- Radiosynthesis and Biological Evaluation of [18F]R91150, a Selective 5-HT2AReceptor Antagonist for PET-Imaging
-
Serotonergic 5-HT2A receptors in cortical and forebrain regions are an important substrate for the neuromodulatory actions of serotonin in the brain. They have been implicated in the etiology of many neuropsychiatric disorders and serve as a target for an
- Willmann, Michael,Hegger, Julian,Neumaier, Bernd,Ermert, Johannes
-
p. 738 - 744
(2021/05/04)
-
- Synthesis, labelling and first evaluation of [18F]R91150 as a serotonin 5-HT2A receptor antagonist for PET
-
In psychiatric disorders such as anxiety, depression and schizophrenia, 5-HT2A receptors play an important role. In order to investigate them in vivo there is an increasing interest in selective and high-affinity radioligands for receptor binding studies using positron emission tomography (PET). Since available radioligands have disadvantages, R91150, which is a selective and high-affinity ligand for 5-HT2A receptors, was labelled with fluorine-18. This was accomplished in six steps via 4-[ 18F]fluorophenol and 1-(3-bromopropoxy)-4-[18F] fluorobenzene within 190 min starting from no-carrier-added [ 18F]fluoride. The overall radiochemical yield was 3.8±2% and the specific activity was at least 335 GBq/μmol at the end of the synthesis. First ex vivo studies in mice proved the uptake of [18F]R91150 in the brain. Radiometabolite studies revealed no radiometabolites in the brain, whereas in the plasma at least two could be detected 30 min p.i. Further preclinical studies are encouraged to evaluate the potential of this new 5-HT2A ligand as a radiotracer for PET. Copyright
- Muehlhausen, Ute,Ermert, Johannes,Coenen, Heinz H.
-
experimental part
p. 13 - 22
(2009/04/18)
-