RELAXOMETRY, ANIMAL BIODISTRIBUTION, AND MAGNETIC-RESONANCE-IMAGING STUDIES OF SOME NEW GADOLINIUM-(III) MACROCYCLIC PHOSPHINATE AND PHOSPHONATE MONOESTER COMPLEXES
RELAXOMETRY, ANIMAL BIODISTRIBUTION, AND MAGNETIC-RESONANCE-IMAGING STUDIES OF SOME NEW GADOLINIUM-(III) MACROCYCLIC PHOSPHINATE AND PHOSPHONATE MONOESTER COMPLEXES
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DOI：
10.1002/mrm.1910300607
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发表时间：
1993-12-01
影响因子：
3.3
通讯作者：
MULLER, RN
中科院分区：
文献类型：
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作者：
GERALDES, CFGC;SHERRY, AD;MULLER, RN
三种新的含磷四氮杂大环化合物（1,4,7,10-四氮杂环十二烷-1,4,7,10-四（亚甲基乙基膦酸），H4DOTEP；1,4,7,10-四氮杂环十二烷-1,4,7,10-四（亚甲基膦酸单乙酯），H4DOTPME；以及相应的Gd3+配合物制备并检查了正丁酯 (H4DOTPMB) 作为 MRI 造影剂的可能性。尽管在盐水和 HSA 溶液中热力学和动力学稳定性不如 Gd(DOTA)-，但这些新的大环配合物的稳定性对于体内应用来说似乎足够高。三种配合物的 NMRD 弛豫曲线表明这些螯合物的内球水分子数量小于或等于 1，并且疏水性更强的螯合物 Gd(DOTPMB) 与人血清白蛋白 (HSA) 结合。放射性 Sm-153 或 Gd-159 螯合物在大鼠体内的生物分布研究、Sm-153 螯合物在大鼠体内的伽马成像以及非放射性物质的质子 MRI 研究。兔子体内的 Gd3+ 螯合物均表明 DOTPMB 复合物优先在肝脏、脾脏和小肠中积聚，而亲水性更强的 DOTEP 和 DOTPME 复合物似乎显示出与其他低分子量造影剂类似的肾脏清除率。
The Gd3+ complexes of three new phosphorus containing tetraaza macrocycles (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis (methylene ethylphosphonic acid), H4DOTEP; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis (methylene phosphonic acid monoethylester), H4DOTPME; and the corresponding n-butyl ester, H4DOTPMB) were prepared and examined for possible use as MRI contrast agents. Although thermodynamically and kinetically less stable than Gd(DOTA)- in saline and HSA solution, the stability of these new macrocyclic complexes appears to be sufficiently high for In vivo applications. NMRD relaxivity profiles of the three complexes indicate that the number of inner sphere water molecules for these chelates is less-than-or-equal-to 1 and that the more hydrophobic chelate, Gd(DOTPMB), binds to human serum albumin (HSA). Biodistribution studies of the radioactive Sm-153 or Gd-159 chelates in rats, gamma imaging of the Sm-153 chelates in rats, and proton MRI studies of the nonradioactive. Gd3+ chelates in rabbits all indicate that the DOTPMB complexes accumulate preferentially in the liver, spleen, and small intestines while the more hydrophilic DOTEP and DOTPME complexes appear to display renal clearances similar to other low molecular weight contrast agents.