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作为σ受体配体的苯烷基1,2 -二胺:新型抗抑郁药的发现

Phenylalkyl 1,2-diamines as sigma-receptor ligands: the discovery of novel antidepressant agents.

作者信息

Kim Y-G, Seo S-Y, Heo J, Park C-E, Lee E-H, Choi Y-M

机构信息

SK Corporation, Bio-Pharmaceutical Business, Daejeon, Korea.

出版信息

Methods Find Exp Clin Pharmacol. 2006 Jan-Feb;28(1):7-11. doi: 10.1358/mf.2006.28.1.962771.

Abstract

This article focuses on the study of phenylalkyl 1,2-diamines as sigma-receptor ligands for the discovery of antidepressant agents. We synthesized N-chain substituted phenylalkyl 1,2-diamine derivatives. Phenylalkyl 1,2-diamines are one of the most important class of therapeutical medicines useful in managing central nervous system diseases and have been used mainly to treat obesity, narcolepsy, minimal brain dysfunction, and mild depression. In the present study, we found that phenylalkyl 1,2-diamine and amide compounds were strongly bound to the sigma-receptors and showed a potent activity of mice forced swimming test. Our article, after briefly outlining the background and nature of sigma-receptor ligands, explores the antidepressant activity of phenylalkyl 1,2-diamines.

摘要

本文聚焦于对苯基烷基1,2 - 二胺作为σ受体配体用于发现抗抑郁药的研究。我们合成了N - 链取代的苯基烷基1,2 - 二胺衍生物。苯基烷基1,2 - 二胺是用于治疗中枢神经系统疾病的最重要的一类治疗药物之一,主要用于治疗肥胖症、发作性睡病、轻微脑功能障碍和轻度抑郁症。在本研究中,我们发现苯基烷基1,2 - 二胺和酰胺化合物与σ受体紧密结合,并在小鼠强迫游泳试验中显示出强效活性。我们的文章在简要概述σ受体配体的背景和性质之后,探讨了苯基烷基1,2 - 二胺的抗抑郁活性。

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