title: Synthesis and biological evaluation of bisphosphonate compound labeled with (99m)Tc(CO)3(+).
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.
authors.affiliation: Ege University Institute of Nuclear Sciences, Bornova, Izmir, 35100, Turkey.
authors.forename: Kamile
authors.initials: K
authors.lastname: Şenocak
authors.forename: Serap
authors.initials: S
authors.lastname: Teksöz
authors.forename: Çiğdem
authors.initials: Ç
authors.lastname: İçhedef
authors.forename: Eser
authors.initials: E
authors.lastname: Uçar
mesh_terms: D019386:Alendronate / Q000737:chemistry; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D056831:Coordination Complexes / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D004164:Diphosphonates / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D005260:Female; D006207:Half-Life; D009682:Magnetic Resonance Spectroscopy; D015609:Organotechnetium Compounds / Q000737:chemistry*; D004369:Pentetic Acid / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: D056831:Coordination Complexes; D004164:Diphosphonates; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D004369:Pentetic Acid; D019386:Alendronate
keywords: DTPA; [99mTc(CO)3]+ core; biodistribution; bisphosphonate