Tert-butyl 4-((1-phenyl-1H-pyrazol-4-yl) methyl) piperazine-1-carboxylate (LQFM104)– New piperazine derivative with antianxiety and antidepressant-like effects: Putative role of serotonergic system
| Autor: | Boniek G. Vaz, Germán Sanz, Adriane Ferreira de Brito, Luciano M. Lião, Ianca Gontijo Cavalcante Santana, Carina Sofia Cardoso, Daiany Priscilla Bueno da Silva, Danillo Ramos de Oliveira, Fábio Fagundes da Rocha, Elson Alves Costa, Pablinny Moreira Galdino, Flávio Silva de Carvalho, Dayane Moreira da Silva, Lorrane Kelle da Silva Moreira, Ricardo Menegatti |
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| Rok vydání: | 2018 |
| Předmět: |
Male
Serotonin Elevated plus maze medicine.drug_class Serotonin 5-HT1 Receptor Antagonists Pharmacology Serotonergic Anxiolytic Piperazines Open field Buspirone Mice 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine medicine Animals Maze Learning Piperazine Dose-Response Relationship Drug Antagonist Trazodone General Medicine Antidepressive Agents 030227 psychiatry Anti-Anxiety Agents Hindlimb Suspension chemistry Receptor Serotonin 5-HT1A Serotonin Antagonists Locomotion 030217 neurology & neurosurgery Serotonergic Neurons medicine.drug |
| Zdroj: | Biomedicine & Pharmacotherapy. 103:546-552 |
| ISSN: | 0753-3322 |
| DOI: | 10.1016/j.biopha.2018.04.077 |
| Popis: | The piperazine derivatives correspond to an extensive chemical class of compounds with numerous neuropharmacological activities, including antidepressant (e.g., nefazodone, trazodone) and anxiolytic (e.g., buspirone) properties. Therefore, aiming to identify a new antidepressant and antianxiety lead-compound, our group designed, synthesized, and investigated the effects of a new piperazine compound, namely, LQFM104, on the behavior of mice. Male albino Swiss mice were treated with LQFM104 prior to predictive behavioral tests as open field (OFT), elevated plus maze (EPM), forced swimming (FST), and tail suspension tests (TST). The participation of the serotonergic system was evaluated by pretreatment with a 5-HT1A antagonist receptor (WAY100635) and serotonin (5-HT) synthesis inhibitor (p-chlorphenylalanine, pCPA) before oral administration of LQFM104 and behavioral tests. The treatment with LQFM104 did not interfere with locomotor activity but revealed suggestive data of anxiolytic-like effects by the increase in the time spent in the center of the OFT. This activity was confirmed by the results obtained in the EPM, and it was abolished after pretreatment with WAY100635 and pCPA. The immobility time decreased in both the FST and TST. The antidepressant-like activity was completely abolished after WAY100635 pretreatment. Altogether, these data revealed that LQFM104 possesses anxiolytic and antidepressant-like properties in behavioral tests on mice, and these activities are possibly mediated, directly and/or indirectly, by serotonergic pathways. |
| Databáze: | OpenAIRE |
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