Title: Synthesis of [F-18]FA-4 and [C-11]pipzA-4 as radioligands for the high affinity choline uptake system
Authors: Gilissen, C ×
Bormans, Guy
de Groot, Tjibbe
Verbruggen, Alfons #
Issue Date: Dec-1999
Publisher: John wiley & sons ltd
Series Title: Journal of labelled compounds & radiopharmaceuticals vol:42 issue:13 pages:1289-1300
Abstract: We have prepared two radiolabelled analogues of hemicholinium-3 (HC-3) as potential in vivo tracers of the sodium dependent high affinity choline uptake (SDHAChU) system. Thus, 4-[1-hydroxy-2-(4-[F-18] fluoromethylpiperidinyl)ethyl]-4'-[1-hydroxy-2-(4-methylpiperidinyl)ethyl] ([F-18]FA-4) and 4-[1-hydroxy-2-(4-[ C-11] methylpiperazinyl)ethyl]-4'-[1-hydroxy-2-(4-methylpiperidinyl)]biphenyl ([C-11]pipzA-4) have been synthesized. [F-18]FA-4 was prepared by reaction of 4-[F-18] fluoromethylpiperidine with 4-(alpha-bromoacetyl)-4'-(4-methylpiperidinyl acetyl)biphenyl followed by reduction of the keto groups to alcohols with: NaBH4. The total synthesis time was 300 minutes and [18F]FA-4 was Obtained with a specific activity of 5.6 GBq/mu mol (EOS) and an overall decay corrected radiochemical yield of 3.1+/-0.6%. [C-11]pipzA-4 was prepared by reaction of [C-11]methyl triflate with 4-[1 -hydroxy-2-piperazinyl)ethyl]-4'-[1-hydroxy-2-(4-methylpiperidinyl)ethyl]- biphenyl. The total synthesis time was 25 minutes and [C-11]pipzA-4 was obtained with:a specific activity of 13.7 GBq/mu mol (EOS) and an overall decay corrected radiochemical yield of 19.5+/-2.2%.
ISSN: 0362-4803
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmaceutical Research
Nuclear Medicine & Molecular Imaging
× corresponding author
# (joint) last author

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