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Título

Biodistribution of [18F]Amylovis®, a new radiotracer for PET imaging of ß-amyloid plaques

AutorFernández-Maza, L. ; Parrado-Gallego, Ángel; Fernández-Gómez, Isabel ; Balcerzyk, Marcin ; Rodríguez-Tanty, Chryslaine
Fecha de publicación2016
Citación18th European Sympossium in Radiopharmacy and Radiopharmaceuticals (2016)
Resumen[Aim]: [18F]-2-(3-fluoropropyl)-6-methoxynaphtalene ([18F]Amylovis®) is a new naphthalene-derivative for detecting β-amyloid plaques in Alzheimer’s disease. The aim of the study is the assessment of the animal biodistribution of this new radiotracer. [Material and methods]: [18F]Amylovis® was synthesized by nucleophilic substitution of the tosyl group of the precursor. Thirty five healthy male Balb/C mice of 10-12 weeks were divided into 6 groups of 5 animals each and injected with similar doses of [18F]Amylovis® through a lateral tail vein. Blood samples were collected and the animals were sacrificed at 5, 15, 30, 45, 70 and 180 minutes. Organs of interest were removed and washed with saline. Radioactivity of blood, plasma, urine, faeces, brain, cerebellum, heart, liver, stomach, spleen, bowel, colon, left kidney, muscle, bone and tail was measured in a well counter. To assess protein binding, plasma samples were diluted with acetonitrile and centrifuged at 4000 g. Pellets of proteins and supernatants were separated and their radioactivity measured in a well counter. RadioTLC analysis of plasma were performed for the same purpose in silicagel 60 and mobile phase of acetonitrile/water (95/5). 20μL of each supernatant was analysed by HPLC-RP using a C18 column and acetonitrile/water (75/25) as mobile phase to identify plasma metabolites. Pharmacokinetic parameters (AUC, t1/2, Cmax, Cl, Vss) were calculated using non-compartmental analysis (NCA). Dynamic PET/CT images of healthy and transgenic APPSwe/PS1dE9 mice were acquired for 2.5 h after i.v. administration. Immunohistochemistry of control and transgenic mice brains were performed to identify β-amyloid plaques. [Results]: [18F]Amylovis® crossed blood brain barrier. PET/CT images showed significant differences between healthy and transgenic mice, expressed in Cortex to cerebellum SUV ratio, with maximum difference at 30 minutes. Postmortem studies of immunohistochemistry showed also differences in healthy vs transgenic mice (amyloid positive). Plasma T1/2 of 37 min. No significant protein binding was observed. Renal and hepatic pathways were the main excretion routes. Some amount of in vivo degradation metabolites appeared in blood from 1 h post-administration. [Conclusion]: [18F]Amylovis® could be a promising PET radiotracer for amyloid plaques visualization.
DescripciónResumen del trabajo presentado al 18th European Sympossium in Radiopharmacy and Radiopharmaceuticals, celebrado en Salzburgo (Austria) del 7 al 10 de abril de 2016.-- et al.
URIhttp://hdl.handle.net/10261/158916
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