1601462-39-8Relevant articles and documents
Polyfluorinated bis-styrylbenzenes as amyloid-β plaque binding ligands
Nabuurs, Rob J.A.,Kapoerchan, Varsha V.,Metaxas, Athanasios,De Jongh, Sanne,De Backer, Maaike,Welling, Mick M.,Jiskoot, Wim,Windhorst, Albert D.,Overkleeft, Hermen S.,Van Buchem, Mark A.,Overhand, Mark,Van Der Weerd, Louise
, p. 2469 - 2481 (2014/05/06)
Detection of cerebral β-amyloid (Aβ) 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 Aβ imaging agents. To further explore their potency as 19F MRI contrast agents we synthetized several novel fluorinated bis-styrylbenzenes and studied their fluorescent properties and amyloid-β binding characteristics. The compounds showed a high affinity for Aβ 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.
