Development of new glucosylated derivatives of gadolinium diethylenetriaminepentaacetic for magnetic resonance angiography.
OBJECTIVE
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.
Burtea
Carmen
C
NMR Laboratory, Department of Organic Chemistry, University of Mons-Hainaut, Mons, Belgium.
Laurent
Sophie
S
Colet
Jean-Marie
JM
Vander Elst
Luce
L
Muller
Robert N
RN
D000818:Animals; D003287:Contrast Media / Q000737:chemistry / Q000493:pharmacokinetics; D019786:Gadolinium DTPA / Q000031:analogs & derivatives*; D006801:Humans; D018810:Magnetic Resonance Angiography; D008297:Male; D051381:Rats; D014018:Tissue Distribution
D003287:Contrast Media; D019786:Gadolinium DTPA