RATIONALE AND OBJECTIVES: A possible approach for the extension of the vascular residence time of contrast agents relies on the renal reabsorption mechanisms of some molecules such as glucose. In this study, various small-molecular-weight glucosyl derivatives of gadolinium diethylenetriaminepentaacetic (Gd-DTPA) were synthesized and their vascular half-life was studied. METHODS: Several Gd-DTPA-bisamides carrying glucosyl groups bound by different linkers were prepared. The pharmacokinetics and biodistribution of these compounds were determined on Wistar rats. RESULTS: The sugar moieties linked to Gd-DTPA efficiently reduce the renal excretion of some derivatives. The interaction with renal carrier has not been clearly demonstrated, nor was any interaction observed with blood components. CONCLUSIONS: Two of the new glucosylated derivatives of Gd-DTPA (Cd-DTPA-BC2-beta-cellobionA 2 and Gd-DTPA-BC4-beta-glucosylA 7) can be proposed as blood-pool MR contrast agents, considering their vascular remanence.
RATIONALE AND OBJECTIVES: A possible approach for the extension of the vascular residence time of contrast agents relies on the renal reabsorption mechanisms of some molecules such as glucose. In this study, various small-molecular-weight glucosyl derivatives of gadolinium diethylenetriaminepentaacetic (Gd-DTPA) were synthesized and their vascular half-life was studied. METHODS: Several Gd-DTPA-bisamides carrying glucosyl groups bound by different linkers were prepared. The pharmacokinetics and biodistribution of these compounds were determined on Wistar rats. RESULTS: The sugar moieties linked to Gd-DTPA efficiently reduce the renal excretion of some derivatives. The interaction with renal carrier has not been clearly demonstrated, nor was any interaction observed with blood components. CONCLUSIONS: Two of the new glucosylated derivatives of Gd-DTPA (Cd-DTPA-BC2-beta-cellobionA 2 and Gd-DTPA-BC4-beta-glucosylA 7) can be proposed as blood-pool MR contrast agents, considering their vascular remanence.