Jump to main content
Jump to site search

Issue 1, 2016
Previous Article Next Article

Synthesis, 64Cu-labeling and PET imaging of 1,4,7-triazacyclononane derived chelators with pendant azaheterocyclic arms

Author affiliations

Abstract

The TACN derived chelators NOTI, NOTI-Me and NOTThia were synthesized in a facile, single reaction step. The new chelators were readily labeled with 64Cu under mild conditions over a wide pH range. The corresponding 64Cu complexes are of high stability in vitro as determined by Cu2+ exchange experiments, acid decomplexation and serum stability studies. Single crystal X-ray analysis showed that the six-coordinate copper complexes exhibited a distorted prismatic CuN3N′3 coordination geometry similar to Cu(NOTA). Biological testing by small animal PET imaging revealed retention of 64Cu complexes in the kidneys and, to a lesser extent, in the liver. Altogether, the results presented support the development of bifunctional derivatives for conjugation to targeting vectors and further testing in vivo.

Graphical abstract: Synthesis, 64Cu-labeling and PET imaging of 1,4,7-triazacyclononane derived chelators with pendant azaheterocyclic arms

Back to tab navigation

Supplementary files

Publication details

The article was received on 12 Oct 2015, accepted on 11 Dec 2015 and first published on 14 Dec 2015


Article type: Paper
DOI: 10.1039/C5RA21131J
RSC Adv., 2016,6, 119-131

  •   Request permissions

    Synthesis, 64Cu-labeling and PET imaging of 1,4,7-triazacyclononane derived chelators with pendant azaheterocyclic arms

    C. Gotzmann, F. Braun and M. D. Bartholomä, RSC Adv., 2016, 6, 119
    DOI: 10.1039/C5RA21131J

Search articles by author

Spotlight

Advertisements