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Preparation, characterization and biological evaluation of 99mTc(CO)3-labelled cyclic polyamines

✍ Scribed by H. P. Vanbilloen; K. Eraets; N. Evens; C. Terwinghe; D. Rattat; G. Bormans; L. Mortelmans; A. M. Verbruggen


Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
114 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis


Three cyclic polyamines, namely 1,4,7-triazacyclononane, 1,4,7,10-tetraazacyclododecane (cyclen) and 1,4,8,11-tetraazacyclotetradecane (cyclam), were evaluated as potential ligands for complexation of a technetium(I) tricarbonyl core. They can be used as bifunctional chelating agents for labelling bioactive compounds. Each of the three ligands forms a positively charged technetium tricarbonyl complex in high yield but heating is required to promote complex formation. The charge of the 99m Tc(I)tricarbonyl labelled derivatives was confirmed using electrophoresis, and radio-LC-MS supports their proposed chemical identity. After i.v. injection in mice, the compounds were rapidly cleared from the blood by the hepatobiliary or urinary pathway depending on their lipophilicity.


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