Abstract
Four neutral gadolinium complexes of diethylenetriaminepentaacetic acid (DTPA)-bisamide derivatives have been synthesized and characterized. Their potential application as tissue-specific and low-osmolarity MRI contrast agents has been evaluated by in vitro and in vivo experiments. Their measured relaxivities in D 2O, bovine serum albumin and human serum transferrin solutions showed favorable relaxation ability. In vivo studies have proven that Gd(DTPA–BDMA), Gd(DTPA–BIN), and Gd(cyclic-DTPA–1,2-pn) could be promising liver-specific MRI contrast agents and Gd(DTPA–BDMA), and Gd(cyclic-DTPA–1,2-pn) have favorable renal excretion capability. Among them, Gd(cyclic-DTPA–1,2-pn) is a more powerful hepatic contrast agent and Gd(DTPA–BIN) provides the stable imaging contrast for several hours. They also show a lower toxicity.
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