1. Synthesis and biological evaluation of bisphosphonate compound labeled with (99m)Tc(CO)3(+).
- Author
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Şenocak K, Teksöz S, İçhedef Ç, and Uçar E
- Subjects
- Alendronate chemistry, Animals, Chromatography, High Pressure Liquid, Coordination Complexes blood, Drug Evaluation, Preclinical, Drug Stability, Female, Half-Life, Magnetic Resonance Spectroscopy, Pentetic Acid chemistry, Radiopharmaceuticals blood, Rats, Rats, Wistar, Tissue Distribution, Coordination Complexes chemical synthesis, Coordination Complexes pharmacokinetics, Diphosphonates chemistry, Organotechnetium Compounds chemistry, Radiopharmaceuticals chemical synthesis, Radiopharmaceuticals pharmacokinetics
- Abstract
In this study, radiolabeling of a bisphosphonate, alendronate (Alendronate sodium), was performed with the help of a bifunctional chelating agent. For that purpose, DTPA-NHS (Diethylenetriaminepentaacetic acid dianhydride-N-hydroxysuccinimide) was synthesized with an esterification between DTPA and NHS. Combining the DTPA-NHS ester with alendronate yields the DTPA-Alendronate compound. The structure of synthesized compound was analyzed by (1) H/(13) C/(31) P-NMR and HPLC. After then, the labeling with [(99m) Tc(CO)3 ](+) core of synthesized compound was provided. Performing quality controls of newly synthesized [(99m) Tc(CO)3 -DTPA-Alendronate] complex with thin layer radiochromatography (TLRC) and high-performance liquid radiochromatography (HPLRC), the labeling yield was found as 99%. It was observed that the compound conserves its stability for 24 h in serum media. Biodistribution of the radiolabeled complex was performed on Wistar Albino rats to determine radiopharmaceutical potential of the [(99m) Tc(CO)3 -DTPA-Alendronate] complex. It is thought that the data gained from this study will contribute to the development of complexes with bisphosphonate., (© 2014 John Wiley & Sons A/S.)
- Published
- 2015
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