Radiosynthesis and in vivo evaluation of novel radioligands for PET imaging of cerebral 5-HT7 receptors

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Hanne D Hansen, Matthias M Herth, Anders Ettrup, Valdemar L Andersen, Szabolcs Lehel, Agnete Dyssegaard, Jesper Langgaard Kristensen, Gitte M Knudsen

The serotonin (5-hydroxytryptamine [5-ΗΤ]) 7 receptor (5-HT7R) is the most recently discovered 5-HT receptor, and its physiologic and possible pathophysiologic roles are not fully elucidated. So far, no suitable 5-HT7R PET radioligand is available, thus limiting the investigation of this receptor in the living brain. Here, we present the radiosynthesis and in vivo evaluation of Cimbi-712 (3-{4-[4-(4-methylphenyl)piperazine-1-yl]butyl}p-1,3-dihydro-2H-indol-2-one) and Cimbi-717 (3-{4-[4-(3-methoxyphenyl)piperazine-1-yl]butyl}-1,3-dihydro-2H-indol-2-one) as selective 5-HT7R PET radioligands in the pig brain. The 5-HT7R distribution in the postmortem pig brain is also assessed.
Original languageEnglish
JournalJournal of Nuclear Medicine
Volume55
Issue number4
Pages (from-to)640-646
ISSN0161-5505
DOIs
Publication statusPublished - 24 Feb 2014

ID: 103038632