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

页码：3852 / 3857

页数：6

共 18 条

[11]

GLASE SA, 2004, ANN REPORTS MEDICINA, V39

[12] 3 alpha-(4-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: Novel ligands with high affinity and selectivity at the dopamine transporter [J].