Raleigh J A, Franko A J, Treiber E O, Lunt J A, Allen P S
Int J Radiat Oncol Biol Phys. 1986 Jul;12(7):1243-5. doi: 10.1016/0360-3016(86)90268-3.
A hexafluorinated 2-nitroimidazole (CCI-103F) has been synthesized and its properties as a hypoxic cell binder investigated. The drug has a plasma half-life of 90 min in Balb/C mice and a tumor-to-plasma ratio of 0.8. Following sustained exposure to the drug and a washout period for the unbound drug, liver and tumor samples were excised. NMR investigation of the excised tissue in a 2.35 T animal sized NMR facility revealed the presence of 19F bound to both tissues. Further improvement in sensitivity is required to make 19F NMR detection of binding in situ feasible.
一种六氟代2-硝基咪唑(CCI-103F)已被合成,并对其作为缺氧细胞结合剂的性质进行了研究。该药物在Balb/C小鼠中的血浆半衰期为90分钟,肿瘤与血浆的比率为0.8。在持续暴露于该药物并对未结合药物进行洗脱期后,切除肝脏和肿瘤样本。在一个2.35 T动物尺寸的核磁共振设备中对切除组织进行核磁共振研究,结果显示两种组织中均存在与19F结合的情况。为了使19F核磁共振原位检测结合情况可行,需要进一步提高灵敏度。