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

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Neurosteroids: endogenous regulators of the GABAA receptor

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

DOI 10.1038/nrn1703

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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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Authors: Belelli, D., & Lambert, J. J.
Affiliations: University of Dundee (GB)
Corresponding author: Lambert, Jeremy J.
ORCID: Belelli, Delia
Lambert, Jeremy J.
Venue: Nature reviews. Neuroscience
Publisher: Springer Science and Business Media LLC
Published: 2005-06-15
Volume: 6
Issue: 7
Pages: 565-575
ISSN: 1471-003X (ISSN-L)
1471-0048
DOI: 10.1038/nrn1703
OpenAlex: W2070510853
Semantic Scholar: 1e15686792dd96994a0bd1337b50f1e4448b7965
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
Licence: www.springer.com/tdm (tdm)
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 › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › 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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Neurosteroids: endogenous regulators of the GABAA receptor

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