~(99)Tc~m标记多巴胺D_2受体配体的合成,标记及生物分布研究
SYNTHEIS, LABELLING AND BIODISTRIBUTION STUDY OF NEW ~(99)Tc~m-LABELED BENZAMIDE DOPAMINE D_2RECEPTOR IMAGING AGENTS
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摘要: 首次合成了 3种苯酰胺类D2 受体配体 :N (2 巯基 )乙基 2 ,3 二甲氧基苯甲酰胺 (MEDM BZM) ,N (2 巯基 )乙基 5 溴 2 ,3 二甲氧基苯甲酰胺 (MEBDM BZM ) ,N (2 巯基 )乙基 3 乙氧基苯甲酰胺 (MEE BZM) ,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中性脂溶性的“3+ 1”型混配99Tcm 螯合物 ,标记率大于 85 %。 3种配合物在小鼠脑中的初始摄取率高于文献报道值Abstract: In developing 99 Tc m labeled dopamine D 2 receptor imaging agents, three new substituted benzamide compounds are designed and synthesized. By tetering a S 3 chelate system onto them, three technetium 3+1 complexes are formed. Initial synthesis and radiolabeling su ggest that the 99 Tc m complexes are neutral and lipophilic. Labeling yield is over 85 %. The brain uptake of three 99 Tc m complexes is higher than the data reported in literature.