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[配体EOB-DTPA的络合特性及钆(EOB-DTPA)的动力学稳定性]

[Complexation properties of the ligand EOB-DTPA and the kinetic stability of Gd(EOB-DTPA)].

作者信息

Burai L, Brücher E, Király R, Solymosi P, Víg T

机构信息

Debreceni Egyetem, Szervetlen és Analitikai Kémiai Tanszék, 4010 Debrecen.

出版信息

Acta Pharm Hung. 2000 Jul-Dec;70(3-6):89-96.

Abstract

Due to the presence of the ethoxy-benzyl group, the lipophilicity of the complex Gd(EOB-DTPA)2- is higher than that of Gd(DTPA)2- and thus Gd(EOB-DTPA)2- can be used as a liver specific contrast agent in Magnetic Resonance Imaging. The stability constants of the complexes of Fe2+, Fe3+, Zn2+ and Cu2+ formed with EOB-DTPA practically agree with those of the respective DTPA complexes. The complexes of EOB-DTPA formed with larger metal ions, like Ca2+, Ba2+, Gd3+ and other lanthanides, exhibit larger stability constants than the complexes of DTPA by 0.5-1 logK unit. The stability constants of the complexes Ln(EOB-DTPA)2- increase with increasing atomic number till the middle of the series. For the elements Tb to Ho the logKLnL values are approximately equal and a weak decrease can be observed for the heaviest elements, probably because of steric hindrance between the functional groups. The exchange reactions between the complex Gd(EOB-DTPA)2- and Y3+ ions occur predominantly through the formation and rate determining dissociation of the mono- and diprotonated complexes. The rate constants characterizing these reaction pathways are lower by a factor of three than the respective rate constants, known for the dissociation of Gd(DTPA)2-. On the basis of its higher kinetic stability, Gd(EOB-DTPA)2- can be used for in vivo investigations in medical diagnosis.

摘要

由于乙氧基苄基的存在,配合物Gd(EOB-DTPA)2-的亲脂性高于Gd(DTPA)2-,因此Gd(EOB-DTPA)2-可作为磁共振成像中的肝脏特异性造影剂。Fe2+、Fe3+、Zn2+和Cu2+与EOB-DTPA形成的配合物的稳定常数实际上与各自的DTPA配合物的稳定常数一致。EOB-DTPA与较大金属离子(如Ca2+、Ba2+、Gd3+和其他镧系元素)形成的配合物的稳定常数比DTPA配合物大0.5-1个logK单位。配合物Ln(EOB-DTPA)2-的稳定常数随着原子序数的增加而增大,直至该系列的中间位置。对于铽到钬元素,logKLnL值大致相等,而对于最重的元素,可以观察到稳定常数略有下降,这可能是由于官能团之间的空间位阻。配合物Gd(EOB-DTPA)2-与Y3+离子之间的交换反应主要通过单质子化和双质子化配合物的形成以及速率决定解离来发生。表征这些反应途径的速率常数比Gd(DTPA)2-解离的相应速率常数低三倍。基于其较高的动力学稳定性,Gd(EOB-DTPA)2-可用于医学诊断的体内研究。

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