Effect of dialkyl- [2-(1-oxa-3,4,9-triaza-fluoren-2-yl-methoxy)ethyl] amines on biogenic amines: new potential antidepressants

2012 ◽  
Vol 90 (12) ◽  
pp. 1585-1590
Author(s):  
Akena Venkatesham ◽  
J. Venkateshwar Rao ◽  
K. Vijay Kumar ◽  
M. Sarangapani ◽  
Krishna Devarakonda
Keyword(s):  
Biogenic Amines ◽  
Forced Swim Test ◽  
Chronic Administration ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Control Group ◽  
Stress Model ◽  
Chronic Unpredictable Stress ◽  
The Brain

A thorough survey of the literature has revealed that indole derivatives have shown various central nervous system activities. This study aims to evaluate the antidepressant activity of the newly synthesized dialkyl- [2-(1-oxa-3,4,9-triaza-fluoren-2-yl-methoxy)ethyl] amines and their effect on biogenic amines. In this study, the synthesized compounds were assessed by in-vivo antidepressant models, by forced swim test and tail suspension test in mice and effect of synthesized compounds on biogenic amines in brain in a chronic unpredictable stress model. The test compounds have demonstrated significant (P < 0.05) reduced immobility duration in mice when compared with the control group animals. The reduced immobility displayed by mice indicates potential antidepressant activity. In this study, chronic unpredictable stress led to decreased monoamine levels in the cortex and hippocampus regions of the brain. With chronic administration of the investigated compounds there is an increased in monoamines in the brain, in the chronic unpredictable stress model. Decreased levels of monoamines induced by the chronic unpredictable stress induced model of depression, were normalized by treatment with the test compounds, which indicates potential antidepressant activity.

scholarly journals Synthesis and Evaluation of Antidepressant Activities of 5-Aryl-4,5-dihydrotetrazolo [1,5-a]thieno[2,3-e]pyridine Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (10) ◽  
pp. 1857 ◽  
Author(s):  
Shiben Wang ◽  
Hui Liu ◽  
Xuekun Wang ◽  
Kang Lei ◽  
Guangyong Li ◽  
...  
Keyword(s):  
Biological Activities ◽  
Forced Swim Test ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Homology Model ◽  
Docking Studies ◽  
Control Group ◽  
Pyridine Derivatives ◽  
Immobility Time

In this study, we synthetized a series of 5-aryl-4,5-dihydrotetrazolo[1,5-a]thieno[2,3-e]pyridine derivatives containing tetrazole and other heterocycle substituents, i.e., triazole, methyltriazole, and triazolone. The forced swim test (FST) and tail suspension test (TST) were used to evaluate the antidepressant activity of the target compounds. The compound 5-[4-(trifluoromethyl)phenyl]-4,5-dihydrotetrazolo[1,5-a]thieno[2,3-e]pyridine (4i) showed the highest antidepressant activity, with a reduced immobility time of 55.33% when compared with the control group. Using an open-field test, compound 4i was shown to not affect spontaneous activity of mice. The determination of in vivo 5-hydroxytryptamine (5-HT) concentration showed that compound 4i may have an effect in the mouse brain. The biological activities of all synthetized compounds were verified by molecular docking studies. Compound 4i showed significant interactions with residues of the 5-HT1A receptor homology model.

scholarly journals Design, Synthesis, and In Vivo and In Silico Evaluation of Coumarin Derivatives with Potential Antidepressant Effects

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5556
Author(s):  
Xuekun Wang ◽  
Hao Zhou ◽  
Xinyu Wang ◽  
Kang Lei ◽  
Shiben Wang
Keyword(s):  
Molecular Docking ◽  
High Resolution Mass Spectrometry ◽  
Forced Swim Test ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Homology Model ◽  
Coumarin Derivatives ◽  
Monitoring Methods ◽  
Discovery Studio

In this study, a series of coumarin derivatives were designed and synthesized, their structures were characterized using nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) testing methods. In the pharmacological experiment, two behavior-monitoring methods, the forced swim test (FST) and the tail suspension test (TST), were used to determine the antidepressant activity of coumarin derivatives. Compounds that showed potential activity were analyzed for their effects on 5-hydroxytryptamine (5-HT) levels in the brains of mice. Molecular docking experiments to simulate the possible interaction of these compounds with the 5-HT1A receptor was also be predicted. The results of the pharmacological experiments showed that most coumarin derivatives exhibited significant antidepressant activity. Among these compounds, 7-(2-(4-(4-fluorobenzyl)piperazin-1-yl)-2-oxoethoxy)-2H-chromen-2-one (6i) showed the highest antidepressant activity. The results of the measurement of 5-HT levels in the brains of mice indicate that the antidepressant activity of coumarin derivatives may be mediated by elevated 5-HT levels. The results of molecular docking demonstrated that compound 6i had a significant interaction with amino acids around the active site of the 5-HT1A receptor in the homology model. The physicochemical and pharmacokinetic properties of the target compounds were also predicted using Discovery Studio (DS) 2020 and Chemdraw 14.0.

