TY  - JOUR
AU  - Mühlhausen, U.
AU  - Ermert, J.
AU  - Herth, M.M.
AU  - Coenen, H. H.
TI  - Synthesis, radiofluorination and first evaluation of (+/-)-[18F]MDL 100907 as serotonin 5-HT2A receptor antagonist for PET
JO  - Journal of labelled compounds and radiopharmaceuticals
VL  - 52
SN  - 0362-4803
CY  - New York, NY [u.a.]
PB  - Wiley
M1  - PreJuSER-1691
SP  - 6 - 12
PY  - 2008
N1  - Record converted from VDB: 12.11.2012
AB  - 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.
KW  - J (WoSType)
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000263985000002
DO  - DOI:10.1002/jlcr.1563
UR  - https://juser.fz-juelich.de/record/1691
ER  -