Journal of Labelled Compounds & Radiopharmaceuticals vol:48 issue:14 pages:1003-1011
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(l) 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 Tc-99m(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. Copyright (c) 2005 John Wiley & Sons, Ltd.