Dual Mode Fluorescent 18F-PET Tracers: Efficient Modular Synthesis of Rhodamine-[cRGD]2-[18F]-Organotrifluoroborate, Rapid, and High Yielding One-Step 18F-Labeling at High Specific Activity, and Correlated in Vivo PET Imaging and ex Vivo Fluorescence
作者： Zhibo Liu , Mark Alex Radtke , May Q. Wong , Kuo-Shyan Lin , Donald T. Yapp
DOI: 10.1021/BC5003357
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摘要: The design of dual mode fluorescent-PET peptidic tracers that can be labeled with [18F]fluoride at high specific activity and yield has been challenged by the short half-life 18F its aqueous indolence toward nucleophilic displacement, often necessitates multistep reactions start punctiliously dry conditions. Here we present a modular approach to constructing fluorescent dimeric peptide pendant radioprosthesis is in water ion single, user-friendly step. starts grafting new zwitterionic organotrifluoroborate onto pentaerythritol core three pendent alkynes enable successive bright fluorophore (rhodamine) followed two peptides (cylcoRGD). construct via isotope exchange within 20 min single step (>3 Ci/μmol) good provide 275 mCi radiochemical purity. Neither drying [18F]f...
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