^(99)Tc^m标记苯托品类多巴胺转运蛋白显像剂的制备和小鼠体内分布

SYNTHESIS, LABELING AND BIODISTRIBUTION OF TECHNETIUM-99-LABELED BENZTROPINE ANALOGS AS DOPAMINE TRANSPORTER IMAGING AGENTS

合成了以苯托品 (Benztropine)为前体的含巯基的单齿化合物 ,其光谱数据和结构相符。使用配体交换法与 3 硫杂 1 ,5 戊二硫醇 (SSS)配位合成了99Tcm 的“3 +1”型混配螯合物a。螯合物a在小鼠脑中有一定的初始摄取和滞留量 ,在t=5min时 ,ID =1 0 3 % /g ;对纹状体也有一定的亲和力 ,纹状体与小脑摄取比值随时间延长而增加 ,在t=60min时 ,R(纹状体 /小脑 ) =1 3。混配螯合物有成为多巴胺转运蛋白显像剂的可能。

In developing 99Tc m-labelled dopamine transporter imaging agents, a new substituted compound is designed and synthesized. By tetering S 3 chelate system onto it, one technetium '3+1' complex is formed. Biodistribution studies are carried out in mice. The results demonstrate that the labeled compound(a) has the ability to penetrate the intergrate blood brain barrier(1.03 %/g), at 5 min, post injection and retains for a certain time in brain. The ST/CB is 1.3 at 60 min after iv injection in mice. It also shows that brain uptake and selectivity of labeled compound(a) are higher and further improving is needed.