高等学校化学学报Issue(3)：499-504,6.DOI:10.7503/cjcu20131061
多巴胺受体显像剂18 F-Fethypride的合成、放射性标记及生物分布
Synthesis, Label and Biodistribution of 18 F-Fethypride for Dopamine Receptor Imaging
摘要
Abstract
Dopamine is one of important neurotransmitters in the brain, many diseases of the nervous system is closely related to it. Developing the dopamine receptor imaging agents of strong specificity and high affinity is a hot topic in the field of molecular nuclear medicine. The precursor( S)-3-[5-{(1-ethylpyrrolidin-2-yl) methylcarbamoyly}-2 , 3-dimethoxy phenyl ] propyl-4-methyl benzemide was synthetized with vanillic acid methyl ester through seven steps, then radioactive compound 18 F-( S)-N-{(1-ethylpyrrolidin-2-yl) methyl}-3-(3-fluropropyl)-4, 5-dimethoxy benzamide(18F-Fethypride) was radiolabeled by 18F through nucleophilic sub-stitution reaction. Synthesis time was 35 min, radiochemical yield rate was ( 36.8±1.4 )%, radiochemical purity of HPLC was 99%, radiochemical purity of TLC was 100%. Sterility test limulus reagent test K2.2.2 content detection and acute toxicity test were all qualified. Biodistribution test showed that 18 F-Fethypride was metabolized through the liver, excreted through the renal, radioactivity gradually decreased with the extension of time. In brain tissue, radioactivity were mainly distributed in striatum, then in hippocampus, hypothalamus and cerebellum were lower. Striatum/cerebellum( Str/Cer) increased gradually, reached the highest at 90 min ( 10.68±0.35 ) . The results showed that 18 F-Fethypride was suit for the diagnosis of the nervous system disea-ses as dopamine receptor imaging agent.关键词
多巴胺受体显像剂/18 F放射性标记/生物分布Key words
Dopamine receptor imaging agent/18 F-labeling/Biodistribution分类
化学化工引用本文复制引用
李英华,王斌,关锋,代玉银,林承赫,陆景彬,林英杰..多巴胺受体显像剂18 F-Fethypride的合成、放射性标记及生物分布[J].高等学校化学学报,2014,(3):499-504,6.基金项目
国家卫生部吴阶平医学基金(批准号:320.6750.07127)资助.@@@@ Supported by the Wu Jieping Medical Fund of the Ministry of Health, China(No.320.6750.07127) （批准号:320.6750.07127）
