@article{e8f18828e4b64bf9bbe9f710be7f26cb,
title = "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",
abstract = "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.",
keywords = "Animals, Brain, Carbon Radioisotopes, Indoles, Ligands, Phenols, Positron-Emission Tomography, Receptors, Serotonin, Sulfonamides, Swine",
author = "Herth, {Matthias M} and {Lykke Andersen}, Valdemar and Hansen, {Hanne D} and Nikolas Stroth and Bal{\'a}zs Volk and Szabolcs Lehel and Agnete Dyssegaard and Anders Ettrup and Per Svenningsson and Knudsen, {Gitte M} and {Langgaard Kristensen}, Jesper",
year = "2015",
month = apr,
day = "23",
doi = "10.1021/acs.jmedchem.5b00095",
language = "English",
volume = "58",
pages = "3631--6",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "8",
}