采用 (68)Ga 接近“Kit-Type”标记：DATA 螯合剂。
Approaching 'Kit-Type' Labelling with (68)Ga: The DATA Chelators.
机构信息
Institute of Nuclear Chemistry, Johannes Gutenberg University, Fritz-Strassmann-Weg 2, 55128 Mainz (Germany).
Department of Chemistry, Durham University, South Road, Durham, DH1 3LE (UK).
出版信息
ChemMedChem. 2015 Jun;10(6):1019-26. doi: 10.1002/cmdc.201500092. Epub 2015 Apr 21.
The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators--DATA(M), DATA(P), DATA(Ph), and DATA(PPh)--with (68)Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using (68)Ga positron emission tomography (PET).
DATA 螯合剂是一类新型的三阴离子配体，基于 6-氨基-1,4-二氮杂环丁烷-三乙酸，最近被引入用于（68）Ga 的螯合。与基于环笼支架的大环螯合剂（即 DOTA、DO3A 和 DO2A 衍生物）相比，DATA 螯合剂在更温和的条件下更快速地进行定量放射性标记。在这项研究中，对四种 DATA 螯合剂-DATA(M)、DATA(P)、DATA(Ph)和 DATA(PPh)-与（68）Ga 的标记进行了系统评估。结果突出了这种新型螯合剂在使用（68）Ga 正电子发射断层扫描（PET）进行分子成像方面的非凡潜力。
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