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首页> 外文期刊>RSC Advances >Synthesis and characterization of lipophilic cationic Ga(III) complexes based on the H(2)CHXdedpa and H(2)dedpa ligands and their Ga-67/68 radiolabeling studies
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Synthesis and characterization of lipophilic cationic Ga(III) complexes based on the H(2)CHXdedpa and H(2)dedpa ligands and their Ga-67/68 radiolabeling studies

机译：基于H（2）Chxdedpa和H（2）Defpa配体及其Ga-67/68放射性标记研究的亲脂性阳离子Ga（III）配合物的合成与表征

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Ga-68 is an attractive isotope for incorporation into a positron-emission tomography (PET) imaging agent, and is finding use as an alternative generator-produced isotope to Tc-99m particularly in imaging of myocardial perfusion. We have synthesized six new chelating ligands based on our previously reported H(2)dedpa and H(2)CHXdedpa scaffolds (CHX = cyclohexyl, H(2)dedpa = 1,2-[[ carboxypyridin-2-yl] methylamino] ethane). These ligands are designed to incorporate several lipophilic appendages at the secondary nitrogens, and upon coordination to Ga-68(III) will form lipophilic, cationic complexes designed to mimic the properties of other clinically relevant myocardial perfusion imaging agents. The non-radioactive Ga(III) complexes were prepared and characterized by NMR spectroscopy; each ligand retained its predicted hexadentate N4O2 binding to Ga(III). The radiolabeling properties of the six ligands were assessed using the longer-lived Ga-68 surrogate, Ga-67. The absence of 'free' uncomplexed Ga-67 in the HPLC radio-chromatograms indicated > 99% radiochemical yields (10 minutes at ambient temperature, ligand concentrations of 10(-4) M). However, the N, N'-benzyl functionalized derivatives displayed multiple peaks corresponding to the presence of additional Ga-67-complexes which complicated further study. Selected Ga-67-CHXdedpa complexes were tested for in vitro stability against the metal-binding protein apo-transferrin, and were found to be sufficiently stable (> 80%) in a 2 h challenge assay, suggesting that alternative N, N'-alkylated derivatives which introduce more lipophilic character will be of interest in future studies.
机译：Ga-68是一种有吸引力的同位素，用于掺入正电子发射断层扫描（PET）成像剂，并以替代发生器产生的同位素的用途，特别是在心肌灌注的成像中。我们已经基于先前报道的H（2）DEDPA和H（2）CHXDEDPA支架（CHX =环己基，H（2）DEDPA = 1,2 - [α-甲基氨基]乙烷乙烷基于六种新的螯合配体）。这些配体被设计成在二次氮的中掺入几种亲脂性阑尾，并且在与Ga-68（III）的协调后，将形成亲脂性的阳离子复合物，该阳离子复合物设计用于模拟其他临床相关的心肌灌注成像剂的性质。制备非放射性Ga（III）配合物，其特征在于NMR光谱;每个配体保留其预测的六向N4O2与Ga（III）结合。使用较长寿命的GA-68替代Ga-67评估六配体的放射性标记性质。没有在HPLC无线电图中没有“自由”未复合的GA-67，表明> 99％的放射化学产率（在环境温度下10分钟，10（-4）M）。然而，N，N'-苄基官能化衍生物显示出对应于另外的GA-67-复合物的存在的多个峰，其复杂的进一步研究。测试的Ga-67-Chxdedpa复合物对金属结合蛋白APO-转移素的体外稳定性进行测试，并且发现在2小时攻击测定中足够稳定（> 80％），表明替代N，N'-引入更亲脂性特征的烷基化衍生物对未来的研究感兴趣。

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  • 来源
    《RSC Advances》 |2016年第105期|共11页
  • 作者

    Ramogida C. F.; Schindler D.; Schneider C.; Tan Y. L. K.; Huh S.; Ferreira C. L.; Adam M. J.; Orvig C.;

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    Univ British Columbia Dept Chem Med Inorgan Chem Grp 2036 Main Mall Vancouver BC V6T 1Z1 Canada;

    Univ British Columbia Dept Chem Med Inorgan Chem Grp 2036 Main Mall Vancouver BC V6T 1Z1 Canada;

    Univ British Columbia Dept Chem Med Inorgan Chem Grp 2036 Main Mall Vancouver BC V6T 1Z1 Canada;

    Univ British Columbia Dept Chem Med Inorgan Chem Grp 2036 Main Mall Vancouver BC V6T 1Z1 Canada;

    Univ British Columbia Dept Chem Med Inorgan Chem Grp 2036 Main Mall Vancouver BC V6T 1Z1 Canada;

    Nordion 4004 Wesbrook Mall Vancouver BC V6T 2A3 Canada;

    TRIUMF Life Sci Div 4004 Wesbrook Mall Vancouver BC V6T 2A3 Canada;

    Univ British Columbia Dept Chem Med Inorgan Chem Grp 2036 Main Mall Vancouver BC V6T 1Z1 Canada;

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