Oxo-bridged isomers of aza-trishomocubane sigma (σ) receptor ligands: Synthesis, in vitro binding, and molecular modeling

被引：28

作者：

Banister, Samuel D. ^{[1
]}

Moussa, Iman A. ^{[1
]}

Jordan, Meredith J. T. ^{[1
]}

Coster, Mark J. ^{[2
]}

Kassiou, Michael ^{[1
,3
,4
]}

机构：

[1] Univ Sydney, Sch Chem, Sydney, NSW 2006, Australia

[2] Griffith Univ, Eskitis Inst Cell & Mol Therapies, Nathan, Qld 4111, Australia

[3] Brain & Mind Res Inst, Sydney, NSW 2050, Australia

[4] Univ Sydney, Discipline Med Radiat Sci, Sydney, NSW 2006, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期

关键词：

Sigma receptor; Trishomocubane; Hemiaminal; Structure-activity; Molecular modeling; Drug design; BASIS-SETS; NALORPHINE; EXPRESSION; CLONING; DRUGS; RAT;

D O I：

10.1016/j.bmcl.2009.11.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Isomeric oxo-bridged analogs of aza-trishomocubane sigma (sigma) receptor ligands were synthesized and shown to display a reduced affinity for the sigma receptor. In the case of phenethyl derivative 4, there was a concomitant introduction of high-affinity for the alpha(2C) adrenergic receptor, and moderate affinity for the dopamine transporter. Molecular modeling was undertaken to rationalize these results. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：145 / 148

页数：4

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