Synthesis of [F-18]-labeled (2-(2-fluoroethoxy)ethyl) triphenylphosphonium cation as a potential agent for myocardial imaging using positron emission tomography

[F-18]-labeled molecular probe for the detection of myocardial perfusion deficit is driving particular interest due to its high clinical applicability. Thus, we synthesized (2-(2-[F-18] fluoroethoxy) ethyl) triphenylphosphonium salt ([F-18] 3) that specifically accumulates in myocardium according to mitochondrial membrane potential. Here, we evaluated the performance of [F-18]3 as a mitochondrial voltage sensor in vitro and in vivo. The [F-18]3 was synthesized with 20 similar to 30% radiochemical yield and radiochemical purity was >98% by analytical HPLC. Specific activity was >6.7 TBq/mu mol. The cellular uptake assay showed preferential uptake of [F-18]3 in cardiomyocytes. The results of biodistribution and micro-PET imaging studies of [F-18]3 in mice and rats showed preferential accumulation in the myocardium. The results suggest that this compound would be a promising candidate for myocardial imaging. (C) 2011 Elsevier Ltd. All rights reserved.