Synthesis and monoamine transporter affinity of 2β-carbomethoxy-3β-(4′-p-substituted phenyl)-piperidine analogs of cocaine

被引：2
|
作者：
Bois, Frederic
Baldwin, Ronald M.
Kula, Nora S.
Baldessarini, Ross J.
Al Tikriti, M.
Innis, Robert B.
Tamagnan, Gilles D.
机构：
[1] Yale Univ, Sch Med, VA Connecticut HCS 116A2, West Haven, CT 06516 USA
[2] Harvard Univ, Sch Med, Massachusetts Gen Hosp,Dept Psychiat & Neurosci P, McLean Div,Mailman Res Ctr, Belmont, MA 02478 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 19期
关键词：
SERT; monoamine transporter; SPECT; cocaine; imaging;
D O I：
10.1016/j.bmcl.2006.07.013
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel piperidine based analogs of cocaine was synthesized and evaluated in vitro against the three monoamine transporters to develop new potential selective SERT radiotracers. Modification of the phenyl substitution with five-membered heterocyclic groups resulted in a wide affinity and selectivity scale. Radiolabeling and mouse in vivo study was performed on the piperidine analog of ZIENT, which crossed the blood-brain barrier but failed to selectively accumulate in the regions of the brain rich in SERT. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5222 / 5225
页数：4
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