Life sciences · 2012
Central pharmacological activity of a new piperazine derivative: 4-(1-phenyl-1h-pyrazol-4-ylmethyl)-piperazine-1-carboxylic acid ethyl ester.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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de Brito Adriane Ferreira, Martins José Luís Rodrigues, Fajemiroye James Oluwagbamigbe, Galdino Pablinny Moreira, De Lima Thereza Christina Monteiro, Menegatti Ricardo, Costa Elson Alves
Аннотация
AIMS: Our study focuses on the design and synthesis of a new piperazinic derivate, 4-(1-phenyl-1h-Pyrazol-4-Ylmethyl)-Piperazine-1-Carboxylic Acid Ethyl ester (LQFM008), and evaluation of its anxiolytic-like profile in Swiss mice.
MAIN METHODS: LQFM008 was evaluated in a screening test of the central nervous system including the rota-rod, sodium pentobarbital-induced sleep, open field, elevated plus maze and light-dark box tests.
KEY FINDINGS: LQFM008 induced convulsions at the dose of 1.1 mmol/kg (i.p., s.c. or p.o.). LQFM008 up to 400 μmol/kg had no effect in the rota rod test. In the open field test, LQFM008 increased the number of crossings and the time spent at the central area as well as the sleeping time in sodium pentobarbital-induced sleep. In the elevated plus maze and light-dark box tests, this compound showed an anxiolytic-like activity. This anxiolytic-like activity was antagonized by NAN-190 (5-HT(1A) antagonist) but not by flumazenil (benzodiazepine antagonist).
SIGNIFICANCE: The compound LQFM008 showed anxiolytic-like activity which may involve serotonergic pathway.
MAIN METHODS: LQFM008 was evaluated in a screening test of the central nervous system including the rota-rod, sodium pentobarbital-induced sleep, open field, elevated plus maze and light-dark box tests.
KEY FINDINGS: LQFM008 induced convulsions at the dose of 1.1 mmol/kg (i.p., s.c. or p.o.). LQFM008 up to 400 μmol/kg had no effect in the rota rod test. In the open field test, LQFM008 increased the number of crossings and the time spent at the central area as well as the sleeping time in sodium pentobarbital-induced sleep. In the elevated plus maze and light-dark box tests, this compound showed an anxiolytic-like activity. This anxiolytic-like activity was antagonized by NAN-190 (5-HT(1A) antagonist) but not by flumazenil (benzodiazepine antagonist).
SIGNIFICANCE: The compound LQFM008 showed anxiolytic-like activity which may involve serotonergic pathway.