Pregnenolone sulfate: a positive allosteric modulator at the N-methyl-D-aspartate receptor


Wu FS, Gibbs TT, Farb DH




Mol Pharmacol . 1991 Sep;40(3):333-6.

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The N-methyl-D-aspartate (NMDA) receptor is believed to play a major role in learning and in excitotoxic neuronal damage associated with stroke and epilepsy.

Pregnenolone sulfate, a neurosteroid, specifically enhances NMDA-gated currents in spinal cord neurons, while inhibiting receptors for the inhibitory amino acids glycine and gamma-aminobutyric acid, as well as non-NMDA glutamate receptors.

This observation is consistent with the hypothesis that neurosteroids such as pregnenolone sulfate are involved in regulating the balance between excitation and inhibition in the central nervous system.


Electrophysiological effects of pregnenolone on the NMDA receptor. (Source: modified from Wu FS et al. 1991)
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