Fluorescence-enhanced europium-diethylenetriaminepentaacetic (DTPA)-monoamide complexes for the assessment of renal function

被引：37

作者：

Chinen, Lori K. ^{[1
]}

Galen, Karen P. ^{[1
]}

Kuan, K. T. ^{[1
]}

Dyszlewski, Mary E. ^{[1
]}

Ozaki, Hiroaki ^{[2
]}

Sawai, Hiroaki ^{[2
]}

Pandurangi, Raghootama S. ^{[1
]}

Jacobs, Frederick G. ^{[1
]}

Dorshow, Richard B. ^{[1
]}

Rajagopalan, Raghavan ^{[1
]}

机构：

[1] Covidien Inc, Hazelwood, MO 63042 USA

[2] Gunma Univ, Grad Sch Engn, Dept Chem & Biol Chem, Gunma 3768515, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 04期

关键词：

D O I：

10.1021/jm070842+

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 In-111 complex 18a, and the data suggest that this complex clears via a complex mechanism that includes glomerular filtration.

引用

页码：957 / 962

页数：6

共 42 条

[1] EXCITATION AND DE-EXCITATION PROCESSES IN LANTHANIDE CHELATES BEARING AROMATIC SIDECHAINS [J].