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2005-01-01 - Article/Dans un journal avec peer-review - Anglais - 9 page(s)

Kubicek V., Rudovsky J., Kotek J., Hermann P., Vander Elst Luce , Muller Robert , Kolar Z.I., Wolterbeek H.T., Peters J. A., Lukes I., "A bisphosphonate monoamide analogue of DOTA: A potential agent for bone targeting" in Journal of the American Chemical Society, 127, 47, 16477-16485

  • Edition : American Chemical Society, Washington (DC)
  • Codes CREF : Résonance magnétique nucléaire (biophysique) (DI131B), Chimie organique (DI1313), Imagerie médicale, radiologie, tomographie (DI3243)
  • Unités de recherche UMONS : Chimie générale, organique et biomédicale (M108)
Texte intégral :

Abstract(s) :

(Anglais) A new macrocyclic DOTA-like ligand (BPAMD) for bone imaging and therapy containing a monoamide bis(phosphonic acid) bone-seeking group was designed and synthesized. Its lanthanide(ill) complexes were prepared and characterized by H-1 and P-31 INIMR spectroscopy. The Gd(III)-BPAMD complex was investigated in detail by H-1 and O-17 relaxometric studies to inspect parameters relevant for its potential application as an MRI contrast agent. Sorption experiments were conducted with Gd(Ill) and Tb(III) complexes using hydroxyapatite (HA) as a model of bone surface. Very effective uptake of the Gd-BPAMD complex by the HA surface was observed in NMR experiments. Radiochemical studies with the (Tb-160-BPAMD)-HA system proved the sorption to be remarkably fast and strong on one hand and fully reversible on the other hand. The strong (Gd-BPAMD)-HA interaction was also supported by H-1 NMRD measurements in the presence of a hydroxyapatite slurry, which showed an increase of the rotational correlation time upon adsorption of the complex on the HA surface, resulting in a significant relaxivity enhancement. The amide-bis(phosphonate) moiety is the only factor responsible for the binding of the complex to HA.