Synthesis and In Vitro Evaluation of Oxindole Derivatives as Potential Radioligands for 5-HT7 Receptor Imaging with PET
Synthesis and In Vitro Evaluation of Oxindole Derivatives as Potential Radioligands for 5-HT7 Receptor Imaging with PET
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DOI：
10.1021/cn3001137
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发表时间：
2012-12-01
影响因子：
5
通讯作者：
Kristensen, Jesper
中科院分区：
文献类型：
--
作者：
Herth, Matthias M.;Volk, Balazs;Kristensen, Jesper
The most recently discovered serotonin (5-HT) receptor subtype, 5-HT7, is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT7 receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT7 receptor. To date, no appropriate 5-HT7 receptor PET ligand has been developed. Here, we modified known 5-HT7 selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT7 ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT7 receptor thalamic regions.
