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Synthesis and biodistribution of two novel 99mTc “3+1”mixed ligand complexes as potential brain perfusion agents

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Abstract

The research in the last decade has been mainly aimed at the development of technetium-99m radiopharmaceuticals, among which are the “3+1”mixed ligand complexes. Two novel [99mTc]“3+1”mixed ligand complexes each carrying the tridentate ligand, the N-(o-Methylthiophenyl)ethylenediamine or the N-(o-Methylthiophenyl)-b-mercaptoacetamide in combination with monothiolate coligand were produced using stannous chloride as reductant and glucoheptonate as transfer ligand. The identification of [99mTc]-6 and [99mTc]-7 was established by thin layer chromatography. The radiochemical purity of two complexes was over 90%. Biodistribution data in mice showed that both [99mTc]-6 and [99mTc]-7 can penetrate the intact blood-brain barrier and exhibited retention in mice brain. The brain uptakes (%ID/g) were 1.76, 1.17, 0.90 and 0.68, 0.38 ,0.37 at 2, 30, and 60 minutes i.v. postinjection for [99mTc]-6 and [99mTc]-7, respectively. Examples in this report comfirm us that it is promising to develop 99mTc complexes as potential brain perfusion agents based on modifying either the tridentate or the monodentate ligands.

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Authors and Affiliations

  1. College of Basic Science and Technology, Beijing Forestry University, Beijing, 100083, P.R. China

    Duan Xin-hong

  2. Department of Chemistry, Beijing Normal University, Beijing, 100875, P.R. China

    Lű Gong-xu & Wang Xue-bin

Authors
  1. Duan Xin-hong
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  2. Lű Gong-xu
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  3. Wang Xue-bin
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Xin-hong, D., Gong-xu, L. & Xue-bin, W. Synthesis and biodistribution of two novel 99mTc “3+1”mixed ligand complexes as potential brain perfusion agents. Journal of Radioanalytical and Nuclear Chemistry 260, 173–177 (2004). https://doi.org/10.1023/B:JRNC.0000027077.79336.7d

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  • DOI: https://doi.org/10.1023/B:JRNC.0000027077.79336.7d

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