多巴胺D_2受体显像剂^(99)Tc^m-mEBZM生物学评价  

Biological evaluation of ^(99)Tc^m-labeled dopamine D_2 receptor imaging agent mEBZM

作　　者：郝彬[1] 钱隽[1] 高秀健[1] 沈鸣华[1] 孟腊平[1] 朱建华[1] 

机构地区：[1]复旦大学药学院,上海200032

出　　处：《核技术》2003年第11期841-844,共4页Nuclear Techniques

摘　　要：将ECD(L,L-ethyl cysteinate dimer)分子与对多巴胺D2受体具有较高亲和力的苯酰胺分子(BZM)偶联,制备99Tcm-mEBZM,并研究了99Tcm-mEBZM在大鼠和小鼠体内的生物分布。结果显示,99Tcm-mEBZM具有较高的体外稳定性和较高的脂溶性,在小鼠的生物分布中呈现较高的进脑量(2 min时为2.97％ID·g-1),小鼠与大鼠的纹状体/小脑比值可达到1.55,提示标记物与纹状体的结合具有特异性。99Tcm-labeled dopamine D2 receptor imaging agent 99Tcm-mEBZM was prepared and the biological evaluation was studied. ECD( L,L-ethyl cysteinate dimer) was conjugated with the benzamide derivative, which has high affinity with dopamine D2 receptor, to yield 99Tcm-mEBZM. The biodistribution of 99Tcm-mEBZM in rats and mice was studied. The results showed that 99Tcm-mEBZM has higher stability in vitro and higher lipophilicity. The brain uptake of 99Tcm-mEBZM in mice is high(2.97%ID·g-1 at 2 min), and the ratios of striatum /cerebellum both in rats and in mice were >1.55.

关 键 词：多巴胺D2受体 受体显像 放射性药物 ^99TC^M 

分 类 号：O614.7[理学—无机化学] R817.4[理学—化学]