Synthesis and In Vitro Evaluation of Oxindole Derivatives as Potential Radioligands for 5-HT7 Receptor Imaging with PET

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• 作者：Matthias M. Herth ; Bal谩zs Volk ; Katalin Pallagi ; Lasse Kofoed Bech ; Ferenc A. Antoni ; Gitte M. Knudsen ; Jesper L. Kristensen
• 刊名：ACS Chemical Neuroscience
• 出版年：2012
• 出版时间：December 19, 2012
• 年：2012
• 卷：3
• 期：12
• 页码：1002-1007
• 全文大小：229K
• 年卷期：v.3,no.12(December 19, 2012)
• ISSN：1948-7193

文摘

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 in thalamic regions.

Keywords:

cs.org/action/doSearch?action=search&searchText=Oxindole&qsSearchArea=searchText">Oxindole; cs.org/action/doSearch?action=search&searchText=5%5C-HT7+receptor+distribution&qsSearchArea=searchText">5-HT₇ receptor distribution; cs.org/action/doSearch?action=search&searchText=PET&qsSearchArea=searchText">PET