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合成并鉴定一种 (68)Ga 标记的 N-(2-二乙氨基乙基)苯甲酰胺衍生物作为恶性黑色素瘤潜在的正电子发射断层扫描 (PET) 探针。

Synthesis and characterization of a (68)Ga-labeled N-(2-diethylaminoethyl)benzamide derivative as potential PET probe for malignant melanoma.

机构信息

Radiation Instrumentation Research Division, Korea Atomic Energy Research Institute, Jeongeup, Republic of Korea.

出版信息

Bioorg Med Chem. 2012 Aug 15;20(16):4915-20. doi: 10.1016/j.bmc.2012.06.047. Epub 2012 Jul 6.

Abstract

Radiolabeled benzamides have been reported to be attractive agents for targeting malignant melanoma as they bind melanin and display high accumulation in melanoma cells. Herein, we report the synthesis and bioevaluation of a novel (68)Ga-labeled benzamide as a potential PET agent for malignant melanoma. The novel radiotracer was synthesized in good radiochemical yields (80% decay corrected yield) and high specific radioactivity (10 GBq/μmol). Cellular uptake of (68)Ga-SCN-NOTA-BZA was significantly higher in B16F10 cells (mouse melanoma) treated with L-tyrosine. Biodistribution and micro-PET studies of (68)Ga-SCN-NOTA-BZA in B16F10-bearing mice showed selective uptake into the tumor. The radiotracer was cleared via renal excretion without further metabolism. These results demonstrate that (68)Ga-SCN-NOTA-BZA is a potential PET probe for malignant melanoma.

摘要

放射性标记的苯甲酰胺被报道为靶向恶性黑色素瘤的有吸引力的药物,因为它们与黑色素结合并在黑色素瘤细胞中显示出高积累。在此,我们报告了一种新型(68)Ga 标记的苯甲酰胺的合成及其作为恶性黑色素瘤潜在 PET 试剂的生物评价。新型放射性示踪剂的放射性化学产率(校正后 80%衰变产率)和比放射性(10GBq/μmol)均较高。用 L-酪氨酸处理的 B16F10 细胞(小鼠黑色素瘤)中,(68)Ga-SCN-NOTA-BZA 的细胞摄取明显更高。(68)Ga-SCN-NOTA-BZA 在荷 B16F10 小鼠中的生物分布和 micro-PET 研究表明,放射性示踪剂选择性地进入肿瘤。放射性示踪剂通过肾脏排泄清除,没有进一步代谢。这些结果表明,(68)Ga-SCN-NOTA-BZA 是一种用于恶性黑色素瘤的潜在 PET 探针。

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