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Cited by 251Sleep and Wakefulness ResearchCircadian rhythm and melatoninNeuroscience of respiration and sleep

Histamine in the regulation of wakefulness

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Thakkar, Mahesh M.·2011·Sleep Medicine Reviews
DOI 10.1016/j.smrv.2010.06.004PMC PMC3016451
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Abstract

The histaminergic system is exclusively localized within the posterior hypothalamus with projection to almost all the major regions of the central nervous system. Strong and consistent evidence exist to suggest that histamine, acting via H₁ and/or H₃ receptor has a pivotal role in the regulation of sleep-wakefulness. Administration of histamine or H₁ receptor agonists induces wakefulness, whereas administration of H₁ receptor antagonists promotes sleep. The H₃ receptor functions as an auto-receptor and regulates the synthesis and release of histamine. Activation of H₃ receptor reduces histamine release and promotes sleep. Conversely, blockade of H₃ receptor promotes wakefulness. Histamine release in the hypothalamus and other target regions is highest during wakefulness. The histaminergic neurons display maximal activity during the state of high vigilance, and cease their activity during non-rapid eye movement (NREM) and rapid eye movement (REM) sleep. The cerebrospinal levels of histamine are reduced in diseased states where hypersomnolence is a major symptom. The histamine deficient L-histidine decarboxylase knockout (HDC KO) mice display sleep fragmentation and increased REM sleep during the light period along with profound wakefulness deficit at dark onset, and in novel environment. Similar results have been obtained when histamine neurons are lesioned. These studies strongly implicate the histaminergic neurons of the TMN to play a critical role in the maintenance of high vigilance state during wakefulness.

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  • In mammals, histamine modulates wakefulness and has diverse immune functions.

    “In mammals, histamine plays several roles in host physiology including modulating wakefulness (Thakkar, 2011) as well as a diverse array of immune functions.”

    From The Microbiota-Gut-Brain Axis (2019) · cites this paper as Thakkar, 2011

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Authors
Thakkar, M. M.
Affiliations
Harry S. Truman Memorial Veterans' Hospital (US)
Corresponding author
Thakkar, Mahesh M.
ORCID
Thakkar, Mahesh M.
Venue
Sleep Medicine Reviews
Publisher
Elsevier BV
Published
2011-02
Volume
15
Issue
1
Pages
65-74
ISSN
1087-0792 (ISSN-L)
DOI
10.1016/j.smrv.2010.06.004
PMC
PMC3016451
OpenAlex
W2011624554
Cited by
251
References
2
Citations by year
2026: 30 · 2025: 23 · 2024: 18 · 2023: 12 · 2022: 20 · 2021: 18 · 2020: 16 · 2019: 16 · 2018: 13 · 2017: 15 · 2016: 10 · 2015: 6 · 2014: 19 · 2013: 12 · 2012: 17
FWCI
6.47
Type
journal article
Language
en
Open access
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Sleep Medicine Reviews (publishedVersion)
  • PubMed (publishedVersion)
  • Europe PMC (PubMed Central) (acceptedVersion)
  • PubMed Central (acceptedVersion)
Funders
National Institute on Alcohol Abuse and Alcoholism (R21AA017472)
Topics
  • Life Sciences › Neuroscience › Cognitive Neuroscience › Sleep and Wakefulness Research
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Circadian rhythm and melatonin
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Neuroscience of respiration and sleep
Keywords
histamine, wakefulness, sleep-wake regulation, histaminergic system, posterior hypothalamus, histamine H1 receptor, histamine H3 receptor, histamine release, REM sleep, NREM sleep, sustained attention, hypersomnolence, histaminergic neurons
MeSH terms
Animals, Arousal, Histamine, Humans, Receptors, Cell Surface, Receptors, Histamine H1, Sleep, Sleep, REM, Wakefulness, Receptors, Neuropeptide, Mice, Knockout, Sleep Disorders, Intrinsic, Mice

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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

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