Synthesis and evaluation of 99mTc(CO)3-DTPA-folate as a folate-receptor-targeted radiopharmaceutical
Synthesis and evaluation of 99mTc(CO)3-DTPA-folate as a folate-receptor-targeted radiopharmaceutical
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DOI：
10.1016/s0969-8051(02)00310-4
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发表时间：
2002-07-01
影响因子：
3.1
通讯作者：
Green, MA
中科院分区：
文献类型：
--
作者：
Trump, DP;Mathias, CJ;Green, MA
通过在先前报道的 DTPA-叶酸缀合物的水溶液中加热 [Tc-99m]Tc(CO)(3)(H2O)(3)(+) 制备叶酸受体靶向 Tc-99m-放射性药物 [Tc-99m]Tc (CO)(3)DTPA-叶酸。该放射性示踪剂经过 HPLC 纯化（> 98% 放射化学纯度），并作为靶向叶酸受体阳性细胞的试剂进行体外和体内评估，[Tc-99m]Tc(CO)(3)DTPA-叶酸在人 KB 肿瘤细胞中经历了高叶酸受体特异性摄取。对携带 KB 细胞肿瘤异种移植物的无胸腺小鼠静脉注射 [Tc-99m]Tc(CO)(3)DTPA-叶酸，导致注射后 30 分钟和 4 小时 Tc-99m 肿瘤摄取分别为 1.8 +/- 0.5 和 3.3 +/- 0.2%ID/g (n = 3)。当叶酸与静脉内[Tc-99m]Tc(CO)(3)DTPA-叶酸共同给药时，肿瘤摄取减少。与叶酸受体介导的放射性药物定位一致。 (C) 2002 Elsevier Science Inc. 保留所有权利。
A folate-receptor-targeted Tc-99m-radiopharmaceutical, [Tc-99m]Tc (CO)(3)DTPA-folate, was prepared by heating [Tc-99m]Tc(CO)(3)(H2O)(3)(+) in an aqueous solution of the previously reported DTPA-folate conjugate. The radiotracer was HPLC purified (> 98% radiochemical purity) and evaluated in vitro and in vivo as an agent for targeting folate-receptor-positive cells, [Tc-99m]Tc(CO)(3)DTPA-folate experienced high, folate-receptor-specific uptake in human KB tumor cells. Intravenous administration of [Tc-99m]Tc(CO)(3)DTPA-folate to athymic mice bearing KB cell tumor xenografts resulted in Tc-99m tumor uptake of 1.8 +/- 0.5 and 3.3 +/- 0.2%ID/g (n = 3) at 30 minutes and 4 hours post-injection, respectively. Tumor uptake was reduced when folic acid was co-administered with the intravenous [Tc-99m]Tc(CO)(3)DTPA-folate. consistent with radiopharmaceutical localization being mediated by the folate receptor. (C) 2002 Elsevier Science Inc. All rights reserved.