| Title | Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase. | | Author(s) | Atucha E, Hammerschmidt F, Zolle I, Sieghart W, Berger ML | | Institution | Department of Biochemistry and Molecular Biology, Center for Brain Research, Medical University of Vienna, Austria. | | Source | Bioorg Med Chem Lett 2009 May 24. | | 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19497738 |
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