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Synthesis and Biological Evaluation of Bisphosphonate Compound Labeled with 99m T c( CO ) 3 +
Author(s) -
Şenocak Kamile,
Teksöz Serap,
İçhedef Çiğdem,
Uçar Eser
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12401
Subject(s) - bisphosphonate , chemistry , biodistribution , chelation , high performance liquid chromatography , nuclear chemistry , diethylenetriaminepentaacetic acid , yield (engineering) , radiochemistry , technetium 99m , diphosphonates , bifunctional , lead compound , chromatography , nuclear medicine , in vitro , organic chemistry , scintigraphy , materials science , biochemistry , medicine , osteoporosis , metallurgy , bone resorption , catalysis , endocrinology
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.