摘要
【摘要】目的应用国产多功能18F标记模块制备4一[18F]氟-3．三氟甲基苯甲酰基-谷氨酸一（RGD．苯丙氨酸一赖氨酸）环肽二聚体（4一18F-TFMB—E[C（RGDfk）2]），并用microPET观察其在肿瘤模型鼠内的生物分布。方法基于PET—MF．2V—IT—I多功能合成模块，采用“一锅法”完成4一18F．TFMB-E[C（RGDfk）：]的制备和纯化。荷人胰腺癌BxPC一3裸鼠给药后行microPET活体显像。结果4一18F—TFMB-E[c（RGDfk）2]放化产率为（27．4±2．3）％（衰减校正后），总合成时间为30min，无需HPLC法分离，放化纯〉98％。荷人胰腺癌BxPC一3裸鼠注射4一18F—TFMB．E[C（RGDfk），]后30、60和120min后肿瘤摄取值（％ID／g）分别为4．03±0．32、3．31±0．20和2．72±0．17；注射后30min肿瘤与对侧肌肉摄取值比值大于6（对侧肌肉摄取值为0．47±0．12）。4一18F．TFMB．E[C（RGDfk）：]主要经肝、肠排泄。结论4_18F·TFMB—E[C（RGDfk）：]自动化合成速度快、效率高，胰腺癌肿瘤模型显影清晰。
Objective To prepare 4-[18F] fluoro-3-trifluoromethylbenzoyl-E[ c（RGDfk） 2 ] （4-18F- TFMB-E [ c （RGDfk）2 ] ） using a domestic multifunctional lS F radiolabeling module and study the biodistri- bution of 4-18 F-TFMB-E [ c （RGDfk） 2 ] in tumor-bearing mice by micro PET. Methods PET-MF-2V-IT-I multifunctional synthesis module and “one-pot” radio-chemical procedure were applied for the synthesis and purification of 4-1SF-TFMB-E[ c（RGDfk） 2 ]- Nude mice bearing human pancreatic cancer BxPC-3 cells were imaged by micro PET after intravenous injection of 4-18 F-TFMB-E [ c （RGDfk）2 ] for biodistribution study. Re- sults The total synthesis duration was 30 min. The radiochemical yield of 4-TM F-TFMB-E [ c （RGDtk） 2 ] was （27.4±2.3 ） % （ decay corrected） and the radiochemical purity was more than 98% without HPLC purifi- cation. Tumor uptake of 4-18 F-TFMB-E [ c （RGDfk） ： ] was （ 4.03±0.32 ）, （ 3.31±0.20 ） and （ 2.72±0.17 ） % ID/g at 30, 60 and 120 min postinjeetion, respectively. The tumor/muscle uptake ratio was grea- ter than 6 （0.47±0.12, % ID/g in muscle） at 30 min postinjection. The predominant excretion pathway was via liver and intestine. The uptake of 4-1SF-TFMB-E[ c（ RGDfk）2 ] in liver and intestine was 2.08±0. 24 and 1.62±0. 24, respectively. Conclusions 4-1s F-TFMB-E [ c （RGDfk） 2 ] can be automatically and quickly synthesized with a high radiochemical yield and purity. The prepared 4-18 F-TFMB-E [ c（RGDfk） 21 might be a ootential agent for pancreatic tumor imaging.
出处
《中华核医学与分子影像杂志》
CSCD
北大核心
2012年第2期90-94,共5页
Chinese Journal of Nuclear Medicine and Molecular Imaging
作者简介
通信作者：杨敏，Email：yangmin@jsinm．org
