Brito, Adriane F.;
Fajemiroye, James O.;
Neri, Hiasmin F. S.;
Silva, Dayane M.;
Silva, Daiany P. B.;
Sanz, Germán;
Vaz, Boniek G.;
de Carvalho, Flávio S.;
Ghedini, Paulo C.;
Lião, Luciano M.;
Menegatti, Ricardo;
Costa, Elson A.
Anxiolytic‐like effect of 2‐(4‐((1‐phenyl‐1H‐pyrazol‐4‐yl)methyl)piperazin‐1‐yl)ethan‐1‐ol is mediated through the benzodiazepine and nicotinic pathways
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Media type:
E-Article
Title:
Anxiolytic‐like effect of 2‐(4‐((1‐phenyl‐1H‐pyrazol‐4‐yl)methyl)piperazin‐1‐yl)ethan‐1‐ol is mediated through the benzodiazepine and nicotinic pathways
Contributor:
Brito, Adriane F.;
Fajemiroye, James O.;
Neri, Hiasmin F. S.;
Silva, Dayane M.;
Silva, Daiany P. B.;
Sanz, Germán;
Vaz, Boniek G.;
de Carvalho, Flávio S.;
Ghedini, Paulo C.;
Lião, Luciano M.;
Menegatti, Ricardo;
Costa, Elson A.
Description:
<jats:p>In this study, we proposed the design, synthesis of a new compound 2‐(4‐((1‐phenyl‐1<jats:italic>H</jats:italic>‐pyrazol‐4‐yl)methyl)piperazin‐1‐yl)ethan‐1‐ol (<jats:styled-content style="fixed-case">LQFM</jats:styled-content>032), and pharmacological evaluation of its anxiolytic‐like effect. This new compound was subjected to pharmacological screening referred to as Irwin test, prior to sodium pentobarbital‐induced sleep, open‐field and wire tests. The anxiolytic‐like effect of this compound was evaluated using elevated plus maze and light–dark box tests. In addition, the mnemonic activity was evaluated through step‐down test. In sodium pentobarbital‐induced sleep test, <jats:styled-content style="fixed-case">LQFM</jats:styled-content>032 decreased latency and increased duration of sleep. In the open‐field test, <jats:styled-content style="fixed-case">LQFM</jats:styled-content>032 altered behavioral parameter, that suggested anxiolytic‐like activity, as increased in crossings and time spent at the center of open field. In the plus maze test and light–dark box test, the <jats:styled-content style="fixed-case">LQFM</jats:styled-content>032 showed anxiolytic‐like activity, increased entries and time spent on open arms, and increased in number of transitions and time spent on light area, respectively. Those effects was antagonized by flumazenil but not with 1‐(2‐Methoxyphenyl)‐4‐(4‐phthalimidobutyl)piperazine (<jats:styled-content style="fixed-case">NAN</jats:styled-content>‐190). The <jats:styled-content style="fixed-case">LQFM</jats:styled-content>032 did not alter mnemonic activity. Moreover, the anxiolytic‐like activity of <jats:styled-content style="fixed-case">LQFM</jats:styled-content>032 was antagonized by mecamylamine. In summary, <jats:styled-content style="fixed-case">LQFM</jats:styled-content>032 showed benzodiazepine and nicotinic pathways mediated anxiolytic‐like activity without altering the mnemonic activity.</jats:p>