[（18）F]标记的2-甲氧基苯基哌嗪衍生物作为一种潜在的脑正电子发射断层显像剂。

[(18)F]-labeled 2-methoxyphenylpiperazine derivative as a potential brain positron emission tomography imaging agent.

作者信息

Mou Tiantian, Yang Wenjiang, Peng Cheng, Zhang Xianzhong, Ma Yunchuan

机构信息

Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, PR China.

出版信息

Appl Radiat Isot. 2009 Nov;67(11):2013-8. doi: 10.1016/j.apradiso.2009.07.012. Epub 2009 Aug 6.

DOI:10.1016/j.apradiso.2009.07.012

PMID:19679486

Abstract

This study reports the synthesis and characterization of N-(3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl-4-[(18)F]fluorobenzamide ([(18)F]MPP3F). The total reaction time for [(18)F]MPP3F, including final high-performance liquid chromatography purification, was about 3h. Typical decay-corrected radiochemical yield was 18.4+/-3.1%. The radiochemical purity was >98%. Biodistribution in mice showed that [(18)F]MPP3F is a potential brain imaging agent for positron emission tomography. The brain uptake of [(18)F]MPP3F was 6.59+/-0.77% Injected Dose/g at 2 min post-injection time. A brain-to-blood ratio of 3.67 was reached at 15 min after injection.

摘要

本研究报告了N-(3-(4-(2-甲氧基苯基)哌嗪-1-基)丙基-4-[(18)F]氟苯甲酰胺([(18)F]MPP3F)的合成与表征。[(18)F]MPP3F的总反应时间，包括最终的高效液相色谱纯化，约为3小时。典型的经衰变校正的放射化学产率为18.4±3.1%。放射化学纯度>98%。在小鼠体内的生物分布表明，[(18)F]MPP3F是一种潜在的用于正电子发射断层扫描的脑显像剂。注射后2分钟时，[(18)F]MPP3F的脑摄取量为6.59±0.77%注射剂量/克。注射后15分钟时，脑血比达到3.67。