中文摘要：

选择了3种三齿配体（二（2-吡啶甲基）-胺基）-乙胺（L^1NH2）、（二（2-吡啶甲基）-氨基）-乙酸（L^2H）和（（6-胺基-N-叔丁氧基羰基-己基）-吡啶-2-甲基氨基）-乙酸（L^3NH2）,用于设计合成新的以fac-[188Re（CO）3]＋为核心的放射性药物。3种配体在低浓度（10^-5mol/L）的条件下,反应时间小于60 min,标记率可达90%以上,放射化学纯度大于92%;3种标记物的体外稳定性均很高,标记后24 h内基本不分解。生物分布结果表明,配合物均能较快地从血液和多数的组织器官中清除,主要通过排泄系统代谢,并初步探讨了这3个配合物在小鼠体内的生物分布行为可能与它们的脂水分配系数lgP有关。lgP值（-0.36）高的配合物[^188Re（CO）3L^3NH2],24h时在各个器官中放射性保留均高于其它2个配合物,但可能不是唯一的影响因素。总的来说,3个配基是用fac-[^188Re（H2O）3（CO）3]＋标记的比较理想的双功能螯合剂。

英文摘要：

Three novel tridentate ligands（L^1NH2 = bis（2-pyridylmethyl）-amino）-ethylamine,L^2H = bis（2-pyridylmethyl）-amino）-acetic acid,L^3NH2 = [（6-amino-hexyl）-pyridyl-2-methyl-amino]-acetic acid） were used as bifunctional chelating agents for the organometallic precursor fac-[^188Re（CO）3（H2O）3]^＋.The results of labeling condition experiments show that a radiochemical purity higher than 92% can be obtained within 60 min by the reaction of fac-[^188Re（CO）3]^＋ core in a condition（pH=7.4） with a very small amount（10^-5 mol/L） of these three ligands. The stability experiments in vitro demonstrate that fac-[^188Re （CO）3L^1NH2]^＋ , fac-[^188Re（CO）3L^2H] and fac-[^188Re（CO）3L^3NH2] do not decompose with-in 24 h （37 ℃, new born calf serum）. Biodistributions results indicate that the complexes with tridentate coordinated ligand systems revealed generally a good and fast clearance from all organs and tissues, primarily through the renal-urinary pathway with a small portion retained in the hepatobiliary tract. The predominant route ot excretlon, the urinary tract, seems to correlate with the lg P values found for the complexes. The highest hepatic retention was found for the complex [^188Re（CO）3L^3NH2] with a lg P value of-0.36. On the basis of these experiments, it appears that functionalization of biomolecules with tridentate-chelating ligand systerns is feasible for the labeling with fac-[^188Re（H2O）3 （CO）3]^＋.