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Synthesis and biological evaluation of fatty acid derivatives for myocardial imaging containing [99mTc(CO)3]+

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Abstract

Radiolabeled fatty acids as myocardial metabolic agent are used for detecting ischemic heart disease, however, no 99mTc-labeled fatty acids have potential use in clinical diagnosis. In this work, five fatty acid analogues labeled with 99mTc were firstly synthesized and characterized, their biological behaviors were investigated. All Radiotracers had good stability when incubated in rat serum for 3 h at 37 °C. 99mTc -CpT-12-ODPPA (8b) showed higher initial myocardial uptake (8.17% ID/g at 1 min postinjection) and good heart/blood ratio (2.58 at 30 min postinjection). 99mTc-11-dpa-OUFA (2b) as positively charged lipophilic compounds had reasonable heart uptake (5.59% ID/g at 1 min postinjection) and good retention (1.89% ID/g at 60 min postinjection). Unfortunately, no great improvement was obtained by the five 99mTc-labeled fatty acid analogues for the short myocardial retention and poor heart/liver ratios.

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Acknowledgment

We gratefully acknowledged the Significant New Drugs Development (Grant No. 2014ZX09507007001), Natural Science Foundation of China (No. 21371026) and Science and Technology Support Program (No. 2014BAA03B03) for financial support.

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Authors and Affiliations

  1. Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, 100875, China

    Jianping Liu, Shuxia Wang, Huan Wang, Lei Yin, Qianqian Xue, Dawei Wang, Yu Fang & Huabei zhang

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  1. Jianping Liu
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  2. Shuxia Wang
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  3. Huan Wang
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  4. Lei Yin
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  5. Qianqian Xue
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  8. Huabei zhang
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Correspondence to Huabei zhang.

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Liu, J., Wang, S., Wang, H. et al. Synthesis and biological evaluation of fatty acid derivatives for myocardial imaging containing [99mTc(CO)3]+ . J Radioanal Nucl Chem 312, 543–555 (2017). https://doi.org/10.1007/s10967-017-5258-2

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  • DOI: https://doi.org/10.1007/s10967-017-5258-2

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