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Efficient synthesis of [11C]befloxatone, a selective radioligand for the in vivo imaging of MAO-A density using PET

✍ Scribed by F. Dollé; Y. Bramoullé; F. Hinnen; S. Demphel; P. George; M. Bottlaender

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
110 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Carbon‐11 labelled befloxatone ((5R)‐5‐(methoxymethyl)‐3‐[4‐[(3R)‐4,4,4‐trifluoro‐3‐hydroxybutoxy]phenyl]‐2‐oxazolidinone) is a reversible and selective monoamine oxidase‐A (MAO‐A) inhibitor and appears to be a new potent PET tracer for the in vivo imaging of MAO‐A density. In this paper, the radiosynthesis of befloxatone was investigated and orientated towards the preparation of multi milliCuries of radiotracer. Typically, using no‐carrier‐added [^11^C]phosgene, 150–300 mCi (5.55–11.10 GBq) of [^11^C]befloxatone was obtained within 20 min of radiosynthesis (including HPLC purification) with specific radioactivities ranging from 500 to 2000 mCi/µmol (18.5–74.0 GBq/µmol). The high efficiency of these radiosyntheses allows for multi‐injection protocols and kinetic approaches for absolute quantification of the tracer. Copyright © 2003 John Wiley & Sons, Ltd.

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