Preparation of the novel fluorine-18-labeled VIP analog for PET imaging studies using two different synthesis methods

被引：16

作者：

Cheng, Dengfeng ^{[1
]}

Yin, Duanzhi ^{[1
]}

Zhang, Lan ^{[1
]}

Wang, Mingwei ^{[1
]}

Li, Gucai ^{[1
]}

Wang, Yongxian ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Appl Phys, Res Ctr Radiopharmaceut, Shanghai 201800, Peoples R China

来源：

JOURNAL OF FLUORINE CHEMISTRY | 2007年 / 128卷 / 03期

基金：

中国国家自然科学基金;

关键词：

fluorine-18; R-8; R-15; R-21; L-17]-VIP; F-18]SFB; F-18]SFMB; PET;

D O I：

10.1016/j.jfluchem.2006.12.007

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Vasoactive intestinal peptide (VIP) receptors are expressed on various tumor cells in much higher density than somatostatin receptors, which provides the basis for radiolabeling VIP as tumor diagnostic agent. However, fast proteolytic degradation of VIP in vivo limits its clinical application. With the aim to develop and evaluate new ligands for depicting the VIP receptors with positron emission tomography (PET), the structure modified [R-8,R-15.21, L-17]-VIP analog was radiolabeled with F-18 using two different methods. With the first method, N-4-[F-18]fluorobenzoyl-[R-8,R-15.21, L-17]-VIP ([F-18]FB-[R-8,R-15.21, L-17]-VIP 7) was produced in a decay-coffected radiochemical yield (RCY) of 33.6 +/- 3%, a specific radioactivity of 255 GBq/mu mol (n = 5) within 100 min in four steps. Similarly, N-4-[F-18](fluoromethyl)-benzoyl-[R-8,R-15.21, L-17]-VIP ([F-18]FMB-[R-8,R-15.21, L-17]-VIP 8) was synthesized in a RCY of 34.85 +/- 5%, a specific radioactivity of 180 GBq/mu mol (n = 5) within 60 min in only one step. The two products 7 and 8 were both shown good stability in HSA. Moreover, the low bone uptakes of 7 and 8 in vivo of mice showed good defluorination stability. (c) 2006 Elsevier B.V. All rights reserved.

引用

页码：196 / 201

页数：6

共 27 条

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