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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kim DY,Kim HJ,Yu KH,Min JJ

doi

10.1016/j.bmcl.2011.11.005

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

319-22

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01537-X

journal_volume

22

pub_type

杂志文章

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