GABA-active steroids: endogenous modulators of GABA-gated chloride ion conductance.

  title={GABA-active steroids: endogenous modulators of GABA-gated chloride ion conductance.},
  author={Stephen I. Deutsch and J. A. Mastropaolo and Ana Hitri},
  journal={Clinical neuropharmacology},
  volume={15 5},
Naturally occurring 3-alpha-hydroxy ring A-reduced metabolites of progesterone and deoxycorticosterone and their synthetic analogues bind to specific sites within the hydrophobic channel domain of the GABAA receptor complex. Acting at these sites, these ligands function as positive allosteric effectors of the complex; they potentiate GABA-stimulated membrane chloride ion conductance, enhance the binding of [3H]muscimol and [3H]flunitrazepam, and displace the binding of [35S]t… CONTINUE READING
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