title: Synthesis of [¹⁸F]-labeled (2-(2-fluoroethoxy)ethyl)triphenylphosphonium cation as a potential agent for myocardial imaging using positron emission tomography.
abstract: [(18)F]-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-[(18)F]fluoroethoxy)ethyl)triphenylphosphonium salt ([(18)F]3) that specifically accumulates in myocardium according to mitochondrial membrane potential. Here, we evaluated the performance of [(18)F]3 as a mitochondrial voltage sensor in vitro and in vivo. The [(18)F]3 was synthesized with 20∼30% radiochemical yield and radiochemical purity was >98% by analytical HPLC. Specific activity was >6.7TBq/μmol. The cellular uptake assay showed preferential uptake of [(18)F]3 in cardiomyocytes. The results of biodistribution and micro-PET imaging studies of [(18)F]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.
authors: Department of Chemistry, Dongguk University-Seoul, Seoul, Republic of Korea.
authors: Dong-Yeon
authors: DY
authors: Kim
authors: Hee-Jung
authors: HJ
authors: Kim
authors: Kook-Hyun
authors: KH
authors: Yu
authors: Jung-Joon
authors: JJ
authors: Min
mesh_terms: D000818:Animals; D002412:Cations; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D015195:Drug Design; D005462:Fluorine Radioisotopes / Q000494:pharmacology; D007477:Ions; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008928:Mitochondria / Q000378:metabolism; D051336:Mitochondrial Membranes / Q000378:metabolism; D008956:Models, Chemical; D009206:Myocardium / Q000473:pathology*; D032383:Myocytes, Cardiac / Q000166:cytology; D009943:Organophosphorus Compounds / Q000737:chemistry*; D010477:Perfusion; D049268:Positron-Emission Tomography / Q000379:methods*; D051381:Rats; D013997:Time Factors; D014018:Tissue Distribution
chemical_list: D002412:Cations; D005462:Fluorine Radioisotopes; D007477:Ions; D009943:Organophosphorus Compounds