Synthesis, in vitro and in vivo behavior of 188Re(I)-tricarbonyl complexes for the future functionalization of biomolecules
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- 作者：Jiaoyun Xia ; Yongxian Wang ; Junfeng Yu ; Shiqiang Li ; Lin Tang ; Mingqiang Zheng ; Xiuqing Liu ; Gucai Li ; Dengfeng Cheng and Sheng Liang ; et al.
- 刊名：Journal of Radioanalytical and Nuclear Chemistry
- 出版年：2008
- 出版时间：February, 2008
- 年：2008
- 卷：275
- 期：2
- 页码：325-330
- 全文大小：179.9 KB
文摘
Radiolabeling of biologically active molecules with fac-[188Re(CO)3(H2O)3]+ unit has been of primary interest in recent years. Therefore, we herein report ligands L1−L4 (L1=histidine, L2=nitrilotriacetic acid, L3=2-picolylamine-N,N-diacetic acid, L4=bis(2-pyridymethy)amine) that have been evaluated by radiochemical reactions with fac-[188Re(CO)3(H2O)3]+. These reactions yielded the radioactive complexes of fac-[188Re(CO)3L] (L = L1−L4, 188Re tricarbonyl complexes 1–4), which were identified by HPLC. Complexes 1–4, with log P o/w values ranging from −2.23 to 2.18, were obtained with yields of ≥95 % using ligand concentrations within 10−6–10−4M range. Thus, specific activities of 220 GBq/μmol could be achieved. Challenge studies with cysteine and histidine revealed high stability for all of these radioactive complexes, and biodistribution studies in mice indicated a fast rate of blood clearance and high rate of total radioactivity excretion occurring primarily through the renal-urinary pathway. In summary, the ligands L1–L4 are potent chelators for the future functionalization of biomolecules labeling with fac-[188Re(CO)3(H2O)3]+.