摘要
通过一系列氨羧缩合反应合成了双功能螯合剂硫代乙酰基-巯基乙酰-二甘氨酰-赖氨酸(S-Acetyl-MAG2Lys),并以生长抑素(somatostatin,SMS)、葡聚糖-10(Dextran10,Dx10)及S-Acetyl-MAG2Lys为原料,合成了糖基化生长抑素配体化合物(SMS-Dx10-MAG2Lys);利用酒石酸钠转换配合进行了SMS-Dx10-MAG2Lys的99Tcm标记,重点探讨了99Tcm标记条件及标记物的体外稳定性。结果表明,合成的双功能螯合剂S-Acetyl-MAG2Lys和配体化合物SMS-Dx10-MAG2Lys可成功用于99Tcm的放射标记,在最佳标记条件:0.3 g/L SnCl2,5 g/L SMS-Dx10-MAG2Lys,标记介质pH=9.5,室温下反应30 min,99Tcm-MAG2Lys-Dx10-SMS标记率约为50%,经分离纯化后,其放射化学纯度大于99%,标记物体外稳定,为进一步研究99Tcm-MAG2Lys-Dx10-SMS体内生物学特性提供了依据。
A new bifunctional chelator S-Acetyl-mercaptoacetyl-glycyl-glycyl-lysine （S-Acetyl- MAG2Lys） was synthesized. Natural somatostatin, dextran-10 and S-Acetyl-MAG2Lys were used to prepare somatostatin-dextran-MAG2Lys （SMS-Dx^10-MAG2Lys） conjugate. The SMS- Dx^10-MAG2Lys was radiolabeled with ^99Tc^m by using sodium tartrate as a transchelator. The ^99Tc^mMAG2 Lys-Dx^10- SMS radiolabeling conditions and its in vitro stability were studied in detail. The new chelator S-Acetyl-MAG2Lys and SMS-Dx^10-MAG2Lys conjugate were radiolabeled with ^99Tc^m successfully. The labeling efficiency of ^99Tc^m MAG2 Lys-Dx^10-SMS is approximately 50% under optimum conditions and its radiochemical purity is more than 99% after purification. The in vitro stability of the radiolabeled conjugate is satisfied. The results indicate that ^99Tc^m-MAG2Lys-Dx^100-SMS makes a base for its in vivo biological properties further investigation.
出处
《核化学与放射化学》
EI
CAS
CSCD
北大核心
2007年第3期178-183,共6页
Journal of Nuclear and Radiochemistry
基金
国家自然科学基金资助项目(30370421)
教育部留学回国人员科研启动基金资助项目(2004)
