title: Radiosynthesis and in vivo evaluation of a ¹⁸F-labelled styryl-benzoxazole derivative for β-amyloid targeting.
abstract: The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer's disease (AD). In vivo molecular imaging by means of amyloid-avid radiotracers will allow for an early and conclusive diagnostic of AD. Herein, we describe the radiosynthesis of the radiofluorinated styryl benzoxazole derivative [¹⁸F]-[2-[N-methyl-N-(2'-fluoroethyl)-4'-aminostyryl]benzoxazole] ([¹⁸F]-1) and its pre-clinical evaluation, including metabolic and biodistribution studies in male Wistar rats. The in vivo biological evaluation of [¹⁸F]-1 showed that this new radiotracer has a moderate brain uptake with a slow brain washout and a poor in vivo stability.
authors: Radiopharmaceutical Sciences Group, IST/ITN, Instituto Superior Técnico, Universidade Técnica de Lisboa, EN 10, 2686-953 Sacavem, Portugal.
authors: G
authors: G
authors: Ribeiro Morais
authors: L
authors: L
authors: Gano
authors: T
authors: T
authors: Kniess
authors: R
authors: R
authors: Bergmann
authors: A
authors: A
authors: Abrunhosa
authors: I
authors: I
authors: Santos
authors: A
authors: A
authors: Paulo
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000818:Animals; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D001812:Blood-Brain Barrier; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: D016229:Amyloid beta-Peptides; D001583:Benzoxazoles; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals
keywords: Alzheimer′s Disease; Fluorine-18; Molecular imaging; β-Amyloid aggregation