期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 14, 期 24, 页码 7250-7258出版社
WILEY-BLACKWELL
DOI: 10.1002/chem.200800402
关键词
dendrimers; imaging agents; lanthanide complexes; MRI contrast agents
资金
- National Institutes of Health [RR-02584, CA-126608, CA-115531]
- Robert A. Welch Foundation [AT-584]
- NATIONAL CANCER INSTITUTE [U24CA126608, R01CA115531] Funding Source: NIH RePORTER
- NATIONAL CENTER FOR RESEARCH RESOURCES [P41RR002584] Funding Source: NIH RePORTER
The design of effective pH responsive MRI contrast agents is a key goal in the development of new diagnostic methods for conditions Such as kidney disease and cancer. A key factor determining the effectiveness of an agent is the difference between the relaxivity of the on state compared to that of the off state. In this paper, we demonstrate that it is possible to improve the pH-responsive action of a low molecular weight agent by conjugating it to a macromolecular construct. The synthesis of it bifunctional pH responsive agent is reported. As part of that synthetic pathway we examine the Ing-Manske reaction, identifying an undesirable by-product and establishing effective conditions for promoting a clean and effective reaction. Reaction of the bifunctional pH responsive agent with a G5-PAMAM dendrimer yielded a product with an average of 96 chelates per dendrimer. The relaxivity of the dendrimer conjugate rises from 10.8mM(-1)s(-1) (pH 9) to 24.0 mM(-1)s(-1) (pH 6) per Gd(3+) ion. This more than doubles the relaxivity pH response, Art, of our agent from just 51 % for the original low molecular weight chelate to 122% for the dendrimer.
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