Fluorescence-Enhanced Europium-Diethylenetriaminepentaacetic (DTPA)-Monoamide Complexes for the Assessment of Renal Function

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• 作者：Lori K. Chinen ; Karen P. Galen ; K. T. Kuan ; Mary E. Dyszlewski ; Hiroaki Ozaki ; Hiroaki Sawai ; Raghootama S. Pandurangi ; Frederick G. Jacobs ; Richard B. Dorshow ; Raghavan Rajagopalan
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：February 28, 2008
• 年：2008
• 卷：51
• 期：4
• 页码：957 - 962
• 全文大小：110K
• 年卷期：v.51,no.4(February 28, 2008)
• ISSN：1520-4804

文摘

Real-time, noninvasive assessment of glomerular filtration rate (GFR) is essential not only for monitoring critically ill patients at the bedside, but also for staging and monitoring patients with chronic kidney disease. In our pursuit to develop exogenous luminescent probes for dynamic optical monitoring of GFR, we have prepared and evaluated Eu³⁺ complexes of several diethylenetriamine pentaacetate (DTPA)-monoamide ligands bearing molecular “antennae” to enhance metal fluorescence via intramolecular ligand–metal fluorescence resonance energy transfer process. The results show that Eu-DTPA-monoamide complex 18b, which contains a quinoxanlinyl antenna, exhibits large (ca. 2700-fold) Eu³⁺ fluorescence enhancement. Indeed, complex 18b exhibits the highest fluorescent enhancement observed thus far in the DTPA-type metal complexes. The renal clearance property was assessed using the corresponding radioactive ¹¹¹In complex 18a, and the data suggest that this complex clears via a complex mechanism that includes glomerular filtration.