Title: Synthesis and Evaluation of F-18-Labeled 2-Phenylbenzothiazoles as Positron Emission Tomography Imaging Agents for Amyloid Plaques in Alzheimer's Disease
Authors: Serdons, Kim ×
Terwinghe, Christelle
Vermaelen, Peter
Van Laere, Koen
Kung, Hank
Mortelmans, Luc
Bormans, Guy
Verbruggen, Alfons #
Issue Date: Mar-2009
Publisher: Amer chemical soc
Series Title: Journal of Medicinal Chemistry vol:52 issue:5 pages:1428-1437
Abstract: Imaging agents targeting amyloid beta(A beta) may be useful for early diagnosis and follow-up of treatment of patients with Alzheimer's disease (AD). Three of five tested 2-(4'-fluorophenyl)-1,3-benzothiazoles displayed high binding affinities for A beta plaques in AD human brain homogenates (K-i between 2.2 and 22.5 nM). They all contained the F-18-label directly attached to the aromatic ring and were synthesized starting from the nitro precursor. Determination of the partition coefficient, biodistribution studies in normal mice, and in vivo mu PET studies in normal rats showed that their initial brain uptake was high and brain washout was fast. The most promising compound [F-18]5, or 6- methyl-2-(4'-[F-18]fluorophenyl)-1,3-benzothiazole, seemed to be metabolically stable in the brain, and its plasma radiometabolites, which do not cross the blood-brain barrier, were determined. The preliminary results strongly suggest that this new fluorinated compound is a promising candidate as an A beta plaque imaging agent for the study of patients with AD.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Nuclear Medicine & Molecular Imaging
× corresponding author
# (joint) last author

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