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Design, Synthesis, and Imaging of Small Amphiphilic Rhenium and (99m)Technetium Tricarbonyl Complexes

TitleDesign, Synthesis, and Imaging of Small Amphiphilic Rhenium and (99m)Technetium Tricarbonyl Complexes
Publication TypeJournal Article
Year of Publication2009
AuthorsBoros, E, Hafeli, UO, Patrick, BO, Adam, MJ, Orvig, C
JournalBioconjugate Chemistry
Volume20
Pagination1002-1009
Date PublishedMay
Type of ArticleArticle
ISBN Number1043-1802
KeywordsBIFUNCTIONAL LIGAND, BIOMOLECULES, SMALL-MOLECULE RADIOPHARMACEUTICALS, SYSTEMS, technetium
Abstract

The design, synthesis, radiolabeling, evaluation of stability, and in vivo investigation are presented of three variably charged, novel, short C-8 chain derivatized chelators for the [M(CO)(3)](+) core (M = Tc-99m or Re). Labeling with [Tc-99m(CO)3](+) showed complex formation in under 1 h reaction time and high stability toward 24 h histidine and cysteine challenges, as well as distinctive log P values for each complex. Distinct localization of small amphiphilic molecules in in vivo systems depends on the charge of the polar moiety and was studied via biodistribution (4 h) and imaging (15 min, 1, 2, and 4 h) in female C57B1/6 mice.

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