The DOI matches its Crossref record; 123 of the 123 references it cites were found in a registry or an index.
Neurosteroids: endogenous regulators of the GABAA receptor
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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“Allopregnanolone is a potent allosteric modulator of GABAA, while 5α-pregnane-3α,20α-diol is less neuroactive”
From Role of aldo-keto reductase family 1 (AKR1) enzymes in human steroid metabolism (2014) · cites this paper as [42]
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Cites
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Is there more to gaba than synaptic inhibition?
Owens, D. F., & Kriegstein, A. R. (2002) · Nature reviews. Neuroscience · doi:10.1038/nrn919 · Cited by 1,172
Receptor trafficking and synaptic plasticity
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Research works printed but not linked: 4
- 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).
- 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).
- 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).
- 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).
Cited by
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Rupprecht, R., Papadopoulos, V., Rammes, G., Baghai, T. C., Fan, J., Akula, N., Groyer, G., Adams, D., & Schumacher, M. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd3295 · Cited by 930
Structure, Function, and Modulation of GABAA Receptors
Sigel, E., & Steinmann, M. E. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.r112.386664 · Cited by 819
Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites
Hosie, A. M., Wilkins, M. E., da Silva, H. M. A., & Smart, T. G. (2006) · Nature · doi:10.1038/nature05324 · Cited by 752
Crystal structure of a human GABAA receptor
Miller, P. S., & Aricescu, A. R. (2014) · Nature · doi:10.1038/nature13293 · Cited by 734
Extrasynaptic GABAA Receptors: Their Function in the CNS and Implications for Disease
Brickley, S. G., & Módy, I. (2012) · Neuron · doi:10.1016/j.neuron.2011.12.012 · Cited by 695
Metadata
- 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
- 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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