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Synthesis, characterization and in vivo evaluation of [62Zn]–benzo-δ-sultam complex as a possible pet imaging agent

Abstract

Objective

The development of a new tracer based on the cyclic sulfonamides (sultams) was investigated.

Methods

3-(Methoxy-phenyl-methyl)-1,6-dimethyl-1H benzo[c][1,2] thiazine 2,2-dioxide (benzo-δ-sultam) was synthesized and characterized by elemental analysis, FT-IR spectroscopy and single crystal X-ray structure determination. The prepared cyclic sulfonamide was labeled with non-commercial 62Zn radioisotope for fast in vivo targeting and Coincidence imaging purposes (radiochemical purity 97 % ITLC, 96 % HPLC, specific activity 20–23 GBq/mmol). In vivo biodistribution of the final complex was investigated in Sprague Dawley® rats bearing fibro sarcoma tumor after 2, 4 and 8 h post injection and compared with free Zn+2 cation.

Results

Using instant paper chromatography method, the physicochemical properties of labeled compounds were found sufficiently stable in organic phases, e.g. a human serum, to be reliably used in bioapplications.

Conclusions

The complex exhibited a rapid as well as high tumor uptake (tumor to blood ratio 4.38 and tumor to muscle ratio 9.63) resulting in an efficient tumor targeting agent.

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The authors report no conflicts of interest in this work.

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Correspondence to Yousef Fazaeli.

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Ghandi, M., Feizi, S., Ziaie, F. et al. Synthesis, characterization and in vivo evaluation of [62Zn]–benzo-δ-sultam complex as a possible pet imaging agent. Ann Nucl Med 28, 880–890 (2014). https://doi.org/10.1007/s12149-014-0885-y

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  • DOI: https://doi.org/10.1007/s12149-014-0885-y

Keywords

  • 62Zn production
  • Benzo-δ-sultam
  • Coincidence imaging
  • Bio distribution