ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2009
Pregnanolone sulfate promotes desensitization of activated NMDA receptors.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
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Who cites it
54 citing papers in PubMed, 82 citations in OpenAlex.
- The positive allosteric modulator GNE-9278 increases gating, conductance, and CaNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Dynamic control of NMDA receptor CaProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Metabolic activation of flunitrazepam via nitroreduction mediated by aldo-keto reductase 1C3.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Experimentally Constrained Mechanistic and Data-Driven Models for Simulating NMDA Receptor Dynamics.Biomedicines · 2025Article
- Allosteric inhibition of NMDA receptors by low dose ketamine.Molecular psychiatry · 2025Article
- 5β-Dihydrosteroids: Formation and Properties.International journal of molecular sciences · 2024Review
- Estimating the CaMethods in molecular biology (Clifton, N.J.) · 2024Article
- Complex functional phenotypes of NMDA receptor disease variants.Molecular psychiatry · 2022Article
- Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.Pharmacological reviews · 2021Review
- Pitfalls of NMDA Receptor Modulation by Neuroactive Steroids. The Effect of Positive and Negative Modulation of NMDA Receptors in an Animal Model of Schizophrenia.Biomolecules · 2021Article
- Cross-subunit interactions that stabilize open states mediate gating in NMDA receptors.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Biosynthesis and signalling functions of central and peripheral nervous system neurosteroids in health and disease.Essays in biochemistry · 2020Review
- CaBiophysical journal · 2020Article
- Positive and Negative Allosteric Modulators of N-Methyl-d-aspartate (NMDA) Receptors: Structure-Activity Relationships and Mechanisms of Action.Journal of medicinal chemistry · 2019Review
- The NMDA receptor intracellular C-terminal domains reciprocally interact with allosteric modulators.Biochemical pharmacology · 2019Article
- Structure, function, and allosteric modulation of NMDA receptors.The Journal of general physiology · 2018Review
- Kinetic models for activation and modulation of NMDA receptor subtypes.Current opinion in physiology · 2018Article
- Calcium-engaged Mechanisms of Nongenomic Action of Neurosteroids.Current neuropharmacology · 2017Review
- Memantine and Ketamine Differentially Alter NMDA Receptor Desensitization.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2017Article
- NMDA Receptors in the Central Nervous System.Methods in molecular biology (Clifton, N.J.) · 2017Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Neurosteroids are potent neuromodulators which act in part by binding to and modifying the activity of neurotransmitter-gated channels. Pregnanolone sulfate (PAS) is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective in vivo. To delineate the mechanism of NMDA receptor inhibition by pregnanolone sulfate we used kinetic analyses of equilibrium single-channel currents recorded from individual GluN1/GluN2A receptors. Results show that PAS (0.1 mM) reduces single-channel open probability by 50% solely by increasing approximately 5-fold the mean time spent by receptors in closed conformations. From these data we derive a kinetic scheme that summarizes the effects of PAS on single channel kinetics, accounts for the PAS effects on macroscopic responses and leads us to propose that PAS inhibits NMDA receptor activity by shifting active receptors into desensitized conformations. These findings highlight the neurosteroid inhibitory site on NMDA receptors as a valuable therapeutic target against excitotoxic pathologies including acute and chronic neurodegeneration.
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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.