肝胆显象剂－^（99m）Tc－芳甲酰肼羰甲基亚氨二乙酸类的合成和动物实验

SYNTHESIS OF ^(99m)Tc-AROYLHYDRAZINOCARBONYLMETHYLIMINODIACETIC ACIDS AND THEIR ANLMAL STUDY, HEPATOBILIARY PHARMACEUTICALS

合成９个新类型芳甲酰肼羰甲基亚氨二乙酸衍生物，用氯化亚锡还原高锝酸钠制得９９ｍＴｃ－标记化合物，用小白鼠和家兔实验的结果，都显示不同程度为肝脏细胞吸收，血中清除和分泌于胆道。其中以９９ｍＴｃ－２－甲氧基－５－溴苯甲酰肼羰甲基亚氨二乙酸的特异性较好。

Based on the structure specificity of a new comPund isonicotinoylhydrazinocarbonylmethyliminodiacetic acid,nine similar derivatives were synthesized by esterification of aromatic acids,followed by hydrazinolysis, and acylation with nitrilotriacetic acid.The 99mTc-complexes of these compounds were prepared by stannous chloride reduction of sodium pertechnetate in aqueous solution at Ph 6～7. The experimental resuhs in mice and rabbits showed that the 99mTc-complexes all exhlbited varying degrees in the uptake by the liver cells,cleared off from the blood and excreted into the biliary traet.The hepatobiliary specificity of 99mTc-2-methoxy-5-bromobenzoylhydrazinocarbonylmethyliminodiacetic acid was the best among them. It is coneluded preliminarily that the aroylhydrazinocarbonylmethyliminodiacetic acids provide to be a fruitful source for 99mTc-labeled hepatobiliary radiopharmaceuticals.