Synthesis, Characterization, and Biodistribution of a Dinuclear Gadolinium Complex with Improved Properties as a Blood Pool MRI Agent.
ChemMedChem
; 13(8): 824-834, 2018 04 23.
Article
em En
| MEDLINE
| ID: mdl-29442438
ABSTRACT
A dinuclear gadolinium(III) chelate containing two moieties of diethylenetriaminepentaacetic acid (DTPA), covalently conjugated to an analogue of deoxycholic acid, was synthesized and thoroughly characterized. A full relaxometric analysis was carried out, consisting of 1)â
the acquisition of nuclear magnetic resonance dispersion (NMRD) profiles in various media; 2)â
the study of binding affinity to serum albumin; 3)â
the measurement of 17 O transverse relaxation rate versus temperature, and 4)â
a transmetallation assay. In vivo biodistribution MRI studies at 1â
T and blood pharmacokinetics assays were carried out in comparison with Gd-DTPA (Magnevist) and gadocoletic acid trisodium salt (B22956/1), two well-known Gd complexes that share the same chelating cage and the same deoxycholic acid residue of the Gd complex investigated herein ((GdDTPA)2 -Chol). High affinity for plasma protein and, in particular, the availability of more than one binding site, allows the complex to reach a fairly high relaxivity value in plasma (â¼20â
mm-1 s-1 , 20â
MHz, 310â
K) as well as to show unexpectedly enhanced properties of blood pooling, with an elimination half-life in rats approximately seven times longer than that of B22956/1.
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Base de dados:
MEDLINE
Assunto principal:
Meios de Contraste
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Gadolínio DTPA
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Ácido Desoxicólico
Limite:
Animals
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article