Studies towards the development of lipophilic bifunctional N3S3 chelators for 68Ga

P. Riss; Nils Hanik; Frank Rösch

doi:10.1524/ract.2010.1731

Published by De Gruyter (O) September 2, 2010

Studies towards the development of lipophilic bifunctional N₃S₃ chelators for ⁶⁸Ga

P. Riss , Nils Hanik and Frank Rösch

From the journal Radiochimica Acta

https://doi.org/10.1524/ract.2010.1731

Showing a limited preview of this publication:

Abstract

The present study is concerned with a concept of charge-neutral, lipophilic, macrocyclic bifunctional chelators, suitable for the introduction of a gallium-68 label into small molecules. The synthesis of a novel bifunctional N₃S₃-type chelator, derived from 1,4,7-triazacyclononane, initial ⁶⁸Ga-radiolabelling and the determination of stability and calculated lipophilicity of the compound are described. The ⁶⁸Ga-labelled chelate was obtained in a maximum radiochemical yield of 93±5% after a reaction time of 2 min. It remained intact over 3 h in a DTPA-challenge and a transferrin challenge experiment, indicating sufficient stability for PET studies.

Keywords: Gallium-68; Trithiolate chelators; Radiopharmaceutical chemistry; Lipophilic complexes; Bifunctional chelators

^* Correspondence address: Universität Mainz, Institute of Nuclear Chemistry, Fritz-Strassmann-Weg 2, 55126 Mainz

Published Online: 2010-09-02

Published in Print: 2010-08

Studies towards the development of lipophilic bifunctional N₃S₃ chelators for ⁶⁸Ga

Abstract

Journal and Issue

Articles in the same Issue