苯酰胺类D_2受体新配体的合成,^(125)I标记及生物分布研究

SYTHESIS AND LABELLING OF DOPAMINE D_2 RECEPTOR NEW LIGAND

合成了苯酰胺类D2 受体配体 (S) N [(1 羟乙基 2 四氢吡咯烷基 )甲基 ] 5 氨基 2 ,3 二甲氧基苯甲酰胺(HEABZM) ,用红外光谱 ,核磁共振和质谱法进行了表征。以HEABZM为标记前体 ,制备了 (S) N [(1 羟乙基 2 四氢吡咯烷基 )甲基 ] 5 氨基 4 12 5I 2 ,3 二甲氧基苯甲酰胺。标记率为 79% ,经萃取分离后 ,放化纯度在90 %以上。小鼠体内初步生物分布研究表明 ,该配合物在小鼠脑中有一定的区域分布 ,纹状体与小脑的比值略大于 1。

One desired dopamine agents,(S) N [(1 hydroxyethyl 2 pyrrolidinyl)methyl] 5 amonio 2,3 dimethoxy benzamide,is synthesized in the first time.The chemical structure is confirmed by spectrum data.The radioiodination of the compound with 125 I is accomplished by an electrophilic iodination reaction using hydrogen peroxide as an oxidant and the labeled compound,(S) N [(1 hydroxyethyl 2 pyrrolidinyl)methyl] 5 amonio 4 125 I 2,3 dimethoxy benzamide,is obtained.The labelling yield is about 79% and the radiochemical purity is higher than 90% after extraction.The regional distribution of this complex in the brain(ratio of striatum/cerebellum is higher than 1)displays the selective localization.