摘要 前列腺特异性膜抗原（PSMA，prostate specific membrane antigen）在大多数前列腺癌细胞中是高表达的，且其过度表达情况与前列腺癌变的位置、发展和转移情况有着强烈的对应关系，因而成为前列腺癌诊断和治疗的研究热点。为了探索性质更加优异的新型的前列腺癌显像剂，本文以PSMA为靶向蛋白，以与PSMA具有高度亲和性的赖氨酸-谷氨酸-脲（lysine-glutamate urea）结构为基本骨架，设计合成了一种新型的氨荒酸盐类PSMA小分子抑制剂（化合物6），并对其进行了99mTcN和99mTcO两种中心核的标记。在0.1 mg配体、pH= 6、100oC条件下通过配体交换反应得到标记率大于95%的99mTcN-6配合物；在0.1 mg配体、pH= 6、100℃条件下通过配体交换反应得到标记率大于90%的99mTcO-6配合物。这两种配合物在室温下放置6 h后标记率仍大于90%，在小鼠血清37oC孵育后99mTcN-6配合物和99mTcO-6配合物的放化纯分别降为80%和75%，脂水分配系数测定表明这两种配合物均为水溶性物质。有关该化合物的其他生物性能还会进一步进行研究。

Prostate specific membrane antigen (PSMA) is transmembrane glycoprotein. It is the research focus in the diagnosis and treatment of prostate cancer because of the strong relationship between its excessive expression in prostate cancer cells and the location, development and transfer of the prostate cancer. In order to explore new prostate cancer imaging agents with a more excellent property, this article is designed to synthesize a new type of PSMA inhibitor, ligand 6 which targets at PSMA protein, uses lysine - glutamate urea structure as the basic frame because of it’s strong affinity with PSMA, transfers into dithiocarbamate. Ligand 6 was labeled with 99mTcN and 99mTcO cores. Complexes 99mTcN-6 successfully obtained with more than 95% radiochemical purity by optimizing the radiochemical conditions, and 99mTcO-6 was obtained no less than 90%. These two complexes exhibited good in vitro stability. The result of partition coefficient study revealed that 99mTcN-6 and 99mTcO-6 were both hydrophilic. By the way, their biological properties will be estimated by further experiments and studies.