Involvement of the monoamine system in antidepressant-like properties of 4-(1-phenyl-1h-pyrazol-4-ylmethyl)-piperazine-1-carboxylic acid ethyl ester

Galdino, Pablinny Moreira; Oliveira, Danillo Ramos de; Florentino, Iziara Ferreira; Fajemiroye, James Oluwagbamigbe; Valadares, Marize Campos; Moura, Soraia Santana de; Rocha, Fábio Fagundes da; Lima, Thereza Christina Monteiro de; Costa, Élson Alves; Menegatti, Ricardo

doi:10.1016/j.lfs.2015.11.009

Cited by 13 publications

(7 citation statements)

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“…Therefore, this paper describes some of the central pharmacological activities of many drugs that are piperazine derivatives used as antipsychotic, antidepressant and anxiolytic drugs as well as other types of drugs that act on the central nervous system. Additionally, the research group of Laboratório de Farmacologia de Produtos Naturais e Sintéticos/UFG has studied the neuropharmacological activity of some piperazine derivatives (LQFM008, LQFM032 and LQFM180) and demonstrated that these compounds possess anxiolytic‐ and antidepressant‐like activity involving mainly the serotonergic pathway .…”

Section: Introductionmentioning

confidence: 99%

Piperazine derivatives with central pharmacological activity used as therapeutic tools

Brito

Moreira

Menegatti

et al. 2018

Fundamemntal Clinical Pharma

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Medicinal chemistry is a science applied to the search and discovery of new therapeutic agents for the treatment of various diseases. Therefore, promising structures have been identified; one of these structures is the piperazine moiety, a cyclic molecule containing two nitrogen atoms in positions 1 and 4 as well as four carbon atoms. Many piperazine derivatives have central pharmacological activity that mainly involves the activation of the monoamine pathway. Thus, piperazine derivatives have been the subject of research for many central therapeutic applications, including antipsychotic, antidepressant and anxiolytic applications. Benzylpiperazine is the prototype of piperazine derivatives; this substance is the main component of recreational drugs, partly due to its stimulant and euphoric effects. This paper describes some piperazine derivatives used therapeutically as antipsychotic (clozapine), antidepressant (vortioxetine) and anxiolytic (buspirone) drugs.

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Section: Introductionmentioning

confidence: 99%

Piperazine derivatives with central pharmacological activity used as therapeutic tools

Brito

Moreira

Menegatti

et al. 2018

Fundamemntal Clinical Pharma

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“…Gladino et al. reported 4‐(1‐phenyl‐1 H ‐pyrazol‐4‐ylmethyl)‐piperazine‐1‐carboxylic acid ethyl ester (PPMP, 52 ), having antidepressant activity via monoamine systems [101] . The results from TST and FST studies revealed that 52 (Figure 20) possesses potential antidepressant activity by serotonergic and catecholaminergic systems.…”

Section: Recent Advancements In Piperazine Derivatives As Antidepressantsmentioning

confidence: 99%

Piperazine, a Key Substructure for Antidepressants: Its Role in Developments and Structure‐Activity Relationships

et al. 2021

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Depression is the single largest contributor to global disability with a huge economic and social burden on the world. There are a number of antidepressant drugs on the market, but treatment‐resistant depression and relapse of depression in a large number of patients have increased problems for clinicians. One peculiarity observed in most of the marketed antidepressants is the presence of a piperazine substructure. Although piperazine is also used in the optimization of other pharmacological agents, it is almost extensively used for the development of novel antidepressants. One common understanding is that this is due to its favorable CNS pharmacokinetic profile; however, in the case of antidepressants, piperazine plays a much bigger role and is involved in specific binding conformations of these agents. Therefore, in this review, a critical analysis of the significance of the piperazine moiety in the development of antidepressants has been performed. An overview of current developments in the designing and synthesis of piperazine‐based antidepressants (2015 onwards) along with SAR studies is also provided. The various piperazine‐based therapeutic agents in early‐ or late‐phase human testing for depression are also discussed. The preclinical compounds discussed in this review will help researchers understand how piperazine actually influences the design and development of novel antidepressant compounds. The SAR studies discussed will provide crucial clues about the structural features and optimizations required to enhance the efficacy and potency of piperazine‐based antidepressants.

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“…5 The monoaminergic hypothesis, the depleted the level of serotonin, noradrenaline, and dopamine in the central nervous system which induces depression. 6 The hypothesis is unable to fully explain the depression complexity and delay in therapeutic effect of antidepressant drugs, other complementary theory such as neurotrophic hypothesis is developed, which postulates that low levels of neurotrophic factors mainly the brain derived neurotrophic factor (BDNF) is associated with depression. 6 Plant species plays a very important role for the development of medicines.…”

Section: Introductionmentioning

confidence: 99%

“…6 The hypothesis is unable to fully explain the depression complexity and delay in therapeutic effect of antidepressant drugs, other complementary theory such as neurotrophic hypothesis is developed, which postulates that low levels of neurotrophic factors mainly the brain derived neurotrophic factor (BDNF) is associated with depression. 6 Plant species plays a very important role for the development of medicines. Native peoples had good knowledge about the medicinal herbs.…”

Section: Introductionmentioning

confidence: 99%

Anti-depressant Activity of the Seeds of Zanthoxylum armatum on Swiss Albino Mice

Yadav

Poudel

Mehta

et al. 2022

Nep. J. Health Sci.

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Introduction: Depression disorder has significant potential morbidity and mortality, contributing to suicide, incidence and adverse outcomes of medical illness, disruption in interpersonal relationships, substance abuse, and lost work time. Objectives: The present study was designed to study the anti-depressant activity of the seeds extract of Zanthoxylum armatum using a forced swim test and tail suspension test on Swiss albino mice. The anti-depressant activity of the seeds of Zanthoxylum armatum was assessed using Chronic Unpredictable Mild-Stress (CUMS) induced depression in mice. Methods: The animals were treated with the methanolic extract of seeds of Zanthoxylum armatum orally at two doses of 100, 200mg/kg body weight for eight days after CUMS induced depression in mice. The results demonstrate that Methanolic extract of seeds of Zanthoxylum armatum has got anti-depressant potential. Results: The study showed that the extract of Zanthoxylum armatum had significant antidepressant activity. Microsoft Excel was used to calculate the mean ± SEM and one-way ANOVA followed by a turkey multiple comparison test was used to analyze the results. The seed extract presented significant antidepressant activity in mice (p<0.05). Conclusions: This study was conducted to explore the antidepressant activity of seeds extracts of plant Zanthoxylum armatum in CUMS induced mice.

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Involvement of the monoamine system in antidepressant-like properties of 4-(1-phenyl-1h-pyrazol-4-ylmethyl)-piperazine-1-carboxylic acid ethyl ester

Abstract: In conclusion, PPMP demonstrates antidepressant-like effect that involve both serotonergic and catecholaminergic systems without inhibition of MAO activity. PPMP administration increased the hippocampal levels of BDNF.

Cited by 13 publications

References 41 publications

Piperazine derivatives with central pharmacological activity used as therapeutic tools

Piperazine derivatives with central pharmacological activity used as therapeutic tools

Piperazine, a Key Substructure for Antidepressants: Its Role in Developments and Structure‐Activity Relationships

Anti-depressant Activity of the Seeds of Zanthoxylum armatum on Swiss Albino Mice

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