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目的:观察脑内β淀粉样蛋白的PET显像剂[11C]6-OH-BTA-1在SD大鼠体内药动学特征和对转基因痴呆小鼠、猕猴的活体显像。方法:①SD大鼠给药后不同时间点(每个时间点为一组),分别取血和心、肝、脾、肺、肾、脑(额叶、颞顶叶、枕叶、小脑和脑干)脏器,测定放射性计数并称重,计算经体重校正后每个时间点的每克组织注射剂量百分数(%ID-kg/g)。②转基因型痴呆小鼠和猕猴静脉给药后,使用PET/CT扫描,勾画出在各器官容积感兴趣区(VOI)的放射性计数。结果:①给药后,SD大鼠血和肺放射性早期摄取较多,但清除迅速,主要通过肝脏代谢。注射后20min时的器官内放射性分布从高至低分别为:肝、肺、肾、血、脾、心。②转基因型痴呆小鼠、正常老龄对照组小鼠和正常猕猴均有明显的肝脏放射性聚积,肾脏中度显影,但脑内未见两组鼠间差异有统计学意义。结论:[11C]6-OH-BTA-1通过血液循环,快速在SD大鼠、转基因型痴呆小鼠和猕猴脑内清除。
OBJECTIVE: To observe the pharmacokinetics of [11C] 6-OH-BTA-1, a beta-amyloid PET imaging agent in brain, and the in vivo imaging of transgenic dementia mice and macaques. Methods: ①SD rats were sacrificed at different time points (one group at each time point), blood and heart, liver, spleen, lung, kidney and brain (frontal, temporal parietal, occipital, cerebellum and brain Dry) organ, radioactive counts were measured and weighed, and the percent of injected dose per gram of tissue (% ID-kg / g) at each time point after body weight correction was calculated. ② After dextran-induced mice and cynomolgus vein administration, PET / CT scans were used to map the radioactive counts in the volume of interest (VOI) of each organ. Results: ①After administration, the early radioactivity of blood and lungs of SD rats were more, but cleared rapidly, mainly through the liver metabolism. 20min after injection of radioactive organ distribution from high to low were: liver, lung, kidney, blood, spleen, heart. ②Transgenic dementia mice, normal aging control mice and normal cynomolgus monkeys have obvious liver radioactive accumulation, moderate renal development, but no significant difference between the two groups in the brain was statistically significant. CONCLUSION: [11C] 6-OH-BTA-1 is rapidly cleared by circulating blood in SD rats, transgenic dementia mice and rhesus monkeys.