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Polyfluorinated bis-styrylbenzenes as amyloid-beta plaque binding ligands

Detection of cerebral beta-amyloid (Abeta) by targeted contrast agents remains of great interest to aid the in vivo diagnosis of Alzheimer's disease (AD). Bis-styrylbenzenes have been previously reported as potential Abeta imaging agents.

Nabuurs, R.J.; Kapoerchan, V.V.; Metaxas, A.; de Jongh, S.; de Backer, M.; Welling, M.M.; Jiskoot, W.; Windhorst, A.D.; Overkleeft, H.S.; van Buchem, M.A.; Overhand, M.; van der Weerd, L.
28 February 2014
Online publication (DOI)

To further explore their potency as 19F MRI contrast agents we synthetized several novel fluorinated bis-styrylbenzenes and studied their fluorescent properties and amyloid-beta binding characteristics. The compounds showed a high affinity for Abeta plaques on murine and human brain sections. Interestingly, competitive binding experiments demonstrated that they bound to a different binding site than chrysamine G. Despite their high logP values, many bis-styrylbenzenes were able to enter the brain and label murine amyloid in vivo. Unfortunately initial post-mortem 19F NMR studies showed that these compounds as yet do not warrant further MRI studies due to the reduction of the 19F signal in the environment of the brain.

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