中文摘要：

分别选用^90Y和^177Lu标记DOTA-Bz-RGD tetramer和DOTA-RGD tetramer,比较不同形式的双功能螯合剂对标记条件以及标记物的体外稳定性的影响。考察了反应pH值、反应温度和反应时间对标记率的影响。ITLC和HPLC分析结果表明,pH=6.0,100℃下反应15～20 min,4种标记物的标记率均大于95%;在生理盐水和牛血清体系中,4种标记物均保持良好的稳定性。苄基（Bz）的引入并不影响标记条件和标记物的体外稳定性,但对整个分子的极性带来了影响。HPLC分析结果和lgP测定结果显示,引入苄基（Bz）使标记物分子的脂溶性略微增加。

英文摘要：

^90Y/^177Lu labeled DOTA-Bz-RGD tetramer and DOTA-RGD tetramer were prepared,and the effect of Bz-DOTA and DOTA on labeling conditions and in vitro stability of radiolabeled compounds was compared.The labeling conditions,including reaction pH,reaction temperature and reaction time,were investigated.ITLC and HPLC show that the labeling yields of four radiolabeled compounds are more than 95% under optimal conditions（pH=6.0,reacting at 100 ℃ for 15-20 min）;the four radiolabeled compounds show pretty good stability in saline and fetal bovine serum. Although introducing of Bz has no effect on labeling conditions and in vitro stability of radiolabeled compounds, it brings a little change on molecule polarity. HPLC analysis and lg P values reveal that introducing of Bz increases the lipophilicity of radiolabeled compounds.