多巴胺D_2受体配体的合成及^(99m)Tc标记(Ⅰ)——悬挂式设计

SYNTHESIS AND LABELING OF ^(99m)Tc-LABELED BENZAMIDE DOPAMINE D_2 RECEPTOR IMAGING AGENTS (Ⅰ) ——EXPANDING DESIGN METHOD

以多巴胺D2 受体配体Cl ABZM为前体 ,合成了末端带有巯基的单齿化合物 ,光谱数据与结构相符 .用配体交换法与 3 硫杂 1,5 戊二硫醇共同配位合成了“3+ 1”型混配螯合物 ,对影响标记率的诸多因素如 pH值、温度、配体用量及反应时间等进行了优化 ,得到最佳标记条件 ,标记率大于 85%

In developing 99m Tc labeled dopamine D 2 receptor imaging agents, a new substituted benzamide compound is designed and synthesized. By tetering a S 3 chelate system onto it, a technetium 3+1 complex is formed.Initial synthesis and radiolabeling suggest that the 99m Tc complex is neutral and lipophilic.The factors which have influence on labeling yield are optimized, including pH value, ligand quantity, reaction temperature and time. Labeling yield is over 85%.