Harrison A, Walker C A, Pereira K A, Parker D, Royle L, Pulukkody K, Norman T J
Medical Research Council, Radiobiology Unit, Chinton, Oxon, UK.
Magn Reson Imaging. 1993;11(6):761-70. doi: 10.1016/0730-725x(93)90194-i.
Tissue distribution of 21 new 157/153Gd complexes was measured at 5 min and 24 hr after an intravenous injection into mice. A complex was judged to be stable in vivo when the percentage of 153Gd retained in the liver and skeleton at 24 hr was comparable with that of 153Gd(DOTA)-. Complexes varied in net charge and lipophilicity and 20 were phosphinic or carboxylic acid derivatives of tetra-aza-cyclo-dodecane. Three anionic, lipophilic complexes were cleared predominantly by the hepato-biliary pathway and were stable in vivo. The remaining 18 complexes were cleared mainly by the kidneys. Of these 18, 1 anionic, 8 neutral, and 3 cationic complexes were stable in vivo. These findings augur well for the future of hepato-biliary and general purpose Gd contrast enhancing agents for MRI.
将21种新的157/153Gd配合物静脉注射到小鼠体内后，在5分钟和24小时测量其组织分布。当24小时时肝脏和骨骼中保留的153Gd百分比与153Gd（DOTA）-的百分比相当时，判断一种配合物在体内是稳定的。配合物的净电荷和亲脂性各不相同，20种是四氮杂环十二烷的次膦酸或羧酸衍生物。三种阴离子亲脂性配合物主要通过肝胆途径清除，且在体内稳定。其余18种配合物主要通过肾脏清除。在这18种配合物中，1种阴离子、8种中性和3种阳离子配合物在体内稳定。这些发现为用于MRI的肝胆和通用钆造影剂的未来发展预示了良好前景。
