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Radiolabeling and In Vivo Behavior of Copper-64-Labeled Cross-Bridged Cyclam Ligands

Summary: Radiolabeling and In Vivo Behavior of Copper-64-Labeled Cross-Bridged
Cyclam Ligands
Xiankai Sun, Melinda Wuest, Gary R. Weisman, Edward H. Wong, David P. Reed, C. Andrew Boswell,
Ramunas Motekaitis,,| Arthur E. Martell, Michael J. Welch, and Carolyn J. Anderson*,
Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, Missouri 63110,
Department of Chemistry, University of New Hampshire, Durham, New Hampshire 03824-3598, and
Department of Chemistry, Texas A&M University, College Station, Texas 77843
Received August 10, 2001
Macrocyclic chelators and their metal complexes have widespread applications in the biomedical
sciences, including radiopharmaceutical chemistry. The use of copper radionuclides in radio-
pharmaceuticals is increasing. Macrocyclic chelators have been found to have enhanced in vivo
stability over acyclic chelators such as ethylenediaminetetraacetic acid (EDTA) and diethyl-
enetriaminepentaacetic acid (DTPA). The currently used chelators of choice for labeling copper
radionuclides to biological molecules are analogues of TETA (1,4,8,11-tetraazacyclotetradecane-
1,4,8,11-tetraacetic acid); however, recent reports have demonstrated evidence of in vivo
instability of the radio-Cu(II)-TETA complexes. A new class of structurally reinforced
macrocycles, the "cross-bridged" cyclam derivatives, form highly stable complexes with Cu(II)
that are resistant to dissociation in strong acid. Here, we evaluate a series of 64
Cu(II) cross-
bridged macrocyclic complexes for biological stability and in vivo behavior. The ligands evaluated


Source: Anderson, Carolyn J. - Department of Molecular Biology and Pharmacology, Washington University in St. Louis


Collections: Biology and Medicine