Journal Title
Title of Journal: Mol Imaging Biol
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Abbravation: Molecular Imaging and Biology
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Authors: Oliver Thews Melanie Zimny Elisabeth Eppard Markus Piel Nicole Bausbacher Verena Nagel Frank Rösch
Publish Date: 2014/06/03
Volume: 16, Issue: 6, Pages: 802-812
Abstract
SPECT eg with 99mTcsestamibi is routinely used for imaging myocardial damage even though PET could offer a higher spatial resolution Using the generatorgained isotope 68Ga would allow a rapid supply of the tracer in the diagnostic unit For this reason the aim of the study was to develop 68Galabeled PET tracers based on different Schiff base amines and to evaluate the cardiomyocyte uptake in vitro as well as the biodistribution of the tracers in vivoFifteen different Schiff bases basing on 3 different backbones were synthesized and labeled with 68Ga Lipophilicity varied between 087 ± 024 and 272 ± 014 logD value All tracers were positively charged and stable in plasma and apotransferrin solution In vitro uptake into cardiomyocytes was assessed in HL1 cells in the absence and presence of the ionophor valinomycin In vivo accumulation in the heart and in various organs was assessed by small animal PET imaging as well as by ex vivo biodistribution The results were compared with 99mTcsestamibi and 18FflurpiridazAll cationic Schiff bases were taken up into cardiomyocytes but the amount varied by a factor of 10 When destroying the membrane potential the cellular uptake was markedly reduced in most of the tracers indicating the applicability of these tracers for identifying ischemic myocardium PET imaging revealed that the in vivo myocardial uptake reached a constant value approximately 10 min after injection but the intracardial amount of the tracer varied profoundly SUV 046 to 335 The most suitable tracers showed a myocardial uptake which was comparable to that of 99mTcsestamibi68Gabased Schiff bases appear suitable for myocardial PET images with uptake comparable to 99mTcsestamibi but offering higher spatial resolution By systematical variation of the backbone and the side chains tracers with optimal properties can be identified for further clinical evaluation
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