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 journal › Journal article › Research › peer-review
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 language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 58 |
Issue number | 8 |
Pages (from-to) | 3631–3636 |
Number of pages | 16 |
ISSN | 0022-2623 |
DOIs | |
Publication status | Published - 13 Apr 2015 |
ID: 135400850