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Experimental Genetics Group

Bolleke Abstract   Pijltje
11C-labelled PIB analogues as potential tracer agents for in vivo imaging of amyloid beta in Alzheimer's disease.

Eur J Med Chem. 2009 Apr;44(4):1415-26.

Serdons K1*, Verduyckt T1, Vanderghinste D1, Borghgraef P2, Cleynhens J1, Van Leuven F2, Kung H, Bormans G3, Verbruggen A1.

1Laboratory for Radiopharmacy, Faculty of Pharmaceutical Sciences, K.U.Leuven, Leuven, Belgium.
2Laboratory of Experimental Genetics and Transgenesis, K.U.Leuven, Leuven, Belgium.
3Department of Radiology, University of Pennsylvania, Philadelphia, USA.
*Corresponding author.

Pittsburgh Compound-B (PIB) is currently being evaluated clinically for in vivo visualization of amyloid plaques in patients with Alzheimer's disease (AD). We have synthesized three structural isomers of 6-hydroxy-2-(4'-aminophenyl)-1,3-benzothiazole, performed radiolabelling with carbon-11 and investigated their in vivo and in vitro properties. Specific binding to amyloid plaques was demonstrated in vitro using post-mortem brain homogenates of AD patients, transgenic AD mice brain sections and post-mortem human AD brain sections. In normal mice, initial brain uptake (at 2 min p.i.) was high and was followed by a fast wash-out. The three structural analogues have a high potential as tracer agents for in vivo visualization of amyloid plaques in AD patients.

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