Synthesis and biological evaluation of 3-{[4-(4-[18F]fluorophenyl)methyl] piperazin-1-yl}-methyl-1H-pyrrolo[2,3-b]pyridine for in vivo studies of dopamine D4 receptor

被引：2
作者：
Tian, HB
Yin, DZ
Zhang, L
Wang, LH
Zhang, CF
Li, JL
Zhou, W
Wu, CY
Wang, YX
机构：
[1] Chinese Acad Sci, Shanghai Inst Nucl Res, Radiopharmaceut Res Ctr, Shanghai 201800, Peoples R China
[2] Fudan Univ, Hua Shang Hosp, Dept Nucl Med, Shanghai 201800, Peoples R China
来源：
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2004年 / 262卷 / 02期
关键词：
D O I：
10.1023/B:JRNC.0000046767.58871.f0
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
The compound 3-{[4-(4-[F-18]fluorophenyl)methyl]piperazin-1-yl}-methyl-1H-pyrrolo[2,3-b]pyridine ([F-18]3), which is an analogue of L-745,870 binding D-4 receptor in vitro was synthesized and evaluated. The compound [F-18] 3 was prepared by reductive alkylation of 3-(piperazin-1-yl)methyl-1H-pyrrolo[2,3-b]pyridine (2) with 4-[F-18]fluorobenzaldehyde with a radiochemical yield of 9.0-12.0% (decay-corrected) and high specific activity (>37 GBq/mumol). Tissue distribution and metabolism studies in rats demonstrated the specific distribution of [F-18] 3 in brain regions, suggesting that this radioligand may be a suitable PET trace agent for in vivo studies of dopamine D-4 receptor.
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收藏
页码：383 / 389
页数：7
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