Structure-activity relationship of three new piperazine derivates with anxiolytic-like and antidepressant-like effects

Autor: Ianca Gontijo Cavalcante Santana, Lorena de Souza Almeida, Lorrane Kelle da Silva Moreira, Flávio Silva de Carvalho, Ricardo Menegatti, André Luis Batista da Rocha, Thais Aline Mazurok, Boniek Gontijo Vaz, Luciano Morais Lião, Adriane Ferreira de Brito, James Oluwagbamigbe Fajemiroye, Elson Alves Costa, Pablinny Moreira Galdino de Carvalho
Rok vydání: 2022
Předmět:
Zdroj: Canadian journal of physiology and pharmacology. 100(6)
ISSN: 1205-7541
Popis: Anxiety and depression are common mental disorders affecting millions of people worldwide. Unsatisfactory clinical outcomes with the use of the available pharmacological interventions among some patients demand newer drugs with proven efficacy, safety, and tolerability profile. In this study, the LQFM211, LQFM213, and LQFM214 were designed from the piperazine scaffold and administered orally in mice. These mice were later evaluated in the open field, elevated plus maze, and forced swimming tests to assess the exploratory, anxiolytic, and antidepressant-like activities, respectively. The mechanism of action of these new derivatives was evaluated using flumazenil (benzodiazepine antagonist) and WAY100635 (5-HT1A receptor antagonist). Unlike LQFM214, the LQFM211 and LQFM213 elicited anxiolytic and antidepressant-like effects. The blockade of the effect of LQFM213 by WAY100635 suggests the involvement of the serotonergic pathway.
Databáze: OpenAIRE