Journal
JOURNAL OF FLUORINE CHEMISTRY
Volume 128, Issue 3, Pages 196-201Publisher
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jfluchem.2006.12.007
Keywords
fluorine-18; [R-8,R-15,R-21; L-17]-VIP; [F-18]SFB; [F-18]SFMB; PET
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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.
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