화학공학소재연구정보센터
학회 한국공업화학회
학술대회 2017년 봄 (05/10 ~ 05/12, 광주 김대중컨벤센센터(Kimdaejung Convention Center))
권호 21권 1호
발표분야 정밀화학
제목 Synthesis of 125I-labeled tetrazine for rapid and efficient radiolabeling of trans-cyclooctene group bearing biomolecules
초록 Herein, we present a rapid and efficient radiolabeling method of trans-cyclooctene (TCO) group conjugated biomoleculs using 125I-labeled tetrazine analog. For this study, radioiodination of the stannylated precursor 2 was carried out at ambient temperature to give ([125I]1) with high radiochemical yield (65±8%) and radiochemical purity (>99%). As a radiolabeling application of ([125I]1), TCO-derivered human serum albumin (HSA) was reacted with [125I]1 under mild condition to yield the radiolabeled product [125I]3 with a high radiochemical yield (>99%). We next carried out the tissue biodistribution study of [125I]3 in normal ICR mice to investigate the level of organ accumulation profile. The biodistribution of [125I]3 showed significantly lower thyroid uptake values than that of 125I-labeled HSA ([125I]4) prepared by a direct iodine labeling method. Therefore [125I]3 will be used as a quite promising radiotracer for the various biomedical and imaging study.
저자 최미희, 심하은, 전종호
소속 한국원자력(연)
키워드 Radiolabeling; Radioactive iodine; Radiotracer; Invers-electron-demand Diels-Aler reaction
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