Preparation, characterization and biological evaluation of99mTc(CO)3-labelled cyclic polyamines

Autor:	Hubert Vanbilloen, Guy Bormans, Dirk Rattat, Nele Evens, Alfons Verbruggen, K Eraets, C Terwinghe, Luc Mortelmans
Rok vydání:	2005
Předmět:	Biodistribution Chemistry Ligand Stereochemistry Organic Chemistry Biochemistry Combinatorial chemistry Analytical Chemistry chemistry.chemical_compound Cyclen Labelling Drug Discovery Cyclam Lipophilicity Radiology Nuclear Medicine and imaging Chelation Bifunctional Spectroscopy
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals. 48:1003-1011
ISSN:	1099-1344 0362-4803
DOI:	10.1002/jlcr.1012
Popis:	Three cyclic polyamines, namely 1,4,7-triazacyclononane, 1,4,7,10-tetraazacyclo-dodecane (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 99mTc(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 © 2005 John Wiley & Sons, Ltd.
Databáze:	OpenAIRE
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