Pregnanolone sulfate
Pregnanolone sulfate is an endogenous neurosteroid and NMDA receptor inhibitor. Pregnanolone sulfate exhibits stronger inhibition of tonically activated NMDA receptors (associated with excitotoxicity) than of phasically activated synaptic receptors. Pregnanolone sulfate enhances glutamate release. Pregnanolone sulfate can be used in research on excitotoxic neurodegenerative diseases.
For research use only. We do not sell to patients.
- CAS No.: 1477-67-4
- Formula: C21H34O5S
- Molecular Weight:398.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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Human Endogenous Metabolite |
NMDA Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
67 μM
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Inhibition of macroscopic NMDA receptor currents in HEK 293 cells expressing recombinant rat GluN1/GluN2A receptors by whole-cell patch-clamp recording using 1 mM glutamate and 0.1 mM glycine at -70 mV.
Inhibition of macroscopic NMDA receptor currents in HEK 293 cells expressing recombinant rat GluN1/GluN2A receptors by whole-cell patch-clamp recording using 1 mM glutamate and 0.1 mM glycine at -70 mV.
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19474309 |
In Vitro
Pregnanolone sulfate (100 μM; 2 min) enhances spontaneous glutamate release in isolated excitatory hippocampal neurons, increasing mEPSC frequency by ~3-fold[1].
Pregnanolone sulfate (100 μM; 2 min) inhibits postsynaptic NMDA receptor-mediated currents but has no net effect on NMDA receptor-mediated eEPSCs, suggesting that presynaptic enhancement of glutamate release compensates for postsynaptic NMDA receptor inhibition[1].
Pregnanolone sulfate (0.1 mM) selectively prolongs the three longest closed-time components (τEC3-5) of GluN1/GluN2A receptor closures by 100-200%, without affecting open-interval distributions or modal gating kinetics[3].
Pregnanolone sulfate (100 μM; 40 min) does not translocate GFP-tagged Munc13-1 to the plasma membrane of HEK293 cells[1].
Pregnanolone sulfate (30-300 μM) inhibits macroscopic NMDA receptor currents in HEK 293 cells expressing GluN1/GluN2A receptors in a concentration-dependent and reversible manner, with an IC50 of 67 μM[3].
Pregnanolone sulfate (0.1 mM) increases macroscopic desensitization of GluN1/GluN2A receptors in HEK 293 cells, decreasing the Iss/Ipk ratio from 0.48 to 0.08[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS No. 1477-67-4
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Molecular Weight 398.56
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Formula C21H34O5S
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SMILES
C[C@@]12[C@@]3([C@]([C@]4([C@](C)(CC3)[C@@H](C(C)=O)CC4)[H])(CC[C@@]1(C[C@H](OS(=O)(=O)O)CC2)[H])[H])[H]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)