^(153)Sm,^(113,117)Sn^m烷基膦酸配合物的表观脂水分配系数及与BSA的结合率  

Apparent Partition Coefficient in Octanol-Water and Binding Percentage to BSA of ^(153)Sm^(113,117)Sn^m Complexes

作　　者：杨玉青[1] 罗顺忠[1] 王关全[1] 何佳恒[1] 邴文增[1] 蒲满飞[1] 魏洪源[1] 王文进[1] 

机构地区：[1]中国工程物理研究院核物理与化学研究所,四川绵阳621900

出　　处：《核化学与放射化学》2004年第3期179-183,共5页Journal of Nuclear and Radiochemistry

摘　　要：测定了NTMP(次氮三亚甲基膦酸),HEDTMP(N (羟乙基)乙二胺基三亚甲基膦酸),DCTMP(1,2 环己二胺四亚甲基膦酸),EDTMP(乙基二胺基四亚甲基膦酸),DTPMP(二乙基三胺基五亚甲基膦酸)的153Sm配合物以及HEDTMP,EDTMP,DTPMP的113,117Snm配合物在正辛醇 水中的表观脂水分配系数和在0 5%牛血清白蛋白(BSA)水溶液中与BSA的结合率。结果表明,这些配合物在正辛醇 水中的相对表观脂水分配系数和在BSA水溶液中与BSA的相对结合率呈线性正相关。两者之间的线性关系为这类配合物脂水分配系数的预测提供了一种新方法,同时也表明,在金属配合物与BSA的结合过程中,疏水作用力起着重要作用。Apparent partition coefficient in octanol-water and binding percentage to BSA of ^(153)Sm-NTMP, ^(153)Sm-HEDTMP, ^(153)Sm-DCTMP, ^(153)Sm-EDTMP, ^(153)Sm-DTPMP, ^(113,117) Sn^m-EDTMP, ^(113,117) Sn^m-HEDTMP, ^(113,117) Sn^m-DTPMP are measured. The results show that there is a linear relationship between the relative magnitude of the apparent partition coefficient in octanol-watetr and the relative magnitude of the binding percentage to BSA of these ^(153)Sm(^(113,117)Sn^m) complexes. This linear relationship provides a new method for determination of the apparent partition coefficient in octanol-water of ^(153)Sm(^(113,117)Sn^m) complexes of this kind. This linear relationship also implicates that hydrophobic force plays an important role in the binding of ^(153)Sm(^(113,117)Sn^m)complexes to BSA.

关 键 词：药物转运代谢 钐配合物 锡配合物 脂水分配系数 结合常数 烷基膦酸 正辛醇-水 牛血清白蛋白 

分 类 号：R969.1[医药卫生—药理学]