99mTc-树枝状聚酰胺-胺-叶酸偶联物的放射性合成及微 SPECT 成像。
Radiosynthesis and micro-SPECT imaging of 99mTc-dendrimer poly(amido)-amine folic acid conjugate.
机构信息
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, 2019 BaoJia Road, Shanghai 201800, PR China.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):927-31. doi: 10.1016/j.bmcl.2009.12.075. Epub 2009 Dec 24.
Acetylated (Ac) dendrimer poly(amido)-amine (PAMAM) generation 5 (G5) reacted with folic acid (FA), followed by reacting with 2-(p-isothiocyanatobenzyl)-6-methyl-diethylenetria minepentaacetic acid (1B4M DTPA) to form the conjugate of Ac-G5-FA-1B4M DTPA which was further radiolabeled with (99m)Tc. The radiochemical yield is up to 98.9% with excellent in vitro/in vivo stability, rapid blood clearance and certain tumor accumulation which was further confirmed by micro-SPECT imaging study.
乙酰化（Ac）树枝状聚酰胺-胺（PAMAM）第五代（G5）与叶酸（FA）反应，然后与 2-（对异硫氰酸苄基）-6-甲基-二乙三胺五乙酸（1B4M DTPA）反应，形成 Ac-G5-FA-1B4M DTPA 缀合物，进一步用（99m）Tc 标记。放射性化学产率高达 98.9%，具有优异的体外/体内稳定性、快速的血液清除率和一定的肿瘤积累，这进一步通过 micro-SPECT 成像研究得到证实。
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