A bisphosphonate monoamide analogue of DOTA: A potential agent for bone targeting

[en] 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.

Disciplines :

Radiology, nuclear medicine & imaging
Chemistry

Author, co-author :

Kubicek, V.

Rudovsky, J.

Kotek, J.

Hermann, P.

Vander Elst, Luce ; Université de Mons > Faculté de Médecine et de Pharmacie > Biochimie métabolique et moléculaire

Muller, Robert ; Université de Mons > Faculté de Médecine et de Pharmacie > Chimie générale, organique et biomédicale

Kolar, Z.I.

Wolterbeek, H.T.

Peters, J. A.

Lukes, I.

Language :

English

Title :

A bisphosphonate monoamide analogue of DOTA: A potential agent for bone targeting

Publication date :

01 January 2005

Journal title :

Journal of the American Chemical Society

ISSN :

0002-7863

Publisher :

American Chemical Society, United States - District of Columbia

Volume :

127

Issue :

Pages :

16477-16485

Peer reviewed :

Peer Reviewed verified by ORBi

Research unit :

M108 - Chimie générale, organique et biomédicale

Available on ORBi UMONS :

since 10 June 2010

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141

Scopus citations^®
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115

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