摘要
目的 制备脂肪酸心肌显像剂 14 (R ,S) 氟 18 6 硫十七烷酸 ( 18F FTHA) ,并在小鼠体内进行初步评价。方法 以 8 溴 1 辛醇为原料 ,经醇氧化、丙基溴化镁格反应、水解、巯基取代、烷基化、酯化、酯水解等反应 ,合成标记前体FTHA OTs( 5 )。以氟化聚铵 (kryptofix/K + 18F)为亲核试剂 ,在乙腈溶液中与FTHA Cts( 5 )进行氟代亲核反应 ,经水解生成18F FTHA ,采用薄层层析 (TLC)和高效液相色谱 (HPLC)法检测放射化学纯度(RCP)。结果 RCP大于 92 % ,稳定性好。小鼠心肌摄取高 [( 2 8.70± 3.5 2 ) %ID/g ,10min],滞留时间长[( 18.6 3± 2 .98) %ID/ g ,12 0min],注药后 10和 12 0min的心 /血比值分别为 9.4 5和 17.2 5。结论 制备的18F FTHA放化纯高 ,稳定性好 。
Objective To prepare the myocardial fatty acid imaging agent 18 F FTHA and to investigate its biodistribution in mice. Methods The labeling precursor of benzyl 14(R,S) tosyloxy 6 thia hepatadecanoate(5) was synthesized by oxidation of 8 bromo 1 octanol, then by propyl magnesium bromide Grignard reaction, hydrolysis, substitution of bromide, alkylation, esterification and hydrolysis of ester. Using kryptofix/K+ 18 F as nucleophilic radiofluorination reagent in acetonitrile solution, stable 18 F FTHA was obtained after hydrolysis. Radiochemical purity(RCP) was determined by TLC and HPLC.Results The RCP was greater than 92% as dertemined by HPLC and was stable within 2 h. Biodistribution of 18 F FTHA in mice demonstrated that the myocardial uptake of 18 F FTHA was (28.70 ±3.52) % ID/g and (18.63±2.98) % ID/g at 10 min and 60 min, respectively. Heart/blood ratio at 10 and 120 min was 9.45 and 17.25, respectively. Conclusion The 18 F FTHA as prepared possesses high purity and good stability for preclinical study.
出处
《上海医学》
CAS
CSCD
北大核心
2004年第1期26-29,共4页
Shanghai Medical Journal
基金
江苏省医学重点人才"13 5"工程基金资助项目(RC2 0 0 2 0 68)
