同位素2001，Vol.14Issue(2)：65-70,6.
多巴胺D2受体显像剂Epidepride的合成及其131I标记
Synthesis and 131I Labeling of Epidepride as a Dopamine D2 Receptor Imaging Agent
杨敏 1胡名扬 1裴著果 1王博诚 1周杏琴1
作者信息
摘要
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 131I by hydrogen peroxide method, and 131I-epidepride is gained, its radiolabelling yield(RLY) and the radiochemical purity(RCP)are all over 95%. The RCP of 131I-epidepride is over 90% under 4 ℃ after 15 days. 131I-epidepride has high affinity to dopamine D2 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 131I-epidepride may be used as a dopamine D2 receptor imaging agent for SPECT.关键词
多巴胺D2受体显像剂/Epidepride/合成/131I标记分类
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杨敏,胡名扬,裴著果,王博诚,周杏琴..多巴胺D2受体显像剂Epidepride的合成及其131I标记[J].同位素,2001,14(2):65-70,6.
