Authors: Yuanyou Yang Ning Liu Jiali Liao Manfei Pu Yebin Liu Min Wei Jiannan Jin
Publish Date: 2009/10/30
Volume: 283, Issue: 2, Pages: 329-335
Abstract
In this paper 3amino1hydroxypropylidene11bisphosphonateAPB a amidobisphophonate was synthesized and labeled with the αemitter 211At by an indirect method using Nsuccinimidyl 5tributylstannyl3pyridinecarboxylate SPC as a bifunctional linker and the conjugated amidobisphophonate 211AtSAPCAPB was preliminarily evaluated in vitro and in vivo by comparison with free astatide 211At− and 99mTcMDP 3amino1hydroxypropylidene11bisphosphonateAPB was prepared using βalanine as the starting material With SPC bifunctional linker APB was conjugated with 211At in a labeling yield of 80–90 with radiochemical purity of more than 99 The conjugated amidobisphophonate 211AtSAPCAPB exhibited considerable stability in vitro in that the radiochemical purity of 211AtSAPCAPB was still more than 98 in 01 mol/L PBS pH 76 or in fetal calf serum even stayed for 24 h at room temperature RT Biodistribution of 211AtSAPCAPB was investigated in NIH strain mice by IV injection The results showed that 211AtSAPCAPB could rapidly locate in shank with the maximum uptake of 2370 ± 229 ID/g at 6 h earlier than that of 99mTcMDP at 12 h and stayed in the bone for long time Moreover 211AtSAPCAPB uptake in some key organs or tissues especially in thyriod stomach lung and spleen was much less than that of free astatide 211At− implying that 211AtSAPCAPB was constantly stable in vivo as well as in vitro These results indicated that 211AtSAPCAPB will be a suitable candidate for the targeted radiotherapy of bone metastases and should be further investigatedThis work was financially supported by China National Natural Science Foundation Grant No 20671065 Specialized Research Fund for the Doctoral Program of Higher Education China Grant No 20030610016 and Science and Technology Tackle Key Problem Program of Sichuan Province China Grant No 006Z02033
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