1 Jun 2023
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Research ArticleJpet Miniseries: H3 Receptors

Histamine H3 Receptors and Sleep-Wake Regulation

Jian-Sheng Lin, Olga A. Sergeeva and Helmut L. Haas
Journal of Pharmacology and Experimental Therapeutics January 1, 2011, 336 (1) 17-23; DOI: https://doi.org/10.1124/jpet.110.170134

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Research ArticleJpet Miniseries: H3 Receptors

Histamine H3 Receptors and Sleep-Wake Regulation

Jian-Sheng Lin, Olga A. Sergeeva and Helmut L. Haas
Journal of Pharmacology and Experimental Therapeutics January 1, 2011, 336 (1) 17-23; DOI: https://doi.org/10.1124/jpet.110.170134
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  • Article
    • Abstract
    • Sleep and Waking
    • Histamine's Role in Waking
    • Autoreceptors and Heteroreceptors
    • Histamine H3 Receptors
    • Mechanisms of H3 Receptor Actions
    • Sleep-Wake Disorders
    • H3 Receptors: Targets for Arousal Control and Treatment of Sleep-Wake Disorders
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Cited By...

More in this TOC Section

  • The Histamine H3 Receptor and Eating Behavior
  • H3 Receptors and Pain Modulation: Peripheral, Spinal, and Brain Interactions
  • Discovery of Histamine H3 Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease
Show more Jpet Miniseries: H3 Receptors

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