Radiosynthesis and in vivo Evaluation of a ¹⁸F-Labelled Styryl-Benzoxazole Derivative for ß-Amyloid Targeting

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.