Publicação
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies
| Resumo: | In this work we report a synthetic strategy of amphiphilic DOTA-based chelators bearing a variable size α-alkyl chain at one of the pendant acetate arms (from six to fourteen carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micelle concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the 67Ga-labeled chelates were performed in Wistar rats showing a predominant liver uptake with almost no traces of the radiochelates in the body after 24 hours. |
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| Autores principais: | Fontes, André Filipe Gomes Soares |
| Outros Autores: | Prata, M. Isabel M.; Geraldes, Carlos F. G. C.; André, João P. |
| Assunto: | DOTA Gallium Amphiphilic Micelles Radiopharmacy PET |
| Ano: | 2011 |
| País: | Portugal |
| Tipo de documento: | artigo |
| Tipo de acesso: | acesso aberto |
| Instituição associada: | Universidade do Minho |
| Idioma: | inglês |
| Origem: | RepositóriUM - Universidade do Minho |
| Resumo: | In this work we report a synthetic strategy of amphiphilic DOTA-based chelators bearing a variable size α-alkyl chain at one of the pendant acetate arms (from six to fourteen carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micelle concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the 67Ga-labeled chelates were performed in Wistar rats showing a predominant liver uptake with almost no traces of the radiochelates in the body after 24 hours. |
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