Employees – University of Copenhagen

Evaluation of 3-Ethyl-3-(phenylpiperazinylbutyl)oxindoles as PET Ligands for the Serotonin 5-HT7 Receptor: Synthesis, Pharmacology, Radiolabeling, and in Vivo Brain Imaging in Pigs

Research output: Contribution to journalJournal articleResearchpeer-review

Matthias M Herth, Valdemar L Andersen, Hanne D Hansen, Nikolas Stroth, Balázs Volk, Szabolcs Lehel, Agnete Dyssegaard, Anders Ettrup, Per Svenningsson, Gitte M Knudsen, Jesper Langgaard Kristensen

We have investigated several oxindole derivatives in the pursuit of a 5-HT7 receptor PET ligand. Herein the synthesis, chiral separation, and pharmacological profiling of two possible PET candidates toward a wide selection of CNS-targets are detailed. Subsequent (11)C-labeling and in vivo evaluation in Danish landrace pigs showed that both ligands displayed high brain uptake. However, neither of the radioligands could be displaced by the 5-HT7 receptor selective inverse agonist SB-269970.

Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume58
Issue number8
Pages (from-to)3631–3636
Number of pages16
ISSN0022-2623
DOIs
Publication statusPublished - 13 Apr 2015

ID: 135400850