Title: Technetium-99m labelled integrated tropane-BAT as a potential dopamine transporter tracer
Authors: Cleynhens, Bernard ×
de Groot, Tjibbe J
Vanbilloen, Hubert P
Kieffer, Davy
Mortelmans, Luc
Bormans, Guy
Verbruggen, Alfons #
Issue Date: Feb-2005
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:13 issue:4 pages:1053-1058
Abstract: To reduce the molecular weight of 99mTc-labelled tropanes with the aim to enhance the passage over the blood-brain barrier, a so-called integrated tropane-BAT construct was developed. For this purpose a mercaptoethyl substituent was attached to the amine nitrogen atom of a nortropane precursor and the methyl carboxylate in 2beta-position was converted to a 2-mercaptoethylaminomethylene substituent. This integrated tropane-BAT construct could be labelled efficiently (85-90%) with technetium-99m. Results of LC-MS analysis of the tracer agent support the assumed structure. Biodistribution studies in normal rats (n=3) showed a slightly higher brain uptake for the new tracer agents as compared to 99mTc-TRODAT-1. These results indicate that further biological evaluation of the integrated 99mTc-tropane-BAT is warranted.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmacy
Nuclear Medicine & Molecular Imaging
× corresponding author
# (joint) last author

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