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Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vitro and in vivo studies
- Source :
- Repositório Científico de Acesso Aberto de Portugal, Repositório Científico de Acesso Aberto de Portugal (RCAAP), instacron:RCAAP
- Publication Year :
- 2011
- Publisher :
- Elsevier, 2011.
-
Abstract
- 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.<br />Fundação para a Ciência e a Tecnologia (FCT)
- Subjects :
- Male
Cancer Research
Biodistribution
Stereochemistry
Gallium Radioisotopes
Gallium
010402 general chemistry
Ligands
01 natural sciences
Micelle
chemistry.chemical_compound
Heterocyclic Compounds, 1-Ring
Blood serum
Amphiphile
Radiopharmacy
DOTA
Animals
Humans
Radiology, Nuclear Medicine and imaging
Chelation
Rats, Wistar
Amphiphilic
Micelles
Chelating Agents
Science & Technology
010405 organic chemistry
Ligand
Combinatorial chemistry
3. Good health
0104 chemical sciences
Rats
PET
chemistry
Lipophilicity
Molecular Medicine
Hydrophobic and Hydrophilic Interactions
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Repositório Científico de Acesso Aberto de Portugal, Repositório Científico de Acesso Aberto de Portugal (RCAAP), instacron:RCAAP
- Accession number :
- edsair.doi.dedup.....05d9cac9184f1ecc1d8f9f753d847cec