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

被引：28

作者：

Atucha, Erika ^{[1
]}

Hammerschmidt, Friedrich ^{[2
]}

Zolle, Ilse ^{[2
]}

Sieghart, Werner ^{[1
]}

Berger, Michael L. ^{[1
]}

机构：

[1] Med Univ Vienna, Ctr Brain Res, Dept Biochem & Mol Biol, Vienna, Austria

[2] Univ Vienna, A-1010 Vienna, Austria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期

关键词：

GABA(A) receptor complex; Etomidate; H-3]EBOB binding; ANESTHETIC ETOMIDATE; ANTIFUNGAL AGENTS; ADRENAL-CORTEX; ACID; SITES;

D O I：

10.1016/j.bmcl.2009.05.065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

At the GABA(A) receptor, low concentrations of etomidate potentiate the inhibitory effect of GABA on specific binding of the closed channel ligand [H-3] ethynylpropylbicycloorthobenzoate ([H-3]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 11 beta-hydroxylase. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4284 / 4287

页数：4

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