Comparative Chemical Structure and Pharmacokinetics of MRI Contrast Agents

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Abstract
Tweedle MF, Eaton SM, Eckelman WC, Gaughan GT, Hagan JJ, Wedeking PW, Yost FJ. Comparative chemical structure and pharmacokinetics of MRI contrast agents. Invest Radiol 1988; 23(Suppl 1):S236-S239. The blood clearance kinetics of five gadolinium complexes, Gd(L), were determined in rats and the results interpreted in terms of an open two-compartment pharmacokinetic model. The complexes were tested in vitro for stability in serum and in aqueous solutions of ions that they might encounter in vivo and that might be expected to react with the Gd(L) complexes to produce uncomplexed gadolinium. Reaction with serum was observed in two instances. Chemical structural differences among the chelating ligands appear to govern the overall reactivity of their Gd(L) complexes. It may be inferred from the results that a preferred structural feature of the ligand is the presence of a 12-membered 1,4,7,10-tetraaza macrocycle.

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