Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 (N-fluoroalkyl) labeled 2β-carbomethoxy-3β-(4′-(3-furyl)phenyl)tropanes and -nortropanes:: Candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography

被引：14

作者：

Stehouwer, JS

Plisson, C

Jarkas, N

Zeng, FX

Voll, RJ

Williams, L

Martarello, L

Votaw, JR

Tamagnan, G

Goodman, MM

机构：

[1] Emory Univ, Dept Radiol, Atlanta, GA 30322 USA

[2] Yale Univ, Dept Psychiat, West Haven, CT 06516 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 22期

关键词：

D O I：

10.1021/jm0504095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2 beta-Carbomethoxy-3 beta-(4'-(3-furyl)phenyl)nortropane (1) was synthesized along with the N-methyl (2), N-fluoroethyl (3), N-fluoropropyl (4), and N-fluorobutyl (5) derivatives. The binding affinity for each compound to the human serotonin, dopamine, and norepinephrine transporters was determined using transfected HEK-293 cells. Radiolabeling and microPET brain imaging studies were performed with [C-11]1, [C-11]2, and [F-18]3 to determine their utility as in vivo imaging agents.

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页码：7080 / 7083

页数：4

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