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Issue 8, 2013
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Synthesis, characterization and biodistribution of new fatty acids conjugates bearing N,N,N-donors incorporated [99mTc/Re(CO)3]+

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Abstract

[99mTc(CO)3]+-6-[N-(2-dipicolyl)amino]hexanoic acid (1a) and [99mTc(CO)3]+-11-[N-(2-dipicolyl)amino]undecanoic acid (1b) were prepared by incorporating [99mTc-(CO)3]+ into 6-[N-(2-dipicolyl)amino]hexanoic acid and 11-[N-(2-dipicolyl)amino]undecanoic acid, respectively. The overall radiochemical yield of 1a and 1b was from 79.7% to 91.3% and radiochemical purity after HPLC purification was more than 94%. The resulting complexes were found to be chemically stable when incubated in SD rat serum for 3 h at 37 °C. Tissue distribution studies in normal mice showed that high initial uptake of Tc-99m complexes were observed, followed by slow clearance from the heart. The maximum heart-to-blood ratio of 1a was 1.46 at 60 min, but 1b showed a poor heart-to-blood ratio. By estimating the tissue distribution and the computing result of the molar volume and the solvation free energy of Tc-99m chelating groups, a small-size and monocationic Tc-99m core is very important to enhance the myocardial accumulation and low liver uptake for the fatty acid tracers.

Graphical abstract: Synthesis, characterization and biodistribution of new fatty acids conjugates bearing N,N,N-donors incorporated [99mTc/Re(CO)3]+

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Publication details

The article was received on 19 Oct 2012, accepted on 10 Dec 2012 and first published on 10 Dec 2012


Article type: Paper
DOI: 10.1039/C2DT32492J
Citation: Dalton Trans., 2013,42, 2894-2901
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    Synthesis, characterization and biodistribution of new fatty acids conjugates bearing N,N,N-donors incorporated [99mTc/Re(CO)3]+

    H. Zeng, L. Zhao, S. Hu, Y. Liu, H. Yu, N. Chen and H. Zhang, Dalton Trans., 2013, 42, 2894
    DOI: 10.1039/C2DT32492J

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