【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。更多还原

【Abstract】 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.更多还原