• Bioorg. Med. Chem. Lett. · Aug 2009

    Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.

    • Erika Atucha, Friedrich Hammerschmidt, Ilse Zolle, Werner Sieghart, and Michael L Berger.
    • Department of Biochemistry and Molecular Biology, Center for Brain Research, Medical University of Vienna, Austria.
    • Bioorg. Med. Chem. Lett. 2009 Aug 1;19(15):4284-7.

    AbstractAt the GABA(A) receptor, low concentrations of etomidate potentiate the inhibitory effect of GABA on specific binding of the closed channel ligand [(3)H]ethynylpropylbicycloorthobenzoate ([(3)H]EBOB). Here, we present SARs for etomidate and structurally related compounds inducing this effect. In the absence of GABA, similar SARs, but 14-20 times weaker potencies were observed. We discuss these SARs in comparison to the much higher potencies of these compounds as inhibitors of 11beta-hydroxylase.

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