<sup>90</sup>Y/<sup>177</sup>Lu标记DOTA-Bz-RGD tetramer 和DOTA-RGD tetramer的比较

张燕; 贺巍巍; 贾兵; 王凡

⁹⁰Y/¹⁷⁷Lu标记DOTA-Bz-RGD tetramer 和DOTA-RGD tetramer的比较

张燕^1,2,
贺巍巍¹,
贾兵^1,2,
王凡^1,2,

1.
北京大学医学同位素研究中心,北京 100083
2.
中国原子能科学研究院同位素研究所,北京 102413

详细信息

通讯作者:
王凡

中图分类号: O615.4
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出版历程
- 收稿日期: 2006-10-25
- 修回日期: 2007-08-13
- 刊出日期: 2008-05-19

Comparison of ⁹⁰Y/¹⁷⁷Lu Labeled DOTA-Bz-RGD Tetramer and DOTA-RGD Tetramer

ZHANG Yan^1,2,
HE Wei-wei¹,
JIA Bing^1,2,
WANG Fan^1,2,

1.
Peking University Medical Isotopes Research Center, Beijing 100083, China
2.
Department of Isotopes, China Institute of Atomic Energy, Beijing 102413, China

More Information

Corresponding author:
WANG Fan

摘要

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lg P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。
- ⁹⁰Y /
- ¹⁷⁷Lu /
- DOTA /
- Bz-DOTA /
- RGD 四聚体
Abstract: 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.
- ⁹⁰Y /
- ¹⁷⁷Lu /
- DOTA /
- Bz-DOTA /
- RGD tetramer

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参考文献(10)

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