Synthesis and Physicochemical Characterization of Gd-DTPA-B(sLex)A, a New MRI Contrast Agent Targeted to Inflammation

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• 作者：Sophie Laurent ; Luce Vander Elst ; Yanjun Fu ; and Robert N. Muller
• 刊名：Bioconjugate Chemistry
• 出版年：2004
• 出版时间：January 2004
• 年：2004
• 卷：15
• 期：1
• 页码：99 - 103
• 全文大小：97K
• 年卷期：v.15,no.1(January 2004)
• ISSN：1520-4812

文摘

A new magnetic resonance imaging (MRI) contrast agent designed to mimic sialyl Lewis X (sLe^X) andto target inflammation has been synthesized and characterized. The evolution of its proton longitudinalrelaxivity as a function of the magnetic field (NMRD) and temperature has been studied. The exchangerate of the water coordinated to the metal has been assessed by oxygen-17 relaxometry. Thetransmetalation by zinc(II) ions and the noncovalent binding to human serum albumin have beenevaluated. The results show no limitation by the residence time of the coordinated water moleculeabove room temperature, a higher stability of the complex versus transmetalation by zinc(II) ionsthan a parent complex, the clinically used Gd-DTPA-BMA, and negligible interaction with humanserum albumin.