Synthesis and monoamine transporter binding properties of 3α-(substituted phenyl)nortropane-2β-carboxylic acid methyl esters.: Norepinephrine transporter selective compounds

被引：14
|
作者：
Carroll, FI
Tyagi, S
Blough, BE
Kuhar, MJ
Navarro, HA
机构：
[1] Res Triangle Inst, Res Triangle Pk, NC 27709 USA
[2] Emory Univ, Yerkes Natl Primate Ctr, Atlanta, GA 30329 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 11期
关键词：
D O I：
10.1021/jm058164j
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
3 alpha-(Substituted phenyl)nortropane-2 beta-carboxylic acid methyl esters (8a-h) showed high affinity for the norepinephrine transporter (NET). The most potent and selective compound was 3 alpha-(3-fluoro-4-methylphenyl)nortropane-2 beta-carboxylic acid methyl ester (8d), with a K-i of 0.43 nM at the NET and 21- and 55-fold selectivity relative to binding at the dopamine and serotonin transporters. The development of 8d makes available compounds selective for all three transporters from the same structural class.
引用
收藏
页码：3852 / 3857
页数：6
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