Kinetic inertness is a key property for a Gd-based contrast agent. The Gd-III complex of a cyclohexyl-fused AAZTA derivative shows the highest kinetic inertness for non-macrocyclic bis hydrated (q = 2) Gd-III-complexes with a dissociation half-life of 91 years under physiological conditions, very close to that of macrocyclic clinically approved contrast agents. It also shows optimal relaxometric performance (r(1) = 8.3 mM(-1) s(-1) at 20 MHz and 25 degrees C) due to the presence of two inner sphere water molecules in fast exchange with bulk water and not displaced by endogenous anions.

High kinetic inertness of a bis-hydrated Gd-complex with a constrained AAZTA-like ligand

TEI, LORENZO
2016-01-01

Abstract

Kinetic inertness is a key property for a Gd-based contrast agent. The Gd-III complex of a cyclohexyl-fused AAZTA derivative shows the highest kinetic inertness for non-macrocyclic bis hydrated (q = 2) Gd-III-complexes with a dissociation half-life of 91 years under physiological conditions, very close to that of macrocyclic clinically approved contrast agents. It also shows optimal relaxometric performance (r(1) = 8.3 mM(-1) s(-1) at 20 MHz and 25 degrees C) due to the presence of two inner sphere water molecules in fast exchange with bulk water and not displaced by endogenous anions.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11579/76789
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