Synthesis and dopamine transporter binding affinities of 3α-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes

被引：12

作者：

Bradley, AL

Izenwasser, S

Wade, D

Klein-Stevens, C

Zhu, NJ

Trudell, ML ^{[1
]}

机构：

[1] Univ New Orleans, Dept Chem, New Orleans, LA 70148 USA

[2] Univ Miami, Sch Med, Dept Psychiat, Miami, FL 33136 USA

[3] Xavier Univ, Dept Chem, New Orleans, LA 70125 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00464-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes was synthesized and the binding affinities of the compounds were determined at the dopamine transporter. The unsubstituted analogue 7b (K-i = 98 nM) was the most potent compound of the series with binding affinity three-times greater than cocaine and only 5-fold less than GBR-12909. The structure-activity data for 7a-f suggests that these compounds may be binding at the dopamine transporter in a similar fashion to GBR 12909. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：2387 / 2390

页数：4

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