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Radio synthesis and in vivo evaluation of two α7 nAChRs radioligands: [125I]CAIPE and [125I]IPPU

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Abstract

The radio synthesis and in vivo evaluation of two α7 nAChRs radioligands [125I]CAIPE and [125I]IPPU were reported. They were obtained from their tributyltin precursors with high radio chemical yields (>90 %) and good radio chemical purities (>95 %). Biodistribution and blockade studies of [125I]CAIPE showed that the accumulation of radioactivity in the mouse brain was specific and selective.

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Acknowledgments

This work was financially supported by Natural Science Foundation of China (No. 21371026), Science and Technology Support Program (No. 2014BAA03B03), Sinificant New Drugs Development (Grant No. 2014ZX09507007).

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Authors and Affiliations

  1. Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, No. 19, Xinjiekouwai Street, Haidian District, Beijing, 100875, People’s Republic of China

    Aiqin Wu, Xiang Li, Qianqian Xue, Xi Yan & Huabei Zhang

  2. Pfizer Investment Co., Ltd, 11F, Tower B, Minmetals Plaza, No. 3-7 North Chao Yang Men Avenue, Dongcheng District, Beijing, 100010, People’s Republic of China

    Yongjuan Liu

  3. Beijing An Zhen Hospital of the Capital University of Medical Sciences, No. 2, Anzhen St., Chaoyang District, Beijing, 100029, People’s Republic of China

    Xia Lu

Authors
  1. Aiqin Wu
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  2. Xiang Li
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  3. Qianqian Xue
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  4. Yongjuan Liu
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  5. Xia Lu
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  6. Xi Yan
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  7. Huabei Zhang
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Correspondence to Huabei Zhang.

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Wu, A., Li, X., Xue, Q. et al. Radio synthesis and in vivo evaluation of two α7 nAChRs radioligands: [125I]CAIPE and [125I]IPPU. J Radioanal Nucl Chem 307, 1345–1351 (2016). https://doi.org/10.1007/s10967-015-4235-x

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  • DOI: https://doi.org/10.1007/s10967-015-4235-x

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