目的　 7 氮杂吲哚的衍生物L 74 5 ,870是一个新的、高亲和性 (Ki=0 4 3nmol·L-1)的多巴胺D4受体选择性配体 ,我们放化合成了其类似结构的新化合物 3 [4 (4 [18F]氟苯甲基 )哌嗪 1 基 ] 甲基 1H 吡咯并 [2 ,3 b]吡啶 ([18F]C) ,并作了大鼠体内生物学评价。方法　 ([18F]C)的放化合成是通过 3 (哌嗪 1 基 )甲基 1H 吡咯并 [2 ,3 b]吡啶和 4 氟[18F]苯甲醛的胺烷基化反应完成 ,放化产率为 9 0 %～12 0 % ,放化纯度大于 98% ,比活度高于 37GBq·mol-1。结果　额叶皮质、海巴和延髓等脑区有较高的放射性摄取率 ,分别为 0 4 3%ID/ g和 0 35 %ID/g ;而纹状体、小脑处放射性摄取率较低。结论　大鼠体内的组织分布和代谢物研究表明 :[18F]C在大鼠脑组织区域有特异性分布 ,暗示其可能作为适合的显像剂用于多巴胺D4受体的体内研究 Purpose 7 The novel azaserindine derivative L 74 5,870 is a new dopamine D4 receptor selective ligand with high affinity (Ki = 0 4 3 nmol·L -1). We synthesized A novel compound 3 of similar structure was synthesized and characterized in rat in vivo biology [4 (4 [18F] fluorobenzyl) piperazine 1yl] methyl 1H pyrrolo [2,3bi] pyridine ([18F] C) Evaluation. The radiochemical synthesis of the method ([18F] C) was accomplished by amine alkylation of 3 (piperazinyl1yl) methyl1Hpyrrolo [2,3b] pyridine and 4fluoro [18F] benzaldehyde, The yield was 90% ~ 120%, the radiochemical purity was greater than 98%, and the specific activity was higher than 37GBq · mol-1. Results The brain regions of the frontal cortex, haiba and medulla oblongata had higher radioactive uptake rates of 0 43% ID / g and 0 35% ID / g, respectively. However, the radioactivity uptake in striatum and cerebellum was lower. Conclusions Tissue distribution and metabolite studies in rats show that [18F] C has a specific distribution in rat brain regions, suggesting that it may serve as a suitable imaging agent for the in vivo study of dopamine D4 receptors