In this study, we proposed the design, synthesis of a new compound 2-(4-((1-phenyl-1H-pyrazol-4-yl)methyl)piperazin-1-yl)ethan-1-ol (LQFM032), 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, LQFM032 decreased latency and increased duration of sleep. In the open-field test, LQFM032 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 LQFM032 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 LQFM032 did not alter mnemonic activity. Moreover, the anxiolytic-like activity of LQFM032 was antagonized by mecamylamine. In summary, LQFM032 showed benzodiazepine and nicotinic pathways mediated anxiolytic-like activity without altering the mnemonic activity.
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http://dx.doi.org/10.1111/cbdd.12961 | DOI Listing |
Behav Brain Res
January 2025
Programa de Pós-Graduação em Nutrição e Saúde (PPGNS), Universidade Estadual do Ceará, CEP 60.741-000, Fortaleza-CE; Laboratório de Bioprospecção de Produtos Naturais e Biotecnologia (LBPNB), Campus CECITEC, CEP 60.660-000, Tauá-CE, Brasil. Electronic address:
Pharmacotherapy in Alcohol Withdrawal Syndrome (AWS), which is a mental disorder, generally involves benzodiazepines due to their action via GABA, but their side effects, such as excessive sedation, mental confusion and risk of dependence, are considerable. It is important to investigate the anxiolytic potential of plants such as Caryocar coriaceum, due to the presence of secondary metabolic compounds, such as isoquercitrin, capable of promoting the reduction of anxiety during AWS. We evaluated the anxiolytic-like potential of ethanolic extracts from the leaves (EEPL) and pulp (EEPP) of C.
View Article and Find Full Text PDFFront Pharmacol
December 2024
Department of Pharmacy, International Institute of Science, Arts, and Technology (IISAT), Gujranwala, Pakistan.
Background: Cancer remains a predominant cause of death worldwide. The advent of effective chemotherapy has enormously decreased the mortality rate and increased the life expectancy of cancer patients. However, the adverse effects allied with chemotherapy contribute to the development of neurotoxicity, anxiety, and depression.
View Article and Find Full Text PDFSynapse
January 2025
Department of Biochemistry & Molecular Biology, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj, Bangladesh.
Sesamol (SES) and linalool (LIN) are aromatic compounds that have neuroprotective effects. The main purpose of this study is to evaluate the anxiolytic activity of LIN and SES co-treatment on Swiss albino mice and analyze its possible mechanism through in silico study. In this sense, the mice were given the gamma-aminobutyric acid type A receptors (GABA) agonist diazepam (DZP; 3 mg/kg, p.
View Article and Find Full Text PDFMolecules
December 2024
Department of Pharmacognosy and Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.
L. has been traditionally applied as a remedy for headaches, rheumatism, digestion, respiratory and neurological problems, and other medical conditions. However, the literature data on its effects on cognitive function are scarce.
View Article and Find Full Text PDFPharmacol Rep
February 2025
Department of Clinical Pharmacy, Faculty of Pharmacy, Medical College, Jagiellonian University, Medyczna 9, Kraków, 30-688, Poland.
Background: Research on new candidates for antidepressant/anxiolytic drugs from the long-chain arylpiperazines (LCAPs) group containing a 1,3-dimethylpurine-2,6-dione as a terminal amide fragment fits into the modern exploration trend. This study aimed to examine, for the first time in male Wistar rats, pharmacodynamic (antidepressant- and anxiolytic-like) and pharmacokinetic properties of 7-(5-(4-(3-chlorophenyl)piperazin-1-yl)pentyl)-1,3-dimethyl-3,7-dihydro-1 H-purine-2,6-dione hydrochloride (GR-14).
Methods: Antidepressant- and anxiolytic-like activities have been assessed in the forced swim test (FST) and Vogel conflict drinking test, respectively.
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