^(18)F标记哒嗪酮类似物的制备及其在小鼠体内的生物分布  

Synthesis and Biodistribution of 2-tert-butyl-4-chloro-5-(2-[^(18)F]fluroethoxy)-2H-pyridazin-3-one

作　　者：彭程[1] 牟甜甜[2,3] 赵祚全[2] 马云川[1] 张现忠[2,4] 

机构地区：[1]首都医科大学宣武医院PET中心,北京100053 [2]放射性药物教育部重点实验室北京师范大学化学学院,北京100875 [3]首都医科大学附属北京安贞医院核医学科,北京100029 [4]分子影像暨转化医学研究中心厦门大学公共卫生学院,厦门361005

出　　处：《同位素》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)

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.

关 键 词：18F-FP2 哒嗪酮 心肌摄取 生物分布 

分 类 号：R817[医药卫生—影像医学与核医学] TQ464.7[医药卫生—放射医学]