摘要
设计并合成了一种18 F标记哒嗪酮类似物:2-特丁基-4-氯-5-(2-氟[18 F]乙氧基)-2H-3-哒嗪酮(18 F-FP2),通过生物分布实验评价了其用于心肌灌注显像的可行性。18 F-FP2的总制备时间为70～90min,校正后的放化产率为53.0%±5.2%,放化纯度>98%;18F-FP2为脂溶性化合物,在水溶液中可稳定放置3h以上。生物分布实验结果显示,18F-FP2在肝、肺中初期摄取高,注射后2min分别为(14.53±2.36)%ID/g和(33.69±10.79)%ID/g,但清除很快,注射后15min,其肝、肺的清除率已分别达57.7%和86.2%。18 F-FP2的心肌摄取较低,最高摄取值为(4.09±0.53)%ID/g(注射后2min)。这可能因标记侧链上未带苯环造成的,说明哒嗪酮侧链的芳环结构对心肌的摄取与滞留有较大影响。
A fluorine-18labeled pyridazinone derivative：2-tert-butyl-4-chloro-5-（2-[18F]fluroethoxy）-2H-pyridazin-3-one（18F-FP2）was designed and prepared as a potential myocar- dial perfusion imaging agent.The total radio-synthesis time was 70-90min,typical decay-corrected radiochemical yield was 53.0%±5.2%,and the radiochemical purities were 98%after purification.It is a lipophilic compound,and stable in water for 3h.The results of biodistribution studies in mice showed that 18F-FP2had high liver and lung uptake at initial post-injection time,the uptake was（14.53±2.36）%ID/g and（33.69±10.79）%ID/g at 2min post-injection,respectively.Radioactivity was washed out very fast from liver and lung,the rate of clearance was 57.7%and 86.2%at 15min post-injection,respectively. However the heart uptake of 18F-FP2was very low,the highest heart uptake was（4.09± 0.53）%ID/g at 2min post-injection.This may due to the removing of phenyl group in the labeling sidechain of pyridazinone,indicating that the aromatic ring has strong influence on the heart uptake and retention.
出处
《同位素》
CAS
2013年第1期23-28,共6页
Journal of Isotopes
基金
国家自然科学基金资助项目(20871020
21271030)
北京市自然科学基金资助项目(2092018)
