DEVELOPMENT OF F-18 LABELED FLUOROERYTHRONITROIMIDIZOLE AS A PET AGENT FOR IMAGING TUMOR HYPOXIA
DEVELOPMENT OF F-18 LABELED FLUOROERYTHRONITROIMIDIZOLE AS A PET AGENT FOR IMAGING TUMOR HYPOXIA
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DOI：
10.1148/radiology.194.3.7862981
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发表时间：
1995-03-01
期刊：
影响因子：
19.7
通讯作者：
PODOLOFF, DA
中科院分区：
文献类型：
--
作者：
YANG, DJ;WALLACE, S;PODOLOFF, DA
目的：开发一种亲水配体，用于在正电子发射断层扫描 (PET) 中对肿瘤缺氧进行成像。 材料和方法：在三只患有乳腺肿瘤的大鼠中，通过 PET 和放射自显影测定氟 18 标记的氟赤硝基咪唑 (FETNIM) 和 F-18 标记的氟米索硝唑 (FMISO) 的生物分布。测定 FETNIM、FMISO 和米索硝唑的分配系数。 结果：F-18 标记的 FETNIM 在 1、2 和 4 小时的生物分布显示，肿瘤与血液的比率分别为 2.29 +/- 0.599、2.41 +/- 0.567 和 8.02 +/- 2.420，肿瘤与肌肉的比率分别为分别为 0.66 +/- 0.267、2.11 +/- 0.347 和 5.92 +/- 2.240。注射后 4 小时，F-18 标记的 FETNIM 的肿瘤与血液计数密度比显着高于 F-18 标记的 FMISO。放射自显影照片表明，两种药物都可以帮助区分肿瘤中的缺氧区域和坏死区域。结论：F-18 标记的 FETNIM 可以帮助检测肿瘤缺氧，并且比 F-18 标记的 FMISO 更容易制备、成本更低且更亲水。
PURPOSE: To develop a hydrophilic ligand to image tumor hypoxia at positron emission tomography (PET).MATERIALS AND METHODS: Biodistribution of fluorine-18-labeled fluoroerythronitroimidazole (FETNIM) and F-18-labeled fluoromisonidazole (FMISO) was determined at PET and autoradiography in three mammary-tumor-bearing rats. The partition coefficient of FETNIM, FMISO, and misonidazole was determined.RESULTS: Biodistribution of F-18-labeled FETNIM at 1, 2, and 4 hours showed tumor-to-blood ratios of 2.29 +/- 0.599, 2.41 +/- 0.567 and 8.02 +/- 2.420, respectively, and tumor-to-muscle ratios of 0.66 +/- 0.267, 2.11 +/- 0.347, and 5.92 +/- 2.240, respectively. The tumor-to-blood count density ratio with F-18-labeled FETNIM at 4 hours after injection was significantly higher than with F-18-labeled FMISO. Autoradiographs indicated that both agents could help differentiate hypoxic versus necrotic region in the tumor.CONCLUSION: F-18-labeled FETNIM can help detect tumor hypoxia and is easier to prepare, less costly, and more hydrophilic than F-18-labeled FMISO.