scholarly journals 11-β hydroxysteroid type 1 knockout mice display an antidepressant-like phenotype in the forced swim test

2015 ◽  
Vol 28 (1) ◽  
pp. 55-60 ◽  
Author(s):  
David A. Slattery ◽  
Doncho P. Uzunov ◽  
John F. Cryan
Keyword(s):  
Knockout Mice ◽  
Forced Swim Test ◽  
Indirect Evidence ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Genetic Ablation ◽  
Swim Test ◽  
Forced Swim ◽  
Biological Substrates

Objective11β-dehydroxysteroid dehydrogenase (HSD) types 1 and 2, enzymes are involved in the activation and inactivation of glucocorticoids in vivo, respectively. Indirect evidence implicates two enzymes in the aetiology of depression but no study has directly assessed the potential role of 11 β-HSD1 in animal tests.MethodsWe assessed 11 β-HSD1 knockout mice in the forced swim test (FST), tail suspension test (TST) and for locomotor activity.ResultsGenetic ablation of the 11β-HSD1 gene results in an antidepressant-like phenotype in the FST; the most widely utilised animal test of antidepressant activity, but not in the related TST. This may be related to the different biological substrates underlying these tests. The decreased FST immobility was not due to alterations in general activity.ConclusionsTaken together these results suggest that 11β-HSD1 may play an important role in depression-related behaviours and further studies are necessary to fully characterise its role in such behaviour.

scholarly journals Phytochemical screening and evaluation of antidepressant activity of methanolic extract of the spadix of Colocasia affinis Schott

2018 ◽  
Vol 18 (4) ◽  
pp. 104-110
Author(s):  
C. Lalremruati ◽  
C. Malsawmtluangi ◽  
H. Lalhlenmawia
Keyword(s):  
Methanolic Extract ◽  
Petroleum Ether Extract ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Chloroform Extract ◽  
Control Group ◽  
Force Swim Test ◽  
Standard Drug ◽  
In Vivo Test

The objective of this study was to determine the phytoconstituents present in successive extracts and the antidepressant activity of methanolic extract of the spadix of Colocasia affinis. The preliminary phytochemical investigation indicated the presence of fats and fixed oils, steroids and triterpenoids in petroleum ether extract, steroids and triterpenoids in chloroform extract, flavonoids and tannins in methanol extract and carbohydrates in the aqueous extract. An in vivo test for antidepressant activity was performed on the methanolic extract of the plant at two different doses using force swim test and tail suspension test on an experimental animal model (rat). Imipramine was used as a standard drug for the study. The methanolic extract at 200 and 400 mg/kg, produced significant reduction (p<0.001) in the immobility period when compared with that of control group animals in both the tests. Thus, the result indicates that the methanolic extract exhibited significantly good antidepressant activity. Further investigation may be needed to understand the actual mechanism of action.

scholarly journals Pharmacological In vivo test to evaluate the antidepressant activity of polyherbal formulation

2019 ◽  
Vol 7 (1) ◽  
pp. 63-73
Author(s):  
Rinki Kumar ◽  
K. Ilango ◽  
G.P.I. Singh ◽  
G.P. Dubey
Keyword(s):  
Forced Swim Test ◽  
Antidepressant Activity ◽  
Control Group ◽  
Potential Candidate ◽  
Standard Drug ◽  
In Vivo Test ◽  
Polyherbal Formulation ◽  
Immobility Time ◽  
Model Control

The antidepressant effects of the polyherbal formulation (PF) (contain four extracts of medicinal plants namely: Nyctanthes arbortristis, Hippophae salcifolia, Ocimum tenuiflorum and Withania somnifera ) was examined by evaluating the extent of reduction of behavioural alterations and neurotransmitter in the rats stressed by forced swim test (FST). In the present study, compared with the model control group (FST), the altered behavioural parameters were attenuated significantly (P < 0.05) in the group treated with the PF (100, 200 and 400 mg•kg−1), comparable with the standard drug treated group, Sertraline (10mg•kg−1). The PF and Sertraline significantly (P < 0.05) increased the level of the neurotransmitter such as serotonin, dopamine, acetylcholine and noradrenalin whereas decreased the level of monoamine oxidase along with oxidant in the brain of the stressed rats. PF and Sertraline were also involved in the reduced oxidant and generated antioxidant in the stressed rats. The results indicated that polyherbal formulation exhibited significant antidepressant activity, as indicated by its ability to decrease force swim stress, induced immobility time in rats as well as restoring the biogenic amines to normal level that were altered by the swim induced stress in whole rat brain. Therefore, PF can be a potential candidate for treatment of depression as well as a potent antidepressant. However, further studies are required to substantiate the same.

