Physical parameters and biological stability of yttrium(III) diethylenetriaminepentaacetic acid derivative conjugates

被引：75

作者：

McMurry, TJ ^{[1
]}

Pippin, CG ^{[1
]}

Wu, CC ^{[1
]}

Deal, KA ^{[1
]}

Brechbiel, MW ^{[1
]}

Mirzadeh, S ^{[1
]}

Gansow, OA ^{[1
]}

机构：

[1] NCI, NIH, Bethesda, MD 20892 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 18期

关键词：

D O I：

10.1021/jm980152t

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The solution equilibria, acid dissociation, and serum stability of a series of Y(III) complexes of DTPA ligands functionalized with p-nitrobenzyl, methyl, and trans-cyclohexyl substituents were studied. The thermodynamic stability of the complexes studied ranged from log K = 21.53 to 24.7. Acid dissociation rates were found to decrease as the substitution on the carbon backbone increased, and significant differences in dissociation rates were observed for the Y(III) complexes of a pair of diasteriomeric cyclohexyl-DTPA ligands. While one diastereomer was found to have the slowest acid dissociation rate of the entire DTPA series, it was remarkably labile in both serum stability and in vivo studies.

引用

页码：3546 / 3549

页数：4

共 34 条

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