Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
Bioorg Med Chem Lett. 2022 Oct 1;73:128918. doi: 10.1016/j.bmcl.2022.128918. Epub 2022 Aug 1.
In order to develop Tc-labeled complexes with bisphosphonate isocyanide as novel bone imaging agents, two bisphosphonate isocyanide derivatives (CNALN and CNPAM) were synthesized and radiolabeling was performed for preparing the corresponding [Tc]Tc(I) complexes. [Tc]Tc-CNALN and [Tc]Tc-CNPAM were obtained with high radiochemical purity and showed good in vitro stability. Both of them were hydrophilic and had high affinity to hydroxyapatite. The biodistribution studies in mice revealed [Tc]Tc-CNALN showed higher bone/background ratios at 60 min post-injection. In single photon emission computed tomography (SPECT) imaging study, [Tc]Tc-CNALN had an obvious accumulation in bone, suggesting it would be a promising bone-seeking agent.
为了开发以双膦酸盐异腈为配体的 Tc 标记配合物作为新型骨显像剂，我们合成了两种双膦酸盐异腈衍生物（CNALN 和 CNPAM），并进行放射性标记以制备相应的 [Tc]Tc（I）配合物。[Tc]Tc-CNALN 和 [Tc]Tc-CNPAM 具有高放射化学纯度，表现出良好的体外稳定性。它们均具有亲水性和对羟磷灰石的高亲和力。小鼠的生物分布研究表明，[Tc]Tc-CNALN 在注射后 60 分钟具有更高的骨/背景比。在单光子发射计算机断层扫描（SPECT）成像研究中，[Tc]Tc-CNALN 在骨组织中有明显的聚集，表明其可能是一种有前途的骨靶向剂。
