Novel synthesis and initial preclinical evaluation of F-18-[FDG] labeled rhodamine: a potential PET myocardial perfusion imaging agent

摘要

Myocardial perfusion imaging is one of the most commonly performed investigations in nuclear medicine studies. Due to the clinical importance of [F-18]-fluoro-2-deoxy-D-glucose ([F-18-FDG) and its availability in almost every PET center, a new radiofluorinated [F-18]-FDG-rhodamine conjugate was synthesized using [F-18]-FDG as a prosthetic group. In a convenient and simple one-step radiosynthesis, [F-18]FDG-rhodamine conjugate was prepared in quantitative radiochemical yields, with total synthesis time of nearly 20 min and radiochemical purity of greater than 98%, without the need for HPLC purification, which make these approaches amenable for automation. Biodistribution studies in normal rats at 60 min post-injection demonstrated a high uptake in the heart (>11% ID/g) and favorable pharmacokinetics. Additionally, [F-18]-FDG-rhodamine showed an extraction value of 27.63% +/- 5.12% in rat hearts. These results demonstrate that [F-18]-FDG-rhodamine conjugate may be useful as an imaging agent for the positron emission tomography evaluation of myocardial perfusion. (C) 2015 Elsevier Inc. All rights reserved.