PMID: 11311894Apr 20, 2001Paper

Unsulfated and sulfated neurosteroids differentially modulate the binding characteristics of various radioligands of GABA(A) receptors following chronic ethanol administration

Neuropharmacology
A K Mehta, M K Ticku

Abstract

Dehydroepiandrosterone (DHEA) and dehydroepiandrosterone sulfate (DHEAS) inhibited the binding of [(3)H]flunitrazepam (2 nM), [(3)H]muscimol (5 nM) and 4 nM [(35)S]t-butylbicyclophosphorothionate [(35)S]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 [(3)H]flunitrazepam binding significantly to a lesser extent in the cerebellum of ethanol-dependent rats as compared to the control group (I(max):82+/-1vs.92+/-2%, p<0.005). However, DHEA, unlike DHEAS, inhibited [(35)S]TBPS binding to a greater extent in the ethanol-dependent rat cerebellum as compared to the control group (I(max):31+/-2vs.19+/-2%, p<0.005). Furthermore, DHEA was more potent in inhibiting [(35)S]TBPS binding in the cerebellum (IC(50):55+/-5 vs. 74+/-7 microM, p<0.05) and cerebral cortex (IC(50):26+/-4vs.64+/-9 microM, p<0.05) of ethanol-dependent rats as compared to the control group. These observations indicate that unsulfated and sulfated androstane-steroids modulate the GABA(A) receptors in the control as well as the ethanol-dependent rats differentially, and also suggest that the a...Continue Reading

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Citations

Feb 16, 2010·Behavior Genetics·Stephane MortaudPierre L Roubertoux
Jun 8, 2006·Cellular and Molecular Neurobiology·György LürJózsef Toldi
Apr 25, 2009·Alcoholism, Clinical and Experimental Research·Olga V GurkovskayaPeter J Winsauer
Nov 11, 2008·Annals of the New York Academy of Sciences·Maharaj K Ticku, Ashok K Mehta
Jul 14, 2004·Brain Research. Molecular Brain Research·Qianxing MoNeal G Simon
Oct 29, 2005·Neurobiology of Aging·Nancy BélangerThérèse Di Paolo
Feb 9, 2012·Journal of Korean Academy of Nursing·Myoung Ae ChoeSonghee Jeon
Feb 28, 2003·The Journal of Pharmacology and Experimental Therapeutics·Huifang WuAndrew Coop

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