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

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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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Conflict of interest

The authors report no conflicts of interest in this work.

Author information

Authors and Affiliations

  1. School of Chemistry, College of Science, University of Tehran, P.O. Box 14155 6455, Tehran, Iran

    Mehdi Ghandi & Shahzad Feizi

  2. Nuclear Science and Technology Research Institute (NSTRI), P.O. Box: 31485-498, Karaj, Iran

    Shahzad Feizi, Farhood Ziaie & Yousef Fazaeli

  3. Department of Chemistry, Shahid Beheshti University, G. C. Evin, P.O. Box 1983963113, Tehran, Iran

    Behrooz Notash

Authors
  1. Mehdi Ghandi
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  2. Shahzad Feizi
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  3. Farhood Ziaie
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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

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