Abstract
Dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEAS) inhibited the binding of [3H]flunitrazepam (2 nM), [3H]muscimol (5 nM) and 4 nM [35S]t-butylbicyclophosphorothionate [35S]TBPS in the rat cerebellum as well as cerebral cortex. DHEAS-induced inhibition of binding of these radioligands (62% to 100%) was more pronounced as compared to that in the case of DHEA (5% to 31%). DHEAS, unlike DHEA, inhibited [3H]flunitrazepam binding significantly to a lesser extent in the cerebellum of ethanol-dependent rats as compared to the control group (Imax:82±1vs.92±2%, p<0.005). However, DHEA, unlike DHEAS, inhibited [35S]TBPS binding to a greater extent in the ethanol-dependent rat cerebellum as compared to the control group (Imax:31±2vs.19±2%, p<0.005). Furthermore, DHEA was more potent in inhibiting [35S]TBPS binding in the cerebellum (IC50:55±5 vs. 74±7 μM, p<0.05) and cerebral cortex (IC50:26±4vs.64±9 μM, p<0.05) of ethanol-dependent rats as compared to the control group. These observations indicate that unsulfated and sulfated androstane-steroids modulate the GABAA receptors in the control as well as the ethanol-dependent rats differentially, and also suggest that the androstane-steroid binding sites associated with the GABAA receptors play an important role during ethanol dependence.
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