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研发多巴胺D4受体显像剂,采用“一锅两步法”制备了一种潜在的多巴胺D4受体PET显像剂3-(4-[18F]氟苄基)-8,9-二甲氧-基1,2,3,4-四氢苯并吡喃[3,4-c]吡啶-5-酮(18F-FDTP),并用高效液相色谱法进行了分离纯化。其合成时间为105 min,放射化学产率为19.8%(衰变校正),纯化后放射化学纯度大于97%,比活度大于6.3×104PBq/mol。通过体外受体竞争结合分析,测定FDTP对多巴胺D4受体的亲和常数为8.1 nmol/L,对D2,D3受体的亲和常数分别大于5800,3000 nmol/L;通过分配实验,测得其脂水分配系数为0.85。初步的体外研究显示,18F-FDTP有希望用于D4受体显像,但还需经进一步试验证实。
To develop a dopamine D4 receptor imaging agent, a potential dopamine D4 receptor PET imaging agent 3- (4- [18F] fluorobenzyl) -8,9- Dimethoxy-1,2,3,4-tetrahydrobenzopyrano [3,4-c] pyridin-5-one (18F-FDTP) was isolated and purified by high performance liquid chromatography. The synthetic time was 105 min and the radiochemical yield was 19.8% (decay correction). The purified radiochemical purity was more than 97% and the specific activity was more than 6.3 × 104PBq / mol. The binding affinity of FDTP to dopamine D4 receptor was determined to be 8.1 nmol / L and the affinity constants of D2 and D3 receptors were greater than 5800 and 3000 nmol / L, respectively. The fat-water partition coefficient is 0.85. Preliminary in vitro studies have shown that 18F-FDTP promising for D4 receptor imaging, but still need further confirmed by the experiment.