scholarly journals In Vivo Gastroprotective and Antidepressant Effects of Iridoids, Verbascoside and Tenuifloroside from Castilleja tenuiflora Benth

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1292 ◽  
Author(s):  
Ricardo López-Rodríguez ◽  
Maribel Herrera-Ruiz ◽  
Gabriela Trejo-Tapia ◽  
Blanca Eda Domínguez-Mendoza ◽  
Manasés González-Cortazar ◽  
...  
Keyword(s):  
Forced Swim Test ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Gastrointestinal Diseases ◽  
Gastric Ulcers ◽  
Antidepressant Effects ◽  
Organic Extracts ◽  
Ulcer Model ◽  
Cold Restraint Stress

Stress is an important factor in the etiology of some illnesses such as gastric ulcers and depression. Castilleja tenuiflora Benth. (Orobanchaceae) is used in Mexican traditional medicine for the treatment of gastrointestinal diseases and nervous disorders. Previous studies indicated that organic extracts from C. tenuiflora had gastroprotective effects and antidepressant activity. In this study, we aimed to evaluate the gastroprotective and antidepressant activity of fractions and isolated compounds from the methanolic extract (MECt) of C. tenuiflora in stressed mice. Chromatographic fractionation of MECt produced four fractions (FCt-1, FCt-2, CFt-3, and FCt-4) as well as four bioactive compounds which were identified using TLC, HPLC and NMR analyses. The cold restraint stress (CRS)-induced gastric ulcer model followed by the tail suspension test and the forced swim test were used to evaluate the gastroprotective effect and antidepressant activity of the extract fractions. FCt-2 and FCt-3 at 100 mg/kg had significant gastroprotective and antidepressant effects. All isolated compounds (verbascoside, teniufloroside and mixture geniposide/ musseanoside) displayed gastroprotective effects and antidepressant activity at 1 or 2 mg/kg. The above results allow us to conclude that these polyphenols and iridoids from C. tenuiflora are responsible for the gastroprotective and antidepressant effects.

Pyrrolopyrazoles: Synthesis, Evaluation and Pharmacological Screening as Antidepressant Agents

2019 ◽  
Vol 15 (8) ◽  
pp. 911-922 ◽  
Author(s):  
Samar S. Fatahala ◽  
Shahira Nofal ◽  
Eman Mahmoud ◽  
Rania H. Abd El-hameed
Keyword(s):  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Positive Control ◽  
Biologically Active ◽  
Control Group ◽  
Standard Drug ◽  
Behavioral Techniques ◽  
Special Concern ◽  
Pharmacological Screening ◽  
The Brain

Background: Pyrroles and fused pyrroles are of great interest as biologically active compounds, among these activities; antidepressant activity is of special concern. Objective: Synthesis of a series of pyrrolopyrazoles and their pyrimidine derivatives and their characterization using spectral data to be monitored for antidepressant activity using behavioral techniques. Methods: A control group was administered the vehicle i.p., positive control group received fluoxetine as standard and all other groups were administered the tested compounds. The groups were subjected to tail suspension test (TST) to determine the antidepressant activity compared with fluoxetine as a standard drug. The compounds exhibiting antidepressant activity were then used to analyze changes in serotonin (5HT) level in the brain of albino mice. Results: TST results showed that both pyrazoles and pyrazolopyrimidines derivatives exhibit promising anti-depressant activity. Conclusion: Compounds [pyrazoles & pyrazlopyrimidines] showed promising antidepressant activity possibly mediated by the increased levels of 5HT.

scholarly journals EXPERIMENTAL EVALUATION OF ANTIDEPRESSANT AND ANTIANXIETY ACTIVITIES OF AQUEOUS LEAF EXTRACTS OF SENNA ALATA (L.) ROXB. USING IN VITRO ANIMAL MODELS

2016 ◽  
Vol 8 (4) ◽  
pp. 60
Author(s):  
Archana Pamulaparthi ◽  
Vamshi Ramana Prathap ◽  
Mahitha Banala ◽  
Rama Swamy Nanna
Keyword(s):  
Forced Swim Test ◽  
Antidepressant Activity ◽  
Tail Suspension Test ◽  
Control Group ◽  
Test Drug ◽  
Leaf Extracts ◽  
Standard Drug ◽  
The Mean ◽  
Senna Alata

