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Amide conjugates of the DO3A-N-(α-amino)propionate ligand: leads for stable, high relaxivity contrast agents for MRI?

AuthorsFerreira, Miguel F.; Rodrigues, Tiago B.; Calle, Daniel ; Cerdán, Sebastián ; López-Larrubia, Pilar ; Martins, José A.; Geraldes, Carlos F. G. C.
Issue Date2013
CitationContrast Media and Molecular Imaging 8(1): 40-49 (2013)
AbstractA novel synthetic methodology for preparing amide conjugates of the DO3A-N-(α-amino)propionate chelator is described, using the synthesis of the DO3A-N-(α-benzoylamido)propionate chelator as an illustrative example. The model Gd[DO3A-N-(α-benzoylamido)propionate] chelate displays accelerated water exchange, stability in a wide pH range and inertness towards transmetallation by Zn2+. The Gd[DO3A-N-(α-benzoylamido)propionate] complex is mainly excreted via the kidneys, producing a significant increase in the kidney medulla/cortex enhancement ratio in MR images of Wistar rats, reflecting probably its higher lipophilicity compared with Gd(DTPA). The results presented suggest that Gd[DO3A-N-(α-amido)propionate] chelates can be valuable leads for preparing potentially safe high relaxivity MRI contrast agents. Copyright © 2012 John Wiley & Sons, Ltd.
Descriptionet al.
Publisher version (URL)http://dx.doi.org/10.1002/cmmi.1492
Identifiersdoi: 10.1002/cmmi.1492
issn: 1555-4309
e-issn: 1555-4317
Appears in Collections:(IIBM) Artículos
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