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肝胆显像剂99m锝-甲溴苯宁的合成和初步动物实验

SYNTHESIS OF 99mTc-MEBROFENIN AND ITS ANIMAL EXPERIMENTAL STUDY

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【作者】 周锡瑞; 郑孝章; 刘贻孙; 赵惠扬; 陈绍亮; 屠之培;

【Author】 ZHOU XIRUI, ZHENG XIAOZHANG, LIU YISUN(Department of Medicinal Chemistry, Faculty of Pharmacy, Shanghai First Medical College, Shanghai)ZHAO HUIYANG, OHEN SHAOLIANG, Tu ZHIPEI(Department of Nuclear Medicine, Zheng Shan Hospital, Hongqi Pharmaceutical Factory, Shanghai First Medical College, Shanghai)

【机构】 上海第一医学院药学系合成药物化学教研室; 上海第一医学院中山医院核医学教研室; 红旗药厂;

【摘要】 99m锝-甲溴苯宁(Mebrofenin)被认为是当前最优良的一种肝胆显像剂,作者参考有关文献后,进行试制获得成功,经初步动物实验,证实该显像剂能使肝胆清楚显像,值得今后在临床上试用。

【Abstract】 Mebrofenin was synthesized by nitration of mesitylene, followed by reduction, bromination and acylation with nitrilotriacetic acid. The 99mTc-complex of this compound was prepared by stannous chloride reduction of sodium pertechnetate in aqueous solution of the appropriate compound. 99mTc-Mebrofenin possesed high hepatic specificity and rapid hepatocellular transit; it was also resistant to competition for hepatobiliary excretion from bilirubin and rapid radiolabeling with high radiochemical purity and stability. 18 cases of patients were studied by this agent, all obtained excellent results.

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