Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5266309 | Tetrahedron Letters | 2012 | 4 Pages |
Abstract
Novel chiral dendrimer-triamine-coordinated Gd complexes were synthesized and shown to have longitudinal relaxivity (r1) 3 times higher than that of clinically used Gd-DTPA. The pharmacokinetic differences between optical isomers were estimated from the affinity of 2-(R) and 2-(S) with bovine serum albumin (BSA), respectively, by a quartz crystal microbalance (QCM) measurement. As a result, the association constant Ka of 2-(S) was about 4 times higher than that of 2-(R), which means that 2-(S) is retained in the vascular retention for a longer time after administration. This result was also supported by T1-weighted MR images of mice before and after the intravenous injection of 2-(R) and 2-(S), as well as the time-course of the signal intensities (SI) at the blood vessels and quantification of Gd3+ concentration in the blood and urine.
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Authors
Yuka Miyake, Yu Kimura, Syungo Ishikawa, Hiroshi Tsujita, Hiroki Miura, Michiko Narazaki, Tetsuya Matsuda, Yasuhiko Tabata, Tetsuya Yano, Akio Toshimitsu, Teruyuki Kondo,