Amide conjugates of the DO3A-N-(alpha-amino)propionate ligand: leads for stable, high relaxivity Contrast Agents for MRI?
| Autor: | Ferreira, M.F., Martins, A.F., Martins, C.I.O., Tóth, É., Rodrigues, T.B., Calle, D., Cerdan, S., López-Larrubia, P., Martins, J.A., Geraldes, C.F.G.C. |
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| Přispěvatelé: | Centre de biophysique moléculaire (CBM), Université d'Orléans (UO)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC) |
| Jazyk: | angličtina |
| Rok vydání: | 2013 |
| Předmět: | |
| Zdroj: | Contrast Media and Molecular Imaging Contrast Media and Molecular Imaging, Wiley, 2013, 8 (1), pp.40-49. ⟨10.1002/cmmi.1492⟩ |
| ISSN: | 1555-4309 1555-4317 |
| DOI: | 10.1002/cmmi.1492⟩ |
| Popis: | International audience; A 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 Zn(2+) . 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. |
| Databáze: | OpenAIRE |
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