Neurosteroid Modulation of GABAA Receptor Function by IndependentAction at Multiple Specific Binding Sites Article Swipe
Lei Wang
,
Douglas F. Covey
,
Gustav Akk
,
Alex S. Evers
·
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.2174/1570159x19666211202150041
YOU?
·
· 2021
· Open Access
·
· DOI: https://doi.org/10.2174/1570159x19666211202150041
: Neurosteroids are endogenous modulators of GABAA receptors that mediate anxiety, pain, mood and arousal. The 3-hydroxyl epimers, allopregnanolone (3α-OH) and epiallopregnanolone (3β-OH) are both prevalent in the mammalian brain and produce opposite effects on GABAA receptor function, acting as positive and negative allosteric modulators, respectively. This Perspective provides a model to explain the actions of 3α-OH and 3β-OH neurosteroids. The model is based on evidence that the neurosteroid epimers bind to an overlapping subset of specific sites on GABAA receptors, with their net functional effect on channel gating being the sum of their independent effects at each site.
Related Topics
Concepts
Neuroactive steroid
Allopregnanolone
GABAA receptor
Allosteric regulation
Pregnanolone
GABAA-rho receptor
Allosteric modulator
Receptor
Neuroscience
Gating
Chemistry
Pharmacology
Biology
Biochemistry
Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.2174/1570159x19666211202150041
- OA Status
- green
- Cited By
- 12
- References
- 33
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3215797441
All OpenAlex metadata
Raw OpenAlex JSON
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https://openalex.org/W3215797441Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.2174/1570159x19666211202150041Digital Object Identifier
- Title
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Neurosteroid Modulation of GABAA Receptor Function by IndependentAction at Multiple Specific Binding SitesWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2021Year of publication
- Publication date
-
2021-12-03Full publication date if available
- Authors
-
Lei Wang, Douglas F. Covey, Gustav Akk, Alex S. EversList of authors in order
- Landing page
-
https://doi.org/10.2174/1570159x19666211202150041Publisher landing page
- Open access
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YesWhether a free full text is available
- OA status
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greenOpen access status per OpenAlex
- OA URL
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https://www.ncbi.nlm.nih.gov/pmc/articles/9881108Direct OA link when available
- Concepts
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Neuroactive steroid, Allopregnanolone, GABAA receptor, Allosteric regulation, Pregnanolone, GABAA-rho receptor, Allosteric modulator, Receptor, Neuroscience, Gating, Chemistry, Pharmacology, Biology, BiochemistryTop concepts (fields/topics) attached by OpenAlex
- Cited by
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12Total citation count in OpenAlex
- Citations by year (recent)
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2025: 3, 2024: 7, 2023: 2Per-year citation counts (last 5 years)
- References (count)
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33Number of works referenced by this work
- Related works (count)
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10Other works algorithmically related by OpenAlex
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