多巴胺D_2受体显像剂Epidepride的合成及其~(131)I标记
Synthesis and ~(131)I Labeling of Epidepride as a Dopamine D_2 Receptor Imaging Agent
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摘要: 以 3-甲氧基水杨酸为原料合成了 EpideprideS- ( - ) - N- ( 1-乙基 - 2 -吡咯烷基 )甲基- 5-碘 - 2, 3-二甲氧基苯甲酰胺及其标记前体 ( S- ( - ) - 5- (三正丁基锡 ) - N- ( 1-乙基 - 2 -吡咯烷基 )甲基2, 3-二甲氧基苯甲酰胺 ), 并采用双氧水法对标记前体进行 131I标记, 获得 131I- epidepride,标记率和放化纯度均大于 95%。13 1I- epidepride溶液体外稳定性好, 4℃放置 15d放化纯度仍大于 90 %。131I- epide-pride与 D2 受体亲和力高, 大鼠脑内纹状体与小脑的摄取比在 32 0 min时高达 2 37;在脑内纹状体的吸收可被 Spiperone完全阻断。因此, 131I- epidepride有望成为多巴胺 D2 受体 SPECT显像剂。Abstract: S (-) N (1 ethyl 2 pyrrolidinyl)methyl 5 iodo 2,3 dimethoxybenzamide (Epidepride) and its iodine labeling precursor S (-) N (1 Ethyl 2 pyrrolidinyl)methyl 5 tributyltin 2,3 dimethoxybenzamide are synthesized from 3 methoxy salicylic acid. The labeling precursor is labeled with 131 I by hydrogen peroxide method, and 131 I epidepride is gained, its radiolabelling yield(RLY) and the radiochemical purity(RCP)are all over 95%. The RCP of 131 I epidepride is over 90% under 4 ℃ after 15 days. 131 I epidepride has high affinity to dopamine D 2 receptor The striatal uptake can be blocked completely by spiperone. The striatum and cerebellum uptake ratio can reach 237 at 320 min in rats.The results show that 131 I epidepride may be used as a dopamine D 2 receptor imaging agent for SPECT.
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