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  • 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.
    Author: Herth MM, Andersen VL, Hansen HD, Stroth N, Volk B, Lehel S, Dyssegaard A, Ettrup A, Svenningsson P, Knudsen GM, Kristensen JL.
    Journal: J Med Chem; 2015 Apr 23; 58(8):3631-6. PubMed ID: 25825999.
    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.
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