Access of inhibitory neurosteroids to the NMDA receptor.

ABSTRACT:

Background and purpose

NMDA receptors are glutamatergic ionotropic receptors involved in excitatory neurotransmission, synaptic plasticity and excitotoxic cell death. Many allosteric modulators can influence the activity of these receptors positively or negatively, with behavioural consequences. 20-Oxo-5β-pregnan-3α-yl sulphate (pregnanolone sulphate; PA-6) is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective. We tested the hypothesis that the interaction of PA-6 with the plasma membrane is critical for its inhibitory effect at NMDA receptors.

Experimental approach

Electrophysiological recordings and live microscopy were performed on heterologous HEK293 cells expressing GluN1/GluN2B receptors and cultured rat hippocampal neurons.

Key results</

SUBMITTER: Borovska J 

PROVIDER: S-EPMC3417430 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature