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| Hauptseite > Publikationsdatenbank > Synthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET > print |
| Hauptseite > Publikationsdatenbank > Synthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET > print |
| 001 | 1691 | ||
| 005 | 20180208193618.0 | ||
| 024 | 7 | _ | |2 DOI |a 10.1002/jlcr.1563 |
| 024 | 7 | _ | |2 WOS |a WOS:000263985000002 |
| 024 | 7 | _ | |2 ISSN |a 0362-4803 |
| 037 | _ | _ | |a PreJuSER-1691 |
| 041 | _ | _ | |a eng |
| 082 | _ | _ | |a 540 |
| 084 | _ | _ | |2 WoS |a Biochemical Research Methods |
| 084 | _ | _ | |2 WoS |a Chemistry, Medicinal |
| 084 | _ | _ | |2 WoS |a Chemistry, Analytical |
| 084 | _ | _ | |2 WoS |a Pharmacology & Pharmacy |
| 100 | 1 | _ | |0 P:(DE-Juel1)VDB73460 |a Mühlhausen, U. |b 0 |u FZJ |
| 245 | _ | _ | |a Synthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET |
| 260 | _ | _ | |a New York, NY [u.a.] |b Wiley |c 2008 |
| 300 | _ | _ | |a 6 - 12 |
| 336 | 7 | _ | |a Journal Article |0 PUB:(DE-HGF)16 |2 PUB:(DE-HGF) |
| 336 | 7 | _ | |a Output Types/Journal article |2 DataCite |
| 336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
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| 336 | 7 | _ | |a article |2 DRIVER |
| 440 | _ | 0 | |0 3464 |a Journal of Labelled Compounds and Radiopharmaceuticals |v 52 |x 0362-4803 |y 1 |
| 500 | _ | _ | |a Record converted from VDB: 12.11.2012 |
| 520 | _ | _ | |a In 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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| 653 | 2 | 0 | |2 Author |a radiofluorination |
| 653 | 2 | 0 | |2 Author |a 1-(2-bromoethyl)-4-[F-18]fluorobenzene |
| 653 | 2 | 0 | |2 Author |a (+/-)-[F-18]MDL 100907 |
| 653 | 2 | 0 | |2 Author |a 5-HT2A antagonist |
| 653 | 2 | 0 | |2 Author |a PET |
| 700 | 1 | _ | |0 P:(DE-Juel1)VDB6242 |a Ermert, J. |b 1 |u FZJ |
| 700 | 1 | _ | |0 P:(DE-Juel1)VDB68284 |a Herth, M.M. |b 2 |u FZJ |
| 700 | 1 | _ | |0 P:(DE-Juel1)131816 |a Coenen, H. H. |b 3 |u FZJ |
| 773 | _ | _ | |0 PERI:(DE-600)1491841-9 |a 10.1002/jlcr.1563 |g Vol. 52, p. 6 - 12 |p 6 - 12 |q 52<6 - 12 |t Journal of labelled compounds and radiopharmaceuticals |v 52 |x 0362-4803 |y 2008 |
| 856 | 7 | _ | |u http://dx.doi.org/10.1002/jlcr.1563 |
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