Cited by 1,159Neuroscience and Neuropharmacology ResearchPharmacological Receptor Mechanisms and EffectsReceptor Mechanisms and Signaling

Neurosteroids: endogenous regulators of the GABAA receptor

Belelli, Delia, Lambert, Jeremy J.·2005·Nature reviews. Neuroscience

Abstract

GABA(A) (gamma-aminobutyric acid type A) receptors mediate most of the 'fast' synaptic inhibition in the mammalian brain and are targeted by many clinically important drugs. Certain naturally occurring pregnane steroids can potently and specifically enhance GABA(A) receptor function in a nongenomic (direct) manner, and consequently have anxiolytic, analgesic, anticonvulsant, sedative, hypnotic and anaesthetic properties. These steroids not only act as remote endocrine messengers, but also can be synthesized in the brain, where they modify neuronal activity locally by modulating GABA(A) receptor function. Such 'neurosteroids' can influence mood and behaviour in various physiological and pathophysiological situations, and might contribute to the behavioural effects of psychoactive drugs.

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Crossref · 10.1038/nrn1703

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Research works printed but not linked: 4

  1. Melcangi, R. C., Magnaghi, V., Galbiati, M. & Martini, L. in Neurosteroid and Brain Function (eds Biggio, G. & Purdy, R. H.) 146–176 (Academic, San Diego, 2001).
  2. Sundstrom-Poromaa, I. in Neurosteroid Effects in the Central Nervous System: the Role of the GABAA Receptor (ed. Smith, S. S.) 291–304 (CRC, New York, 2004).
  3. Mtchedlishvili, Z. & Kapur, J. in Neurosteroid Effects in the Central Nervous System: the Role of the GABAA Receptor (ed. Smith, S. S.) 305–316 (CRC, New York, 2004).
  4. Gibbs, T. T. & Farb, D. H. in Neurosteroid Effects in the Central Nervous System: the Role of the GABAA Receptor (ed. Smith S. S.) 339–358 (CRC, New York, 2004).

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Authors
Belelli, D., & Lambert, J. J.
Affiliations
University of Dundee (GB)
Corresponding author
Lambert, Jeremy J.
Venue
Nature reviews. Neuroscience
Published
2005-06-15
Volume
6
Issue
7
Pages
565-575
ISSN
  • 1471-003X (ISSN-L)
  • 1471-0048
OpenAlex
W2070510853
Cited by
1,159
References
123
Citations by year
2026: 32 · 2025: 40 · 2024: 45 · 2023: 51 · 2022: 49 · 2021: 52 · 2020: 53 · 2019: 49 · 2018: 54 · 2017: 43 · 2016: 57 · 2015: 57 · 2014: 71 · 2013: 64 · 2012: 55
FWCI
5.43
Type
journal article
Language
en
Open access
closed
Locations
  • Nature reviews. Neuroscience (publishedVersion)
  • PubMed (publishedVersion)
  • Discovery Research Portal (University of Dundee) (publishedVersion)
Topics
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Pharmacological Receptor Mechanisms and Effects
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords
neurosteroids, GABAA receptor, pregnane steroids, non-genomic steroid action, synaptic inhibition, anxiolytic effects, anticonvulsant activity, anesthesia, psychoactive substances
MeSH terms
Animals, Brain, Humans, Models, Biological, Neural Inhibition, Synaptic Transmission, Pregnanes, Receptors, GABA-A, Antipsychotic Agents, Mood Disorders

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