Preparation of the novel fluorine-18-labeled VIP analog for PET imaging studies using two different synthesis methods
Preparation of the novel fluorine-18-labeled VIP analog for PET imaging studies using two different synthesis methods
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DOI：
10.1016/j.jfluchem.2006.12.007
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发表时间：
2007-03-01
影响因子：
1.9
通讯作者：
Wang, Yongxian
中科院分区：
文献类型：
--
作者：
Cheng, Dengfeng;Yin, Duanzhi;Wang, Yongxian
血管活性肠肽（VIP）受体在各种肿瘤细胞上的表达密度远高于生长抑素受体，这为放射性标记VIP作为肿瘤诊断剂提供了基础。然而，VIP在体内的快速蛋白水解降解限制了其临床应用。为了开发和评估用于通过正电子发射断层扫描 (PET) 描绘 VIP 受体的新配体，使用两种不同的方法用 F-18 对结构修饰的 [R-8,R-15.21, L-17]-VIP 类似物进行放射性标记。采用第一种方法，产生 N-4-[F-18]氟苯甲酰基-[R-8,R-15.21, L-17]-VIP ([F-18]FB-[R-8,R-15.21, L-17]-VIP 7)，衰变影响的放射化学产率 (RCY) 为 33.6 +/- 3%，比放射性为 255 GBq/mu mol （n = 5） 100分钟内分四步完成。类似地，N-4-[F-18](氟甲基)-苯甲酰基-[R-8,R-15.21, L-17]-VIP ([F-18]FMB-[R-8,R-15.21, L-17]-VIP 8) 的 RCY 为 34.85 +/- 5%，比放射性为 180 GBq/mu mol (n = 5)。 60 分钟 只需一步。两种产品7和8在HSA中均表现出良好的稳定性。而且，7和8在小鼠体内的低骨摄取表现出良好的脱氟稳定性。 (c) 2006 Elsevier B.V. 保留所有权利。
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.