| Literature DB >> 31586817 |
Martyna Z Wróbel1, Andrzej Chodkowski2, Franciszek Herold2, Monika Marciniak2, Maciej Dawidowski2, Agata Siwek3, Gabriela Starowicz3, Katarzyna Stachowicz4, Bernadeta Szewczyk4, Gabriel Nowak5, Mariusz Belka6, Tomasz Bączek6, Grzegorz Satała7, Andrzej J Bojarski7, Jadwiga Turło2.
Abstract
A series of novel 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesised and evaluated for their 5-HT1A/D2/5-HT2A/5-HT6/5-HT7 receptor affinity and serotonin reuptake inhibition. Most of the evaluated compounds displayed high affinities for 5-HT1A receptors (e.g., 4cKi = 2.3 nM, 4lKi = 3.2 nM). The antidepressant activity of the selected compounds was screened in vivo using the forced swim test (FST). The results indicate that compound MW005 (agonist of the pre- and postsynaptic 5-HT1A receptor) exhibited promising affinities for the 5-HT1A/SERT/D2/5-HT6/5-HT7 receptors and showed an antidepressant-like activity in the FST model.Entities:
Keywords: 5-HT(1A) agonists; 5-HT(1A)/SERT dual activity; Antidepressants; D(2) receptor ligands; Multitarget directed ligand; Serotonin reuptake inhibitors
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Year: 2019 PMID： 31586817 DOI： 10.1016/j.ejmech.2019.111736
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514