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

• DOI: 10.1007/s10967-017-5201-6
• Publication Date: 2017-02-20T14:51:07Z
• Authors: Kaouther Zenati; Nadia Malek Saied; Amine Asmi; Mouldi Saidi
• Keywords: 01 natural sciences; 0104 chemical sciences; 3. Good health

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.