DISSOCIATION OF GADOLINIUM CHELATES IN MICE - RELATIONSHIP TO CHEMICAL CHARACTERISTICS

被引：191

作者：

WEDEKING, P ^{[1
]}

KUMAR, K ^{[1
]}

TWEEDLE, MF ^{[1
]}

机构：

[1] BRISTOL MYERS SQUIBB PHARMACEUT RES INST,CONTRAST MEDIA RES DEPT,NEW BRUNSWICK,NJ 08903

来源：

MAGNETIC RESONANCE IMAGING | 1992年 / 10卷 / 04期

关键词：

MRI CONTRAST AGENTS; GADOLINIUM; TISSUE DISTRIBUTION; ACID DISSOCIATION; THERMODYNAMIC EQUILIBRIUM; CONDITIONAL STABILITY; LIPOPHILICITY;

D O I：

10.1016/0730-725X(92)90016-S

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

Tissue distributions of seven Gd-153-labeled Gd chelates were determined at five residence intervals (5 min to 14 days) following intravenous administration of 0.4 mmol/kg to mice. Relationships were sought among physico-chemical parameters: thermodynamic and conditional (pH 7.4) equilibrium stability constants (log K and log K'), acid dissociation rate constants (k(obs)), lipophilicity (log P), overall charge, and size (molecular weight). Size and lipophilicity did not correlate with tissue distributions. There were possible correlations between anionic charge and rapid, early renal excretion and between stability constants and long-term residual Gd deposition. Strong correlations (r > 0.99) were found between acid dissociation rates and long-term deposition of Gd in the whole body, liver, and femur. This is attributed to dissociation of Gd from the chelates in vivo. Acid dissociation rates may be useful in predicting dissociation of Gd from chelates in vivo.

引用

页码：641 / 648

页数：8

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