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Summary: Labeling and in Vivo Evaluation of Novel Copper(II)
Dioxotetraazamacrocyclic Complexes
Cathy S. Cutler,1,
* Melinda Wuest,1
Carolyn J. Anderson,1
David E. Reichert,1
Yizhen Sun,2
Arthur E. Martell2
and Michael J. Welch1
1
MALLINCKRODT INSTITUTE OF RADIOLOGY, WASHINGTON UNIVERSITY SCHOOL OF MEDICINE, ST. LOUIS, MISSOURI USA;
AND 2
DEPARTMENT OF CHEMISTRY, TEXAS A & M UNIVERSITY, COLLEGE STATION, TEXAS, USA
ABSTRACT. 64
Cu shows promise as both a positron emission tomography imaging and radiotherapeutic
radionuclide due to its half-life (T1/2 12.7 h), decay characteristics ( [19%]; [40%]), and the
capability to produce it on a large-scale with high specific activity on a biomedical cyclotron. Macrocyclic
chelators are generally used as bifunctional chelators to attach Cu(II) to antibodies and peptides due to their
relatively high in vitro stability. To investigate neutral Cu(II) complexes, we performed labeling experiments
with six tetraazamacrocyclic ligands with different chelate ring sizes. 1,4,8,11-Tetraazacyclotetradecane-3,9-
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