ArticleMolecular pharmacology2011
Occupation of either site for the neurosteroid allopregnanolone potentiates the opening of the GABAA receptor induced from either transmitter binding site.
Article in Molecular pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
What it found
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Who cites it
24 citing papers in PubMed, 30 citations in OpenAlex.
- The relationship between apparent potentiation and the magnitude of the control response.The Journal of general physiology · 2026Article
- A bupropion modulatory site in the Gloeobacter violaceus ligand-gated ion channel.Biophysical journal · 2024Article
- Potentiation of the GABABiophysical journal · 2024Article
- Structural insights into opposing actions of neurosteroids on GABANature communications · 2023Article
- Activation of the Rat α1β2ε GABABiomolecules · 2022Article
- Intrasubunit and Intersubunit Steroid Binding Sites Independently and Additively MediateMolecular pharmacology · 2021Article
- Steady-State Activation and Modulation of the ConcatemericMolecular pharmacology · 2019Article
- Multiple functional neurosteroid binding sites on GABAA receptors.PLoS biology · 2019Article
- Analysis of GABAMolecular pharmacology · 2019Article
- Application of the Co-Agonist Concerted Transition Model to Analysis of GABAA Receptor Properties.Current neuropharmacology · 2019Review
- Enhanced GABAergic actions resulting from the coapplication of the steroid 3α-hydroxy-5α-pregnane-11,20-dione (alfaxalone) with propofol or diazepam.Scientific reports · 2018Article
- High Constitutive Activity Accounts for the Combination of Enhanced Direct Activation and Reduced Potentiation in Mutated GABAMolecular pharmacology · 2018Article
- GABA Type A Receptor Activation in the Allosteric Coagonist Model Framework: Relationship between ECMolecular pharmacology · 2018Article
- Propofol Is an Allosteric Agonist with Multiple Binding Sites on Concatemeric Ternary GABAMolecular pharmacology · 2018Article
- The Actions of Drug Combinations on the GABAMolecular pharmacology · 2017Article
- Cerebellar Changes in Guinea Pig Offspring Following Suppression of Neurosteroid Synthesis During Late Gestation.Cerebellum (London, England) · 2017Article
- Etomidate produces similar allosteric modulation in α1β3δ and α1β3γ2L GABA(A) receptors.British journal of pharmacology · 2014Article
- Neurosteroid interactions with synaptic and extrasynaptic GABA(A) receptors: regulation of subunit plasticity, phasic and tonic inhibition, and neuronal network excitability.Psychopharmacology · 2013Review
- Article
- A neurosteroid potentiation site can be moved among GABAA receptor subunits.The Journal of physiology · 2012Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Potentiating neuroactive steroids are potent and efficacious modulators of the GABA(A) receptor that act by allosterically enhancing channel activation elicited by GABA. Steroids interact with the membrane-spanning domains of the α subunits of the receptor, whereas GABA binds to pockets in the interfaces between β and α subunits. Steroid interaction with a single site is known to be sufficient to produce potentiation, but it is not clear whether effects within the same β-α pair mediate potentiation. Here, we have investigated whether the sites for GABA and steroids are functionally linked (i.e., whether the occupancy of a steroid site selectively affects activation elicited by GABA binding to the transmitter binding site within the same β-α pair). For that, we used receptors formed of mutated concatenated subunits to selectively eliminate one of the two GABA sites and one of the two steroid sites. The data demonstrate that receptors containing a single functional GABA site are potentiated by the neurosteroid allopregnanolone regardless of whether the steroid interacts with the α subunit from the same or the other β-α pair. We conclude that steroids potentiate the opening of the GABA(A) receptor induced by either agonist binding site.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.