~(99)Tc~m-吡哆醛氨基酸类肝胆显像剂结构与生物体内分布行为的关系
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摘要: 采用３种分子结构不同的吡哆醛氨基酸（ＰＡ）即吡哆醛色氨酸（ＰＨＴ）、吡哆醛胱氨酸（ＰＨＣ）和吡哆醛酪氨酸（ＰＨＹ）进行９９Ｔｃｍ标记，ｐＨ＝７时标记率≥９５％。进行了３种９９Ｔｃｍ－ＰＡ在小白鼠体内生物分布的实验研究，并测定了３种９９Ｔｃｍ－ＰＡ在正辛醇与水相间的分配系数，结果表明：配体的分配系数愈高，亲脂性愈大，小鼠体内的血液清除愈快，肝胆浓集量愈高，这为寻找理想的肝胆显像药物提供了一定的理论依据
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关键词:
- ~（９９）Ｔｃ~ｍ－吡哆醛氨基酸（~（９９）Ｔｃ~ｍ－ＰＡ） /
- 肝胆显像剂 /
- 结构 /
- 生物体内分布 /
- 关系
Abstract: THE RELATIONSHIP BETWEEN STRUCTURE AND BIODISTRIBUTION OF 99TcmPYRIDOXYLAMINO ACIDS FOR HEPATOBILIARY IMAGING AGENTSZhang Huaming Luo Shunzhong Liu Zhonglin Zhao Pengji(Institute of Nuclear Physics and Chemistry, China Academy of Engineering Physics, Chengdu 610003)ABSTRACTIn order to investigate the relationship between structure and biodistribution of 99Tcmpyridoxylamino acids(PA), pyridoxylLtryptophan(PHT), pyridoxylaminoLcystine(PHC) and pyridoxylaminotyrosine (PHY) are labelled with 99Tcm using Sn(Ⅱ) as a reductant. The labelling yields of 99TcmPA is better than 95% at pH=7.0. The partition coefficients as lipophilic parameter in the octanolwater system are determined. The biodistribution in male mice shows that 99TcmPA have fast blood clearance, but the difference is apparent in their hepatobiliary uptakes and intestinal accumulations. Particularly, there is a good correlation between the hepatobiliary uptake and the partition coefficient. The larger the partition coefficient, the higher the lipophilicity. This result may be valuable for developing new 99TcmPA of hepatobiliary imaging agent.Key words 99Tcmpyridoxylamino acids 99TcmPA) hepatobiliary imaging agent structure biodistribution relationship -
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１ＥｃｋｅｌｍａｎＷＣ，ＶｏｌｋｅｒｔＷＡ．ＩｎＶｉｖｏＣｈｅｍｉｓｔｒｙｏｆ９９Ｔｃｍ－ｃｈｅｌａｔｅｓ．ＩｎｔＪＡｐｐｌＲａｄｉａｔＩｓｏｔ，１９８２，３３：９４５—９５１．２ＡｚｕｍａＭＫ．Ｔｃ－９９ｍ（Ｓｎ）－Ｎ′－ｐｙｒｉｄｏｘｙｌａｍｉｎａｔｅｓ：ＡＮｅｗＳｅｒｉｅｓｏｆＨｅｐａｔｏｂｉｌｉａｒｙ．ＪＮｕｃｌＭｅｄ，１９８２，２３（６）：５１７－５２４．３ＡｚｕｍａＭＫ，ＨａｚｕｅＭ．ＰｒｅｐａｒａｔｉｏｎａｎｄＢｉｏｌｏｇｉｃＥｖａｌｕａｔｉｏｎｏｆＬｉｐｏｐｈｉｌｉｃＤｅｒｉｖａｔｉｖｅｓｏｆＴｃ－９９ｍ（Ｓｎ）－ｐｙｒｉ－ｄｏｘｙｌｉｄｅｎｅｐｈｅｎｙｌａｌａｍｉｎｅ：ＡｎＡｐｐｒｏａｃｈｔｏＳｔｒｕｃｔｕｒｅＢｉｏｄｉｓｔｒｉｂｕｔｉｏｎＲｅｌａｔｉｏｎｓｈｉｐｏｆＴｅｃｈｎｅｔｉｕｍＣｏｍ－ｐｌｅｘｅｓ．ＪＬａｂｅｌＣｏｍｐＲａｄｉｏｐｈａｒｍ，１９８０，１８（１２２）：１３３－１３５．４ＵｒｓｕｌａＳ，ＨｏｗａｒｄＷＧ，ＳｕｓａｎＺＬ，ｅｔａｌ．ＣｏｍｐａｒｉｓｏｎｏｆＴｅｃｈｎｅｔｉｕｍ－９９ｍＡｍｉｎｏａｌｋｙｌＤｉａｍｉｎｏｄｉｔｈｉｏｌ（ＤＡＤＴ）ＡｎａｌｏｇｓａｓＰｏｔｅｎｔｉａｌＢｒａｉｎＢｌｏｏｄＦｌｏｗＩｍａｇｉｎｇＡｇｅｎｔｓ．ＪＮｕｃｌＭｅｄ，１９８８，２９（１）：７３－８２．
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