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Novel spirohydantoin derivative as a potent multireceptor : active antipsychotic and antidepressant agent

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Novel spirohydantoin derivative as a potent multireceptor : active antipsychotic and antidepressant agent

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dc.contributor.author Czopek, Anna [SAP20002400] pl
dc.contributor.author Kołaczkowski, Marcin [SAP20002091] pl
dc.contributor.author Bucki, Adam [SAP20012664] pl
dc.contributor.author Byrtus, Hanna [SAP20000695] pl
dc.contributor.author Pawłowski, Maciej [SAP20000690] pl
dc.contributor.author Kazek, Grzegorz [SAP20008717] pl
dc.contributor.author Bojarski, Andrzej J. pl
dc.contributor.author Piaskowska, Agata [USOS79633] pl
dc.contributor.author Kalinowska-Tłuścik, Justyna [SAP12019196] pl
dc.contributor.author Partyka, Anna [SAP20001958] pl
dc.contributor.author Wesołowska, Anna [SAP20002553] pl
dc.date.accessioned 2015-11-30T09:37:23Z
dc.date.available 2015-11-30T09:37:23Z
dc.date.issued 2015 pl
dc.identifier.issn 0968-0896 pl
dc.identifier.uri http://ruj.uj.edu.pl/xmlui/handle/item/17275
dc.language eng pl
dc.title Novel spirohydantoin derivative as a potent multireceptor : active antipsychotic and antidepressant agent pl
dc.type JournalArticle pl
dc.description.physical 3436-3447 pl
dc.abstract.en A series of novel spirohydantoin derivatives with arylpiperazinylbutyl moiety were synthesized and evaluated for serotonin 5-HT1A, 5-HT2A, 5-HT7 and dopamine D2 receptors. Based on these data, four compounds were selected for further binding affinity assays on dopamine D1, D3, D4, and 5-HT2C, 5-HT6 as well as adrenergic α1 and α2C receptors, which are involved in various CNS diseases such as schizophrenia, anxiety and/or depression. The compound 14, 1-{4-[4-(2-metoxyphe-nyl)piperazin-1-yl]butyl}-3′,4′-dihydro-2H,2′H,5H-spiro[imidazolidine-4,1′-naphthalene]-2,5-dione, with the most promising functional profile, mixed 5-HT2A/D2 antagonist and 5-HT1A partial agonist, was selected. In the mouse d-amphetamine-induced locomotor hyperactivity model, compound 14 produced antipsychotic-like activity, which is devoid of cataleptogenic effects and in the forced swim test in mice, it showed a significant antidepressant-like effect unlike the reference drug aripiprazole. pl
dc.subject.en antidepressant activity pl
dc.subject.en antipsychotic activity pl
dc.subject.en imidazolidine-2,4-dione spirohydantoins pl
dc.subject.en D2/5-HT2A antagonist pl
dc.subject.en 5-HT1A partial agonist pl
dc.description.volume 23 pl
dc.description.number 13 pl
dc.identifier.doi 10.1016/j.bmc.2015.04.026 pl
dc.identifier.eissn 1464-3391 pl
dc.title.journal Bioorganic & Medicinal Chemistry pl
dc.language.container eng pl
dc.affiliation Wydział Chemii : Zakład Krystalochemii i Krystalofizyki pl
dc.affiliation Wydział Farmaceutyczny : Zakład Farmacji Klinicznej pl
dc.affiliation Wydział Farmaceutyczny : Zakład Wstępnych Badań Farmakologicznych pl
dc.affiliation Wydział Farmaceutyczny : Zakład Chemii Leków pl
dc.subtype Article pl
dc.rights.original bez licencji pl
dc.cm.id 73077
.pointsMNiSW [2015 A]: 30


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