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Synthesis and biological evaluation of 99mTc labeled aryl piperazine derivatives as cerebral radiotracers

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Abstract

The aim of this study is to develop cerebral radiotracers for central nervous system receptors imaging. The synthesis, characterization and biological evaluation of two aryl piperazine 99mTc-radiocomplexes based on the piano stool motif [CpM(CO3)] (Cp = cyclopentadienyl, M = 99mTc/Re) is reported. The 99mTc-radiocomplexes were obtained quickly (time < 5 min) with high radiochemical yields. The 99mTc-radiocomplexes characterized by high performance liquid chromatography comparison with the rhenium surrogates have both a suitable lipophilicity and are able to cross the blood brain barrier with 0.43 ± 0.05 and 1.96 ± 0.06% ID/g of brain uptake, at 10 min post injection.

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Authors and Affiliations

  1. Unit of Radiopharmaceuticals, Laboratory of Biotechnology and Nuclear Technology, National Center of Nuclear Sciences and Technology, Sidi Thabet, 2020, Tunis, Tunisia

    Kaouther Zenati, Nadia Malek Saied, Amine Asmi & Mouldi Saidi

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  1. Kaouther Zenati
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  2. Nadia Malek Saied
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  3. Amine Asmi
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  4. Mouldi Saidi
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Correspondence to Kaouther Zenati.

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Zenati, K., Malek Saied, N., Asmi, A. et al. Synthesis and biological evaluation of 99mTc labeled aryl piperazine derivatives as cerebral radiotracers. J Radioanal Nucl Chem 312, 67–74 (2017). https://doi.org/10.1007/s10967-017-5201-6

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  • DOI: https://doi.org/10.1007/s10967-017-5201-6

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