Kit-like 18F-labeling of RGD-19F-Arytrifluroborate in high yield and at extraordinarily high specific activity with preliminary in vivo tumor imaging

摘要: Abstract Introduction Positron Emission Tomography (PET) is a rapidly expanding, cutting edge technology for preclinical evaluation, cancer diagnosis and staging, patient management. A one-step aqueous 18 F-labeling method, which can be applied to peptides provide functional in vivo images, has been long-standing challenge PET imaging. Over the past few years, we have sought rapid mild radiolabeling method based on radiosynthesis of stable aryltrifluoroborate (ArBF 3 − ) conjugates. Recent access production levels F-Fluoride led fluorescent- F-ArBF at unprecedentedly high specific activities 15Ci/μmol. However, extending this labeling as imaging agents not explored. Methods In order extend these results peptide clinical interest context production-level radiosynthesis, new RGD, measured its activity by standard curve analysis, carried out preliminary evaluation properties. Results RGD was labeled excellent radiochemical yields exceptionally (~14Ci/μmol) (n=3). Preliminary tumor-specific images corroborated ex biodistribution data with blocking controls show statistically significant albeit relatively low tumor uptake along reasonably tumor:blood ratios Conclusions Isotope exchange clinically useful radiotracer leads while anionic nature prosthetic very clearance. Since clearance radioactive tracer generally desirable development, suggest directions varying linker arm composition slightly retard rather than enhancing it. Advances Knowledge Implications Care This work first use F-activity directly label that are an magnitude higher most reports thereby increases distribution window delivery.