Synthesis of 2β-acyl-3β-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites

被引：27

作者：

Davies, HML ^{[1
]}

Gilliatt, V

Kuhn, LA

Saikali, E

Ren, PD

Hammond, PS

Sexton, T

Childers, SR

机构：

[1] SUNY Buffalo, Dept Chem, Buffalo, NY 14260 USA

[2] Wake Forest Univ, Sch Med, Dept Chem, Winston Salem, NC 27109 USA

[3] Wake Forest Univ, Sch Med, Dept Radiol, Winston Salem, NC 27157 USA

[4] Targacept Inc, Winston Salem, NC 27102 USA

[5] Wake Forest Univ, Sch Med, Dept Physiol, Winston Salem, NC 27157 USA

[6] Wake Forest Univ, Sch Med, Dept Pharmacol, Winston Salem, NC 27157 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 10期

关键词：

D O I：

10.1021/jm000363+

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3 beta -naphthyltropane derivatives were synthesized and found to show high affinity at both the dopamine and serotonin transporter sites, leading to some of the most potent inhibitors known based on the tropane structure. Comparative molecular field analysis (CoMFA) models were developed for both dopamine and serotonin transporter binding data. These models provide insights into those factors that influence binding at the two transporters.

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页码：1509 / 1515

页数：7

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