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

[18F]-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-[18F]fluoroethoxy)ethyl)triphenylphosphonium salt ([18F]3) that specifically accumulates in myocardium according to mitochondrial membrane potential. Here, we evaluated the performance of [18F]3 as a mitochondrial voltage sensor in vitro and in vivo. The [18F]3 was synthesized with 20∼30% radiochemical yield and radiochemical purity was >98% by analytical HPLC. Specific activity was >6.7 TBq/μmol. The cellular uptake assay showed preferential uptake of [18F]3 in cardiomyocytes. The results of biodistribution and micro-PET imaging studies of [18F]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.