911381-81-2Relevant academic research and scientific papers
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
supporting information, 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.
18F-FESB: Synthesis and automated radiofluorination of a novel 18F-labeled pet tracer for β-amyloid plaques
Kumar, Piyush,Zheng, Weizhong,McQuarrie, Stephen A.,Jhamandas, Jack H.,Wiebe, Leonard I.
, p. 983 - 996 (2007/10/03)
1-(2′-[18F]-fluoroethoxy)-2,5-bis(4′-methoxystyryl) benzene (18F-FESB) was synthesized in ～76% radiochemical yield (specific activity > 58.6 GBq or 1.58 Ci/μmol) in an Advanced Cyclotron Systems' automated synthesis unit by nucleophi
