EVALUATION DE NOUVEAUX RADIOPHARMACEUTIQUES
Synthèse, évaluation, et biodistribution de nouveaux radioligands peptidiques de VCAM-1 et avb3

Abstract : The development of nuclear medicine implies the search for new isotopes but also for new vectors specific of functions or metabolic pathways. We investigated new radiopharmaceuticals intended for new diagnostic approaches of two physiopathological mechanisms frequently met in our populations: the atherosclerosis vulnerable plaque and the tumor angiogenesis. We studied and optimized the iodine and 99m-technetium radiolabelling, of a series of peptides in order to allow the in vivo use of these tracers for imaging studies in animals and possibly in humans. The radioiodination was carried out by electrophilic substitution, and technetium was linked by a tricarbonyle BFCA (IsoLink). The reaction parameters were defined so that the labelling reaction presents a high radiochemical purity (>95%), and a high specific activity. The reactions are fast and reproducible. Various physicochemical properties: liposolubility, stability of labelling, and pharmacokinetic properties: nonspecific binding, metabolization and organ biodistribution of peptides in animal model, were studied. These results indicate which peptide may be a suitable candidate for targeting trials.
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Contributor : Valérie Ardisson <>
Submitted on : Thursday, December 7, 2006 - 6:15:27 PM
Last modification on : Thursday, January 18, 2007 - 3:44:50 PM
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Valérie Ardisson. EVALUATION DE NOUVEAUX RADIOPHARMACEUTIQUES
Synthèse, évaluation, et biodistribution de nouveaux radioligands peptidiques de VCAM-1 et avb3. Médicaments. Université Joseph-Fourier - Grenoble I, 2006. Français. ⟨tel-00119156⟩

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