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Anxiolytic‐like effect of 2‐(4‐((1‐phenyl‐1 H ‐pyrazol‐4‐yl)methyl)piperazin‐1‐yl)ethan‐1‐ol is mediated through the benzodiazepine and nicotinic pathways
Author(s) -
Brito Adriane F.,
Fajemiroye James O.,
Neri Hiasmin F. S.,
Silva Dayane M.,
Silva Daiany P. B.,
Sanz Germán,
Vaz Boniek G.,
Carvalho Flávio S.,
Ghedini Paulo C.,
Lião Luciano M.,
Menegatti Ricardo,
Costa Elson A.
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12961
Subject(s) - open field , anxiolytic , mecamylamine , pharmacology , benzodiazepine , flumazenil , elevated plus maze , chemistry , pentobarbital , diazepam , nicotinic agonist , psychology , medicine , biochemistry , psychiatry , receptor , anxiety
In this study, we proposed the design, synthesis of a new compound 2‐(4‐((1‐phenyl‐1 H ‐pyrazol‐4‐yl)methyl)piperazin‐1‐yl)ethan‐1‐ol ( LQFM 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, LQFM 032 decreased latency and increased duration of sleep. In the open‐field test, LQFM 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 LQFM 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 ( NAN ‐190). The LQFM 032 did not alter mnemonic activity. Moreover, the anxiolytic‐like activity of LQFM 032 was antagonized by mecamylamine. In summary, LQFM 032 showed benzodiazepine and nicotinic pathways mediated anxiolytic‐like activity without altering the mnemonic activity.