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完成了5-羟色胺转运体显像剂[125I]-2-((2-((二甲基氨基)甲基)苯基)巯基)5-碘苯胺([125I]-2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine,[125I]ADAM)的制备和初步生物学特性的评价。以2,5-二溴-硝基苯和2-巯基苯甲酸为起始原料,合成标记前体5-三丁基锡-2-[2-(二甲基氨基甲基苯基巯基)]苯胺,采用双氧水标记法标记;并进行了大鼠体内和脑内的初步生物分布研究。合成标记前体5-三丁基锡-2-[2-(二甲基氨基甲基苯基巯基)]苯胺的总产率为42%,用[125I]NaI标记后,TLC测放射化学纯度(RCP)大于95%;125I-ADAM大鼠脑摄取高,在富含5-羟色胺转运蛋白的丘脑中的摄取随时间延长而增加,滞留时间长,其特异结合在注射后60min、120min和240min分别为3.38,3.62和4.36。本合成方法总收率高,标记方法简便,放射化学纯度高,125I-ADAM初始进脑量高,与SERT结合特异,可望用于研究脑内SERT功能。
[125I] -2 - ((2 - ((dimethylamino) methyl) phenyl) sulfhydryl) 5-iodoaniline (dimethylamino) methyl) phenyl) thio) -5-iodophenylamine, [125I] ADAM) and evaluation of preliminary biological properties. Starting from 2,5-dibromo-nitrobenzene and 2-mercaptobenzoic acid, 5-tributyltin-2- [2- (dimethylaminomethylphenylmercapto)] aniline was synthesized. Using hydrogen peroxide labeling method; and preliminary rat biodistribution studies in vivo and in vivo. The overall yield of 5-tributyltin-2- [2- (dimethylaminomethylphenylmercapto)] aniline as a synthetic tag precursor was 42%. After labeling with [125I] NaI, the radiochemical purity (RCP ) Was greater than 95%. The uptake of 125I-ADAM rat brain increased with time, increased in serotonin transporter-rich thalamic brain with long residence time. The specific binding of 125I-ADAM rats at 60min, 120min and 240min after injection were 3.38, 3.62 and 4.36. The method has the advantages of high total yield, simple labeling method, high radiochemical purity, high initial 125I-ADAM intake and specific binding to SERT, which is expected to be used for studying SERT function in the brain.