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Synthesis, labelling and first evaluation of [18F]R91150 as a serotonin 5-HT2A receptor antagonist for PET

✍ Scribed by Ute Mühlhausen; Johannes Ermert; Heinz H. Coenen

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
226 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

In psychiatric disorders such as anxiety, depression and schizophrenia, 5‐HT~2A~ receptors play an important role. In order to investigate them in vivo there is an increasing interest in selective and high‐affinity radioligands for receptor binding studies using positron emission tomography (PET). Since available radioligands have disadvantages, R91150, which is a selective and high‐affinity ligand for 5‐HT~2A~ receptors, was labelled with fluorine‐18. This was accomplished in six steps via 4‐[^18^F]fluorophenol and 1‐(3‐bromopropoxy)‐4‐[^18^F]fluorobenzene within 190 min starting from no‐carrier‐added [^18^F]fluoride. The overall radiochemical yield was 3.8±2% and the specific activity was at least 335 GBq/µmol at the end of the synthesis. First ex vivo studies in mice proved the uptake of [^18^F]R91150 in the brain. Radiometabolite studies revealed no radiometabolites in the brain, whereas in the plasma at least two could be detected 30 min p.i. Further preclinical studies are encouraged to evaluate the potential of this new 5‐HT~2A~ ligand as a radiotracer for PET. Copyright © 2008 John Wiley & Sons, Ltd.

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