Binding of pregnenolone sulfate to rat brain membranes suggests multiple sites of steroid action at the GABAA receptor.

@article{Majewska1990BindingOP,
  title={Binding of pregnenolone sulfate to rat brain membranes suggests multiple sites of steroid action at the GABAA receptor.},
  author={Maria Dorota Majewska and S Demirg{\"o}ren and Edythe D. London},
  journal={European journal of pharmacology},
  year={1990},
  volume={189 4-5},
  pages={307-15}
}
The steroid pregnenolone sulfate (PS) interacts with the GABAA receptor complex in a mixed GABA-agonistic/antagonistic manner in binding experiments. However, in functional assays pregnenolone sulfate (at micromolar concentrations) behaves as an allosteric GABAA receptor antagonist, similar to the convulsant, picrotoxin. In the present work, we examined the binding of [3H] pregnenolone sulfate to membranes from rat brain. We report that this steroid binds to two or three populations of sites… CONTINUE READING

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