Structure–activity relationship of etomidate derivatives at the GABAA receptor: Comparison with binding to 11β-hydroxylase

Abstract

At the GABAA receptor, low concentrations of etomidate potentiate the inhibitory effect of GABA on specific binding of the closed channel ligand [3H]ethynylpropylbicycloorthobenzoate ([3H]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 11β-hydroxylase.