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  • Title: Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.
    Author: Atucha E, Hammerschmidt F, Zolle I, Sieghart W, Berger ML.
    Journal: Bioorg Med Chem Lett; 2009 Aug 01; 19(15):4284-7. PubMed ID: 19497738.
    Abstract:
    At 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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