一种用于 Ga 正电子发射断层扫描的螯合剂：[Ga][Ga(BnDT3A)(OH)]中氢氧化物的配位增加了生物稳定性。
, a Chelator for Ga Positron Emission Tomography: Hydroxide Coordination Increases Biological Stability of [Ga][Ga(BnDT3A)(OH)].
机构信息
Department of Imaging Chemistry and Biology, School of Biomedical Engineering and Imaging Sciences, King's College London, London SE1 7EH, U.K.
Department of Biomedical Sciences, University of Hull, Cottingham Road, Hull HU6 7RX, U.K.
出版信息
Inorg Chem. 2022 Oct 31;61(43):17059-17067. doi: 10.1021/acs.inorgchem.2c01992. Epub 2022 Oct 17.
The chelator was used to produce a novel Ga complex for positron emission tomography (PET). Unusually, this system is stabilized by a coordinated hydroxide in aqueous solutions above pH 5, which confers sufficient stability for it to be used for PET. complexes Ga in a hexadentate manner, forming a complex with log ([Ga()]) = 18.25. Above pH 5, the hydroxide ion coordinates the Ga ion following dissociation of a coordinated amine. radiolabeling displayed a pH-dependent speciation, with [Ga][Ga()(OH)] being formed above pH 5 and efficiently radiolabeled at pH 7.4. Surprisingly, [Ga][Ga()(OH)] was found to show an increased stability (for over 2 h in fetal bovine serum) compared to [Ga][Ga()]. The biodistribution of [Ga][Ga()(OH)] in healthy rats showed rapid clearance and excretion the kidneys, with no uptake seen in the lungs or bones.
螯合剂用于合成一种新型的正电子发射断层扫描（PET）用镓配合物。不同寻常的是，该体系在 pH 值高于 5 的水溶液中由配位的氢氧化物稳定，这使其具有足够的稳定性，可用于 PET。该配合物以六配位的方式稳定 Ga ，形成一个 log([Ga()]）=18.25 的配合物。在 pH 值高于 5 时，氢氧根离子在配位的胺解离后与 Ga 离子配位。放射性标记显示出 pH 值依赖性的形态，在 pH 值高于 5 时形成[Ga][Ga()(OH)]，在 pH 值为 7.4 时能有效进行放射性标记。令人惊讶的是，与[Ga][Ga()]相比，[Ga][Ga()(OH)]显示出了稳定性的提高（在胎牛血清中超过 2 小时）。[Ga][Ga()(OH)]在健康大鼠中的生物分布显示出肾脏的快速清除和排泄，肺部和骨骼均未见摄取。
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