Title: Synthesis of carbon-11- and fluorine-18-labeled 1-methyl-4-piperidyl-4'-fluorobenzoate and their biodistribution in mice
Authors: Bormans, Guy ×
Sherman, P
Snyder, S E
Kilbourn, M R #
Issue Date: May-1996
Publisher: Pergamon Press
Series Title: International Journal of Radiation Applications and Instrumentation B, Nuclear Medicine and Biology vol:23 issue:4 pages:513-7
Abstract: Carbon-11- and fluorine-18-labeled forms of 1-methyl-4-piperidyl-4'-fluorobenzoate were prepared as potential in vivo substrates for brain acetylcholinesterase. The 1-methyl-4-piperidyl-4'-[18F]fluorobenzoate was prepared by aromatic nucleophilic substitution using the nitro precursor and no-carrier added [18F]fluoride ion. The 1-[11C]methyl-4-piperidyl-4'-fluorobenzoate was synthesized by N-[11C]methylation of the appropriate nor-methyl precursor. Biodistribution studies in mice showed high brain uptake of these radiotracers followed by a fast washout with no significant retention of radioactivity in areas of high acetylcholinesterase enzymatic activity. This is contrasted with 1-[11C]methyl-4-piperidylacetate, which is rapidly trapped in brain tissues through hydrolysis by AChE. Further in vivo and in vitro studies demonstrated that 1-methyl-4-piperidyl-4'-fluorobenzoate was not a substrate for AChE, and thus not suitable as an in vivo radiotracer for studying this enzyme in the brain.
ISSN: 0883-2897
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmaceutical Research
× corresponding author
# (joint) last author

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