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Preparation and biological evaluation of 166Ho-BPAMD as a potential therapeutic bone-seeking agent

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Abstract

In this work 166Ho-(4-{[(bis(phosphonomethyl))carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid (166Ho-BPAMD) complex was prepared successfully with sufficient radiochemical purity of >94 % and specific activity of 244 GBq/mmol at the optimized conditions. The complex demonstrated significant stability at room temperature and in human serum at least for 24 h. Hydroxyapatite (HA) binding assay demonstrated that even at the small amount of HA, >10 mg, above 98 % of the complex is bound to HA. At the pH 7.4, LogP0/w was −1.73 ± 0.02. Both planar imaging and biodistribution studies showed major accumulation of the labelled compound in the bone tissue.

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Authors and Affiliations

  1. Nuclear Science and Technology Research Institute (NSTRI), 14155-1339, Tehran, Iran

    Hassan Yousefnia, Samaneh Zolghadri & Ali Bahrami-Samani

  2. Faculty of Engineering, Science and Research Branch, Islamic Azad University (IAU), Tehran, Iran

    Naeimeh Amraei & Mohammad Hosntalab

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  1. Hassan Yousefnia
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  2. Naeimeh Amraei
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  3. Mohammad Hosntalab
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  4. Samaneh Zolghadri
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  5. Ali Bahrami-Samani
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Correspondence to Hassan Yousefnia.

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Yousefnia, H., Amraei, N., Hosntalab, M. et al. Preparation and biological evaluation of 166Ho-BPAMD as a potential therapeutic bone-seeking agent. J Radioanal Nucl Chem 304, 1285–1291 (2015). https://doi.org/10.1007/s10967-014-3924-1

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  • DOI: https://doi.org/10.1007/s10967-014-3924-1

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