Pregnane steroids, particularly 3-alpha-hydroxylated metabolites of progesterone, are known to have rapid and profound effects on brain excitability. Recent evidence suggests that the gamma-aminobutyric acid (GABA(A))-benzodiazepine receptor-Cl- ionophore complex may mediate these actions. The data further suggest that these steroids modulate the complex through a novel site independent of other known sites on the complex. The hypothesis that this site is on the GABA(A)-benzodiazepine receptor-Cl- ionophore complex is tested in the present study by determining its presence on transiently expressed GABA(A)-benzodiazepine receptors.