This title appears in the Scientific Report :
2008
Please use the identifier:
http://dx.doi.org/10.1002/jlcr.1563 in citations.
Synthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET
Synthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET
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). Com...
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Personal Name(s): | Mühlhausen, U. |
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Ermert, J. / Herth, M.M. / Coenen, H. H. | |
Contributing Institute: |
Nuklearchemie; INB-4 |
Published in: | Journal of labelled compounds and radiopharmaceuticals, 52 (2008) S. 6 - 12 |
Imprint: |
New York, NY [u.a.]
Wiley
2008
|
Physical Description: |
6 - 12 |
DOI: |
10.1002/jlcr.1563 |
Document Type: |
Journal Article |
Research Program: |
Funktion und Dysfunktion des Nervensystems |
Series Title: |
Journal of Labelled Compounds and Radiopharmaceuticals
52 |
Subject (ZB): | |
Publikationsportal JuSER |
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. |