Authors:
Yuanyou Yang Institute of Nuclear Science and Technology, Sichuan University Key Laboratory of Radiation Physics and Technology (Sichuan University), Ministry of Education Chengdu 610064 People’s Republic of China

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Ning Liu Institute of Nuclear Science and Technology, Sichuan University Key Laboratory of Radiation Physics and Technology (Sichuan University), Ministry of Education Chengdu 610064 People’s Republic of China

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Jiali Liao Institute of Nuclear Science and Technology, Sichuan University Key Laboratory of Radiation Physics and Technology (Sichuan University), Ministry of Education Chengdu 610064 People’s Republic of China

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Manfei Pu Institute of Nuclear Physics and Chemistry, CAEP Mianyang 621900 People’s Republic of China

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Yebin Liu Institute of Nuclear Physics and Chemistry, CAEP Mianyang 621900 People’s Republic of China

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Min Wei Institute of Nuclear Science and Technology, Sichuan University Key Laboratory of Radiation Physics and Technology (Sichuan University), Ministry of Education Chengdu 610064 People’s Republic of China

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Jiannan Jin Institute of Nuclear Science and Technology, Sichuan University Key Laboratory of Radiation Physics and Technology (Sichuan University), Ministry of Education Chengdu 610064 People’s Republic of China

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Abstract  

In this paper, 3-amino-1-hydroxypropylidene-1,1-bisphosphonate(APB), a amidobisphophonate was synthesized and labeled with the α-emitter 211At by an indirect method using N-succinimidyl 5-(tributylstannyl)-3-pyridinecarboxylate (SPC) as a bi-functional linker, and the conjugated amidobisphophonate (211At-SAPC-APB) was preliminarily evaluated in vitro and in vivo by comparison with free astatide (211At) and 99mTc-MDP. 3-amino-1-hydroxypropylidene-1,1-bisphosphonate(APB) was prepared using β-alanine as the starting material. With SPC bi-functional linker, APB was conjugated with 211At in a labeling yield of 80–90% with radiochemical purity of more than 99%. The conjugated amidobisphophonate (211At-SAPC-APB) exhibited considerable stability in vitro, in that the radiochemical purity of 211At-SAPC-APB was still more than 98% in 0.1 mol/L PBS (pH 7.6) or in fetal calf serum, even stayed for 24 h at room temperature (RT). Biodistribution of 211At-SAPC-APB was investigated in NIH strain mice by I.V injection. The results showed that 211At-SAPC-APB could rapidly locate in shank, with the maximum uptake of 23.70 ± 2.29% I.D/g at 6 h, earlier than that of 99mTc-MDP at 12 h, and stayed in the bone for long time. Moreover, 211At-SAPC-APB 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 211At-SAPC-APB was constantly stable in vivo as well as in vitro. These results indicated that 211At-SAPC-APB will be a suitable candidate for the targeted radiotherapy of bone metastases and should be further investigated.

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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation
1968
Volumes
per Year
1
Issues
per Year
12
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)