Nuclear and Optical Dual-labelled Imaging Agents


Nuclear and Optical Dual-labelled Imaging Agents

Stephan, H.

For the past decade, nuclear and optical dual-labelled imaging agents have attracted enormous attention 1. Applied to cancer imaging, tumours can be tracked down by nuclear techniques such as SPECT and PET, and subsequently resected using image-guided surgery with the appropriate fluorophores. Moreover, the high spatial resolution of fluorescence imaging permits the elucidation of cell-biological events and thereby gaining a deeper insight into in vitro and in vivo processes. The development of dual imaging probes can be achieved using sophisticated low-molecular compounds that combine moieties for the desired imaging modalities, e.g. dyes for fluorescence optical imaging, and appropriate bifunctional chelator agents (BFCAs) for radiometals enabling SPECT or PET. We have developed BFCAs based on bis(2-pyridylmethyl)-1,4,7-triazacyclononane (DMPTACN) and 3,7-diazabicyclo[3.3.1]nonane (bispidine) that rapidly form stable 64CuII complexes under mild conditions. These BFCAs are well-suited for in vivo application in cancer imaging 2, 3. Since they are also relatively easy to functionalize with multiple modalities, they are ideal chelators for the design of targeted dual-labelled imaging agents (PET, fluorescence imaging) 4, 5.
Here, important features of 64CuII-labelled DMPTACN and bispidine complexes, e.g. stabilities, coordination geometry, ligand exchange kinetics, serum stability, partition coefficients (n-octanol/water), photophysical properties of dye-labelled compounds and biodistribution data will be reported.

1 A. Azhdarinia et al., Mol. Imag. Biol. 2012, 14, 261. 2 S. Juran et al., Bioconjugate Chem. 2009, 20, 347.
3 R. Bergmann et al., Eur. J. Med Chem. 2013, 70, 434. 4 K. Viehweger et al., Bioconjugate Chem. 2014, 25, 1011. 5 H. Stephan et al., Chem. Eur. J. 2014, 20, 17011.

  • Lecture (Conference)
    6th EuCheMS Chemistry Congress, 11.-15.09.2016, Seville, Spain

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Publ.-Id: 24198