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Synthesis of [18F]fluoroethoxy-benzovesamicol, a radiotracer for cholinergic neurons

✍ Scribed by G. Keith Mulholland; Yong-Woon Jung; Donald M. Wieland; Michael R. Kilbourn; David E. Kuhl

Book ID
102901480
Publisher
John Wiley and Sons
Year
1993
Tongue
French
Weight
522 KB
Volume
33
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Full experimental details are given for the preparation of [^18^F]fluoroethoxy‐benzovesamicol, (−)‐(2R, 3R)‐trans‐2‐hydroxy‐3‐(4‐phenylpiperidino)‐5‐(2‐[^18^F]fluoroethoxy)‐1,2,3,4‐tetralin, a new fluorine‐18 labeled cholinergic neuron mapping agent for use in positron emission tomography (PET). This radiotracer was made by nucleophilic radiofluorination of tosyloxyethoxy‐benzovesamicol, followed by reverse phase HPLC purification, in decay corrected radiochemical yield exceeding 60%.

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[18F]fluoroethoxy-benzovesamicol, a PET
[18F]fluoroethoxy-benzovesamicol, a PET radiotracer for the vesicular acetylcholine transporter and cholinergic synapses
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Loss of cholinergic transmission in the cortex and hippocampus is a characteristic feature of Alzheimer's disease, and visualization of functional cholinergic synapses in the brain with PET could be a useful method for studying this degenerative condition in living humans. We investigated [ 18 F]flu