Towards an Improved Design of MRI Contrast Agents: Synthesis and Relaxometric Characterisation of Gd-HPDO3A Analogues(308 views) Tear LR, Carrera C, Gianolio E, Aime S
Chemistry (ISSN: 0947-6539linking, 1521-3765electronic), 2020 May 12; 26(27): 6056-6063.
Keywords: Contrast Media Chemistry, Europium Chemistry, Gadolinium Chemistry, Heterocyclic Compounds Chemistry, Kinetics, Lanthanoid Series Elements Chemistry, Magnetic Resonance Imaging Methods, Organometallic Compounds Chemistry, Water, Mri Contrast Agents, Lanthanides, Macrocycles, Relaxometry,
Affiliations: *** IBB - CNR ***
Department of Molecular Biotechnology and Health Sciences, Molecular Imaging Centre, University of Torino, Via Nizza 52, 10126, Torino, Italy.
Institute of Biostructures and Bioimaging, National Research Council, Via Nizza 52, 10126, Torino, Italy.
References: Not available.
Towards an Improved Design of MRI Contrast Agents: Synthesis and Relaxometric Characterisation of Gd-HPDO3A Analogues
The properties of Ln(III) -HPDO3A complexes as relaxation enhancers and paraCEST agents are essentially related to the hydroxylpropyl moiety. A series of three HPDO3A derivatives, with small modifications to the hydroxyl arm, were herein investigated to understand how heightened control can be gained over the parameters involved in the design of these agents. A full (1) H and (17) O-NMR relaxometric analysis was conducted and demonstrated that increasing the length of the OH group from the lanthanide centre significantly enhanced the water exchange rate of the gadolinium complex, but with a subsequent reduction in kinetic stability. Alternatively, the introduction of an additional methyl group, which increased the steric bulk around the OH moiety, resulted in the formation of almost exclusively the TSAP isomer (95 %) as identified by (1) H-NMR of the europium complex. The gadolinium analogue of this complex also exhibited a very fast water exchange rate, but with no detectable loss of kinetic stability. This complex therefore demonstrates a notable improvement over Gd-HPDO3A.
Towards an Improved Design of MRI Contrast Agents: Synthesis and Relaxometric Characterisation of Gd-HPDO3A Analogues
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Towards an Improved Design of MRI Contrast Agents: Synthesis and Relaxometric Characterisation of Gd-HPDO3A Analogues