The in vivo behavior of copper-64-labeled azamacrocyclic complexes

Teresa M. Jones-Wilson, Kim A. Deal, Carolyn J. Anderson, Deborah W. McCarthy, Zoltan Kovacs, Ramunas J. Motekaitis, A. Dean Sherry, Arthur E. Martell, Michael J. Welch

Research output: Contribution to journalArticlepeer-review

148 Scopus citations


The use of copper radioisotopes in imaging and therapy applications has created a greater need for bifunctional chelates (BFCs) for complexing copper radioisotopes to biomolecules. It has been demonstrated that the charge and lipophilicity of the Cu-BFC complex has a significant effect on the in vivo behavior of the radiolabeled Cu-BFC-biomolecule conjugate. To evaluate the effects of charge, stability, and macrocyclic backbone size on the biological behavior of 64Cu complexes, a series of macrocyclic 64Cu complexes have been prepared, and the biodistributions of these agents were evaluated in normal Sprague-Dawley rats. Two macrocyclic backbones, dodecane and tetradecane, were evaluated; cyclen, DOTA, and DO2A were dodecane backbone derivatives, and cyclam, TETA, and et-cyclam were tetradecane backbone derivatives. The biodistributions of the 64Cu-labeled complexes correlated with differences in the size of the macrocycle backbone and the formal charge of the complex. All compounds showed uptake and clearance through the liver and kidneys; however, the positively charged 64Cu complexes showed significantly higher uptake in both of these organs than did the negatively charged or neutral complexes. 64Cu-TETA, a negatively charged complex with the tetradecane backbone, had the most efficient clearance by 24 hours' postinjection. These data suggest that negatively charged complexes may have more favorable clearance properties when used as BFCs.

Original languageEnglish (US)
Pages (from-to)523-530
Number of pages8
JournalNuclear Medicine and Biology
Issue number6
StatePublished - Aug 1998


  • Biodistribution
  • Copper-64
  • Macrocycle
  • Stability constant

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research


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