Objective: In the present investigation antidepressant and antianxiety activities of aqueous leaf extracts of Senna alata (200 mg/Kg) were carried out to establish the species as a potent natural antidepressant and anxiolytic drug.Methods: Antidepressant activity was carried out using forced swim test and tail suspension test. In both these tests, the animals were subjected to external stress that results in alteration of the behavior of animal due to fear.The antianxiety activity of aqueous leaf extracts of S. alata has been studied by the elevated plus-maze test in rats. The mean number of entries and the time spent in the open arm after 45 min of the administration of test drug was noted to determine the antianxiety effect of the test drug.Results: For antidepressant activity administration of test drug (200 mg/Kg) showed a significant decrease in the time spent by the animal in state of depression in both the assays which clearly indicates that the aqueous leaf extracts of S. alata exhibited a strong antidepressant activity similar to that of the control drug (Imipramine).In the antianxiety activity, administration of aqueous leaf extract (200 mg/Kg) of S. alata significantly increased the mean number of entries (2.25±0.98) in the open arm and the time spent in open arm (2.23±0.04) compared to the control group. The activity of the extract was slightly greater than standard drug Diazepam.Conclusion: From the above-presented results, it can be concluded that administration of Senna alata aqueous leaf extracts (200 mg/Kg) showed a considerable decrease in both antidepressant and antianxiety activities in all the test animals and can be used in the replacement of commercially available synthetic drugs in the near future.

scholarly journals Synthesis and Evaluation of the Antidepressant-like Properties of HBK-10, a Novel 2-Methoxyphenylpiperazine Derivative Targeting the 5-HT1A and D2 Receptors

2021 ◽  
Vol 14 (8) ◽  
pp. 744
Author(s):  
Kinga Sałaciak ◽  
Natalia Malikowska-Racia ◽  
Klaudia Lustyk ◽  
Agata Siwek ◽  
Monika Głuch-Lutwin ◽  
...  
Keyword(s):  
Forced Swim Test ◽  
Chronic Administration ◽  
Tail Suspension Test ◽  
D2 Receptors ◽  
Intrinsic Activity ◽  
Pharmacological Profile ◽  
Behavioral Experiments ◽  
Number Of Patients

The increasing number of patients reporting depressive symptoms requires the design of new antidepressants with higher efficacy and limited side effects. As our previous research showed, 2-methoxyphenylpiperazine derivatives are promising candidates to fulfill these criteria. In this study, we aimed to synthesize a novel 2-methoxyphenylpiperazine derivative, HBK-10, and investigate its in vitro and in vivo pharmacological profile. After assessing the affinity for serotonergic and dopaminergic receptors, and serotonin transporter, we determined intrinsic activity of the compound at the 5-HT1A and D2 receptors. Next, we performed behavioral experiments (forced swim test, tail suspension test) to evaluate the antidepressant-like activity of HBK-10 in naïve and corticosterone-treated mice. We also assessed the safety profile of the compound. We showed that HBK-10 bound strongly to 5-HT1A and D2 receptors and presented antagonistic properties at these receptors in the functional assays. HBK-10 displayed the antidepressant-like effect not only in naïve animals, but also in the corticosterone-induced mouse depression model, i.e., chronic administration of HBK-10 reversed corticosterone-induced changes in behavior. Moreover, the compound’s sedative effect was observed at around 26-fold higher doses than the antidepressant-like ones. Our study showed that HBK-10 displayed a favorable pharmacological profile and may represent an attractive putative treatment candidate for depression.

Hypothalamic regulation of reproduction under the chronic influence of toluene and melatonin

2021 ◽  
Vol 50 (2) ◽  
pp. 42-46
Author(s):  
G. O. Kerkeshko
Keyword(s):  
Biogenic Amines ◽  
Preoptic Area ◽  
Chronic Administration ◽  
Female Rats ◽  
Control Group ◽  
Simultaneous Administration ◽  
Chronic Effect ◽  
Circadian Variations ◽  
Hypothalamic Regulation ◽  
Maximal Permissible Concentration

Experiments on chronic administration of melatonin with and without chronic inhalation of toluene dosed at both maximal permissible concentration (50 mg/ml) and limited chronical range (500 mg/m3) have been carried out on female rats to discover their effects on biogenic amines system in hypothalamic structures related to gonadoliberin synthesis and secretion - preoptic area (PA) and median eminence (ME). Contents of biogenic amines in ME and especially in PA have been shown to have circadian variations with maximum in the morning in control group of rats.The chronic effect of synchronizing agent melatonin (administered dissolved in drinking water in concentration of 10 pg/m l, at night during 2 months) on neotransmitters and their circadian variations in both hypothalamic structures proved surprisingly to be much alike the effect of toluene. Both chemicals cause the disturbances of normal circadian variations o f norepinephrine, dopamine and serotonine in PA and dopamine in ME. The simultaneous administration of toluene and melatonin showed likewise no synchronizing ability of the latter under the conditions described.

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