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Pregnenolone sulfate block of GABAA receptors: mechanism and involvement of a residue in the M2 region of the α subunit
Open accessAbstract
Neurosteroids are produced in the brain, and can have rapid actions on membrane channels of neurons. Pregnenolone sulfate (PS) is a sulfated neurosteroid which reduces the responses of the [gamma]-aminobutyric acid A (GABA(A)) receptor. We analysed the actions of PS on single-channel currents from recombinant GABA(A) receptors formed from [alpha]1, [beta]2 and [gamma]2L subunits. Currents were elicited by a concentration of GABA eliciting a half-maximal response (50 microM) and a saturating concentration (1 mM). PS reduced the duration of clusters of single-channel activity at either concentration of GABA. PS had no discernable effect on rapid processes: no effects were apparent on channel opening and closing, nor on GABA affinity, and a rapidly recovering desensitised state was not affected. Instead, PS produced a slowly developing block which occurred at a similar rate for receptors with open or closed channels and with one or two bound GABA molecules. The rate of block was independent of membrane potential, implying that the charged sulfate moiety does not move through the membrane field. Change in a specific residue near the intracellular end of the channel lining portion of the [alpha]1 subunit had a major effect on the rate of block. Mutation of the residue [alpha]1 V256S reduced the rate of block by 30-fold. A mutation at the homologous position of the [beta]2 subunit ([beta]2 A252S) had no effect, nor did a complementary mutation in the [gamma]2L subunit ([gamma]2L S266A). It seems likely that this residue is involved in a conformational change underlying block by PS, instead of forming part of the binding site for PS.
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“In the work with inhibitory steroids and steroid analogues, it was also shown that a valine-to-serine mutation of the 2 0 residue of the a1-subunit M2 transmembrane domain (a1V256S) strongly diminished the ability of these compounds to block the GABA A receptor (Akk et al., 2001;Li et al., 2006).”
From The insecticide fipronil and its metabolite fipronil sulphone inhibit the rat α1β2γ2L GABAAreceptor (2008) · cites this paper as Akk et al., 2001
In the citing paper
“But in contrast to these drugs whose effect is drastically diminished in the a1V256S mutant receptor, the inhibitory actions of fipronil were little affected by the a1V256S mutation.”
From The insecticide fipronil and its metabolite fipronil sulphone inhibit the rat α1β2γ2L GABAAreceptor (2008) · cites this paper as Akk et al., 2001
In the citing paper
“The kinetic mechanism of action of fipronil is similar to that of an inhibitory neurosteroid, pregnenolone sulphate and some tricyclic neurosteroid analogues (Akk et al., 2001;Li et al., 2006).”
From The insecticide fipronil and its metabolite fipronil sulphone inhibit the rat α1β2γ2L GABAAreceptor (2008) · cites this paper as Akk et al., 2001
In the citing paper
“Thus, these findings may suggest a role for CA1 α1 GABAARs in memory consolidation, providing temporal and anatomical specificity to early reports that the amnestic effects of diazepam were abolished in α1 (H101R) mice, in which diazepam does not bind to α1GABAARs [63].”
From An emerging circuit pharmacology of GABAA receptors (2018) · cites this paper as [83]
In the citing paper
“Pregnenolone sulfate is a negative modulator of GABAARs including α1 GABAARs [83].”
From An emerging circuit pharmacology of GABAA receptors (2018) · cites this paper as [83]
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Metadata
- Authors
- Akk, G., Bracamontes, J., & Steinbach, J. H.
- Affiliations
- Washington University in St. Louis (US)
- Venue
- The Journal of Physiology
- Publisher
- Wiley
- Published
- 2001-05
- Volume
- 532
- Issue
- 3
- Pages
- 673-684
- ISSN
- 0022-3751 (ISSN-L)
- 1469-7793
- PMC
- PMC2278584
- OpenAlex
- W2145087907
- Cited by
- 137
- References
- 49
- Citations by year
- 2025: 3 · 2024: 6 · 2023: 11 · 2022: 2 · 2021: 4 · 2020: 6 · 2019: 4 · 2018: 3 · 2017: 3 · 2016: 3 · 2015: 1 · 2014: 6 · 2013: 6 · 2012: 4
- FWCI
- 2.96
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- The Journal of Physiology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institute of General Medical Sciences (P01GM047969, P01GM47969)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Keywords
- pregnenolone sulfate, neurosteroids, GABAA receptor, alpha1 subunit, single-channel currents, desensitization, conformational change, channel gating
- MeSH terms
- Binding Sites, Cell Line, Estranes, gamma-Aminobutyric Acid, Humans, Kidney, Ligands, Membrane Potentials, Nitriles, Pentobarbital, Piperidines, Pregnenolone, Receptors, GABA-A, Transfection, Ion Channel Gating, Mutagenesis, Patch-Clamp Techniques, GABA Agonists, GABA Modulators
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