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Synthesis and evaluation of a novel 99mTc nitrido radiopharmaceutical with alendronate dithiocarbamate as a potential bone‐imaging agent
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-10-31 , DOI: 10.1111/cbdd.13117 Xiaoqing Song 1 , Yue Wang 1 , Junbo Zhang 1 , Zhonghui Jin 2 , Weifang Zhang 2 , Yanyan Zhang 2
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-10-31 , DOI: 10.1111/cbdd.13117 Xiaoqing Song 1 , Yue Wang 1 , Junbo Zhang 1 , Zhonghui Jin 2 , Weifang Zhang 2 , Yanyan Zhang 2
Affiliation
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Currently, a popular strategy for designing novel radioprobes as bone‐imaging agents is based on the concept of bifunctional radiopharmaceuticals. Considering the dithiocarbamate ligand can act as a suitable bifunctional linking agent to attach technetium‐99m (99mTc) to corresponding target molecules, in this study, alendronate dithiocarbamate (ALNDTC) was synthesized and radiolabeled with [99mTc≡N]2+ core by ligand exchange reaction to produce 99mTcN‐ALNDTC complex, for the potential use as a novel probe for bone imaging. The radiochemical purity of the complex was over 90%. The complex was stable in vitro and could bind to hydroxyapatite. The partition coefficient result indicated it was hydrophilic, and an evaluation of biodistribution in mice indicated that the complex exhibited a higher bone uptake than did 99mTc‐labeled methylenediphosphonate (99mTc‐MDP). Further, single photon emission computed tomography imaging study indicated clear accumulation in bone, suggesting that 99mTcN‐ALNDTC would be a promising candidate for bone imaging.
中文翻译：
阿仑膦酸二硫代氨基甲酸酯作为潜在的骨显像剂的新型99mTc硝化放射性药物的合成与评价
当前，基于双功能放射性药物的概念，设计新颖的放射性探针作为骨显像剂的流行策略。考虑到二硫代氨基甲酸配体可以作为合适的双官能连接剂锝-99m（连接动作99米TC）给相应的目标分子，在这项研究中，阿仑膦酸盐二硫代氨基甲酸（ALNDTC）合成，并通过[放射性标记99米Tc≡N] 2+通过芯配体交换反应产生99mTcN-ALNDTC复合物，有可能用作骨成像的新型探针。该配合物的放射化学纯度超过90％。该复合物在体外是稳定的并且可以与羟基磷灰石结合。分配系数的结果表明它是亲水的，对小鼠体内生物分布的评估表明，该复合物比99m Tc标记的亚甲基二膦酸酯（99m Tc-MDP）表现出更高的骨吸收。此外，单光子发射计算机断层摄影成像研究表明骨中明显积聚，这表明99m TcN-ALNDTC将是有前途的骨成像候选者。
更新日期：2017-10-31
中文翻译：
阿仑膦酸二硫代氨基甲酸酯作为潜在的骨显像剂的新型99mTc硝化放射性药物的合成与评价
当前，基于双功能放射性药物的概念，设计新颖的放射性探针作为骨显像剂的流行策略。考虑到二硫代氨基甲酸配体可以作为合适的双官能连接剂锝-99m（连接动作99米TC）给相应的目标分子，在这项研究中，阿仑膦酸盐二硫代氨基甲酸（ALNDTC）合成，并通过[放射性标记99米Tc≡N] 2+通过芯配体交换反应产生99mTcN-ALNDTC复合物，有可能用作骨成像的新型探针。该配合物的放射化学纯度超过90％。该复合物在体外是稳定的并且可以与羟基磷灰石结合。分配系数的结果表明它是亲水的，对小鼠体内生物分布的评估表明，该复合物比99m Tc标记的亚甲基二膦酸酯（99m Tc-MDP）表现出更高的骨吸收。此外，单光子发射计算机断层摄影成像研究表明骨中明显积聚，这表明99m TcN-ALNDTC将是有前途的骨成像候选者。
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