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NOUVEAUX RADIOTRACEURS PEPTIDIQUES POUR L'IMAGERIE NUCLEAIRE
Radiomarquage, évaluations physico-chimiques et pharmacologiques

Abstract : During the past decade, radiolabeled peptides have emerged as an important class of radiopharmaceuticals for diagnosis and therapy in nuclear medicine. The concept of using radiolabeled peptides in vivo stimulates a large body of research for new peptidic vectors but also for radiochemical and radiopharmaceutical evaluations of these peptides after labeling.
We studied and optimized the 99m-technetium, 125-iodine and 111-indium radiolabeling of a serie of peptides in order to allow the in vivo use of these tracers for imaging studies of three pathologies: tumoral angiogenesis, atherosclerosis and systemic lupus erythematosus. The radiolabeling with technetium was carried out using a tricarbonyle agent (IsoLink) and Indium was linked by DOTA macromolecule. Radioiodination was realized by electrophilic substitution.
The reaction parameters were defined so that the labeling reaction presents a high radiochemical purity (>95%) and a high specific activity. The reactions were fast and reproducible. Various physicochemical and pharmacokinetic properties (lipophily, stability of labeling in vitro and in vivo, non-specific fixation, metabolization and organ biodistribution of peptides) were studied. These results permitted to select the best peptide for in vivo imaging.
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https://tel.archives-ouvertes.fr/tel-00332512
Contributor : Mitra Ahmadi <>
Submitted on : Thursday, February 11, 2010 - 7:00:05 AM
Last modification on : Friday, November 6, 2020 - 4:04:21 AM
Long-term archiving on: : Wednesday, November 30, 2016 - 10:07:55 AM

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Mitra Ahmadi. NOUVEAUX RADIOTRACEURS PEPTIDIQUES POUR L'IMAGERIE NUCLEAIRE
Radiomarquage, évaluations physico-chimiques et pharmacologiques. Sciences pharmaceutiques. Université Joseph-Fourier - Grenoble I, 2008. Français. ⟨tel-00332512⟩

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