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Rigshospitalet - a part of Copenhagen University Hospital
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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

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  1. In Vivo Veritas: 18F-Radiolabeled Glycomimetics Allow Insights into the Pharmacological Fate of Galectin-3 Inhibitors

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  2. Tailoring cytotoxicity of antimicrobial peptidomimetics with high activity against multidrug-resistant Escherichia coli

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  1. The Modulatory Role of Serotonin on Human Impulsive Aggression

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  2. Hot and cold cognitive disturbances in antidepressant-free patients with major depressive disorder: a NeuroPharm study

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  3. Structural brain abnormalities associated with cognitive impairments in bipolar disorder

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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)3631-6
Number of pages6
ISSN0022-2623
DOIs
Publication statusPublished - 23 Apr 2015

    Research areas

  • Animals, Brain, Carbon Radioisotopes, Indoles, Ligands, Phenols, Positron-Emission Tomography, Receptors, Serotonin, Sulfonamides, Swine

ID: 45588916