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Novel 99mTc labeled complexes with bisphosphonate isocyanide: Radiosynthesis and evaluation as potential bone-seeking agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2022-08-01 , DOI: 10.1016/j.bmcl.2022.128918
Di Xiao 1 , Yuhao Jiang 1 , Junhong Feng 1 , Qing Ruan 1 , Qianna Wang 1 , Guangxing Yin 1 , Junbo Zhang 1
Affiliation  

In order to develop 99mTc-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 [99mTc]Tc(I) complexes. [99mTc]Tc-CNALN and [99mTc]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 [99mTc]Tc-CNALN showed higher bone/background ratios at 60 min post-injection. In single photon emission computed tomography (SPECT) imaging study, [99mTc]Tc-CNALN had an obvious accumulation in bone, suggesting it would be a promising bone-seeking agent.



中文翻译:

新型 99mTc 标记的双膦酸异氰化物复合物:放射合成和评估作为潜在的寻骨剂

为了开发99m Tc 标记的双膦酸盐异氰化物复合物作为新型骨显像剂,合成了两种双膦酸盐异氰化物衍生物(CNALN 和 CNPAM),并进行了放射性标记以制备相应的 [ 99m Tc]Tc(I) 配合物。[ 99m Tc]Tc-CNALN和[ 99m Tc]Tc-CNPAM均获得高放射化学纯度,并表现出良好的体外稳定性。它们都是亲水性的并且对羟基磷灰石具有高亲和力。小鼠体内的生物分布研究表明,[ 99m Tc]Tc-CNALN 在注射后 60 分钟显示出更高的骨/背景比率。在单光子发射计算机断层扫描 (SPECT) 成像研究中,[ 99mTc]Tc-CNALN在骨中有明显的积累,表明它是一种很有前途的寻骨剂。

更新日期:2022-08-03
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