Pen-Ahx-c(RGDfK) and Re-[Pen-Ahx-c(RGDfK)]2, respectively. 99mTc-[Pen-Ahx-c(RGDfK)]2 provided tumor image without removing unlabeled ligand, while a 99mTc-labeled monovalent probe prepared from a monovalent ligand could not. These findings indicate the availability of the design concept to prepare 99mTc-labeled bivalent probes with a variety of 99mTc core and other metallic radionuclides of clinical relevance
在the 99m(99m Tc)标记的靶标特异性
配体的合成中,注射液中超过99m Tc的大量未标记
配体的存在阻碍了99m Tc标记的
配体通过竞争靶分子而积累靶标。为了解决该问题,我们最近开发了一种
金属配位介导的多价概念,并用99m Tc标记的三价化合物[ 99m Tc(CO)3(CN-RGD)3 ] +证明了这一概念。在这项研究中,
D-青霉胺(Pen)被选作螯合分子,环状RGDfK肽通过
己酸键(Pen-Ahx-c(RGDfK))与Pen缀合。99m
锝络合反应,并且稳定,整合素α v β 3的结合亲和力,和
生物分布99米Tc-标记的探针进行了研究,以评估的概念的二价探针的适用性。在低Pen-Ahx-c(RGDfK)浓度(50μM)下,以95%的放射
化学收率获得了99m Tc- [Pen-Ahx-c(RGDfK)] 2。99米TC- [笔AHX-C(RGDfK)] 2显示出更高的整合素α大约10倍v