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000001691 1001_ $$0P:(DE-Juel1)VDB73460$$aMühlhausen, U.$$b0$$uFZJ
000001691 245__ $$aSynthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET
000001691 260__ $$aNew York, NY [u.a.]$$bWiley$$c2008
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000001691 520__ $$aIn some psychiatric disorders 5-HT2A receptors play an important role. In order to investigate those in vivo there is an increasing interest in obtaining a metabolically stable, subtype selective and high affinity radioligand for receptor binding studies using positron emission tomography (PET). Combining the excellent in vivo properties of [C-11]MDL 100907 for PET imaging of 5-HT2A receptors and the more suitable half-life of fluorine-18, MDL 100907 was radiofluorinated in four steps using 1-(2-bromoethyl)-4-[F-18]fluorobenzene as a secondary labelling precursor. The complex reaction required an overall reaction time of 140 min and [+/-)-[F-18]MDL 100907 was obtained with a specific activity of at least 30 GBq/mu mol (EOS) and an overall radiochemical yield of 1-2%. In order to verify its binding to 5-HT2A receptors, in vitro rat brain autoradiography was conducted showing the typical distribution of 5-HT2A receptors and a very low non-specific binding of about 6% in frontal cortex, using ketanserin or spiperone for blocking. Thus, [F-18]MDL 100907 appears to be a promising new 5-HT2A PET ligand.
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000001691 65320 $$2Author$$a1-(2-bromoethyl)-4-[F-18]fluorobenzene
000001691 65320 $$2Author$$a(+/-)-[F-18]MDL 100907
000001691 65320 $$2Author$$a5-HT2A antagonist
000001691 65320 $$2Author$$aPET
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000001691 7001_ $$0P:(DE-Juel1)VDB6242$$aErmert, J.$$b1$$uFZJ
000001691 7001_ $$0P:(DE-Juel1)VDB68284$$aHerth, M.M.$$b2$$uFZJ
000001691 7001_ $$0P:(DE-Juel1)131816$$aCoenen, H. H.$$b3$$uFZJ
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