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Synthesis, radiofluorination and first evaluation of (±)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET

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

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

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✦ Synopsis

In some psychiatric disorders 5-HT 2A receptors play an important role. In order to investigate those in vivo there is an increasing interest in obtaining a metabolically stable, subtype selective and high affinity radioligand for receptor binding studies using positron emission tomography (PET). Combining the excellent in vivo properties of [ 11 C]MDL 100907 for PET imaging of 5-HT 2A receptors and the more suitable half-life of fluorine-18, MDL 100907 was radiofluorinated in four steps using 1-(2-bromoethyl)-4-[ 18 F]fluorobenzene as a secondary labelling precursor. The complex reaction required an overall reaction time of 140 min and (7)-[ 18 F]MDL 100907 was obtained with a specific activity of at least 30 GBq/mmol (EOS) and an overall radiochemical yield of 1-2%. In order to verify its binding to 5-HT 2A receptors, in vitro rat brain autoradiography was conducted showing the typical distribution of 5-HT 2A receptors and a very low non-specific binding of about 6% in frontal cortex, using ketanserin or spiperone for blocking. Thus, [ 18 F]MDL 100907 appears to be a promising new 5-HT 2A PET ligand.

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