NMDA positive modulator (neurosteroid)
NMDA receptor positive modulator (neurosteroid)
- Neurosteroid enhancement of NMDA currents (largely indirect, via sigma-1 signaling)
- Not a glutamate-site agonist — potentiates the receptor’s response to glutamate
- Excess NMDA facilitation → excitability, proconvulsant potential
- Neurosteroid enhancement of NMDA currents (largely indirect, via sigma-1 signaling)
- Not a glutamate-site agonist — potentiates the receptor’s response to glutamate
- Excess NMDA facilitation → excitability, proconvulsant potential
Drugs with this mechanism (2)
- Dehydroepi androsterone — Adrenal precursor of testosterone and estradiol, and a sigma-1 agonist in the central nervous system.
- DHEAS — The sulfated, circulating reservoir form of DHEA; a negative modulator at GABA-A.
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