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Issue 1, 2016
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Synthesis, 64Cu-labeling and PET imaging of 1,4,7-triazacyclononane derived chelators with pendant azaheterocyclic arms

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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

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Article information


Submitted
12 Oct 2015
Accepted
11 Dec 2015
First published
14 Dec 2015

RSC Adv., 2016,6, 119-131
Article type
Paper

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

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