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Radiosynthesis and in vivo study of [18F]1-(2-fluoroethyl)-4-[(4-cyanophenoxy)methyl]piperidine: a promising new sigma-1 receptor ligand

✍ Scribed by Jun Zhao; Raymond Chang; Patty Carambot; Rikki N. Waterhouse

Publisher
John Wiley and Sons
Year
2005
Tongue
French
Weight
124 KB
Volume
48
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The novel sigma‐1 receptor PET radiotracer [^18^F]1‐(2‐fluoroethyl)‐4‐[(4‐cyanophenoxy)methyl]piperidine ([^18^F]WLS1.002, [^18^F]‐2) was synthesized (n=6) by heating the corresponding N‐ethylmesylate precursor in an anhydrous acetonitrile solution containing [^18^F]fluoride, Kryptofix K~222~ and potassium carbonate for 15 min. Purification was accomplished by reverse‐phase HPLC methods, providing [^18^F]‐2 in 59±8% radiochemical yield (EOB), with specific activity of 2.89±0.80 Ci/µmol (EOS) and radiochemical purity of 98.3±2.1%. Rat biodistribution studies revealed relatively high uptake in many organs known to contain sigma‐1 receptors, including the lungs, kidney, heart, spleen, and brain. Good clearance from normal tissues was observed over time. Blocking studies (60 min) demonstrated high (>80%) specific binding of [^18^F]‐2 in the brain, with reduction also noted in other organs known to express these sites. Copyright © 2005 John Wiley & Sons, Ltd.

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