scholarly journals Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine

2014 ◽  
Vol 50 (1) ◽  
pp. 73-81
Author(s):  
Martín Hermógenes Estrada ◽  
Henry Insuasty ◽  
Luis Enrique Cuca ◽  
Mariel Marder ◽  
Angélica Fierro ◽  
...  
Keyword(s):  
Maximal Electroshock ◽  
Dependent Manner ◽  
Maximal Electroshock Seizure ◽  
Gaba A ◽  
Mao B ◽  
Plus Maze ◽  
Marble Burying ◽  
One Step ◽  
Dose Dependent ◽  
Benzodiazepine Site

This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.

scholarly journals ANTICONVULSANT ACTIVITY OF CITRUS MAXIMUS LEAVES IN EXPERIMENTAL ANIMAL MODELS

2016 ◽  
Vol 9 (9) ◽  
pp. 97
Author(s):  
Nishanta Thakuria ◽  
Swarnamoni Das ◽  
Babul Dewan
Keyword(s):  
Anticonvulsant Activity ◽  
Albino Rats ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Dependent Manner ◽  
Maximal Electroshock Seizure ◽  
Wistar Strain ◽  
Seizure Models ◽  
Clonic Convulsions ◽  
Dose Dependent

ABSTRACTObjective: To assess the anticonvulsant activity of ethanolic extract of Citrus maximus (EECM) leaves of maximal electroshock seizure (MES) andpentylenetetrazol (PTZ)-induced seizure models on albino (Wistar strain) rats and mice.Methods: Anticonvulsant activity was carried out by MES model and PTZ-induced clonic convulsions model; in each model, albino rats (Wistar strain)of either sex were taken and divided into five groups, each consisting of 6 rats. One group was used as control (3% w/v gum acacia), one as standard(phenytoin), and three groups for the test drug of EECM leaves (doses of 50, 100, and 200 mg/kg) treatment. The reduction in time or abolition of tonicextensor phase of MES-convulsions was recorded for all the animals. In PTZ model, either delay or complete abolition of convulsions in rats treatedwith diazepam and EECM leaves was noted for all the animals.Result: EECM leaves reduced the extensor phase of convulsion in MES in a dose-dependent manner and decrease in the duration of convulsions in PTZmodel with increasing dose. Anticonvulsant activity was seen maximum at the dose of 200 mg/kg.Conclusions: Thus, from the above two seizure models of MES and PTZ, it can be concluded that EECM leaves have got an anticonvulsant effect in anincreasing dose-dependent manner.Keywords: Anticonvulsant, Citrus maximus, Maximal electroshock seizure, Pentylenetetrazol.

Synthesis of Chromen-1-phenylpropen-1-one Derivatives and their Antidepressant/Anticonvulsant Activities

2021 ◽  
Vol 18 ◽  
Author(s):  
Shan-Shan Zhang ◽  
Wei-Hua Liu ◽  
Zhi-Wen He ◽  
Qiu-Wan Tan ◽  
Li-Ping Guan
Keyword(s):  
Biological Activities ◽  
Serotonin Level ◽  
Maximal Electroshock ◽  
Dependent Manner ◽  
Plant Metabolites ◽  
Maximal Electroshock Seizure ◽  
High Biological Activity ◽  
Secondary Plant Metabolites ◽  
Antidepressant Effects ◽  
Immobility Time

Background: Coumarin and chalcone are important secondary plant metabolites that exhibit a range of biological activities. Accordingly, the synthetic derivatives and analogs of these molecules have attracted attention as potential pharmacological agents Objective: This study aims to study new antidepressants with high biological activity and low side effects, and to provide a basis for the treatment of epilepsy and depression. Method: In this study, a series of chalcone derivatives containing a coumarin moiety (2a–2s) was designed, synthesized, and evaluated using classic antidepressant and anticonvulsant mouse models. Results: Forced swimming test results revealed that all but one of the compounds tested significantly decrease immobility time at a dose of 10 mg/kg and exhibit some antidepressant activity. Furthermore, compounds 2a, 2c, 2h, and 2k exhibit relatively high antidepressant effects in a dose-dependent manner from 10 to 30 mg/kg. Maximal electroshock seizure tests showed that compounds 2a, 2b, 2c, 2h, 2l, 2r, and 2s exhibit anticonvulsant activity at a dose of 30 mg/kg. Conclusion: Accordingly, compounds 2a, 2c, and 2h show promise as antidepressant adjunct therapy agents for treating depression in patients with epilepsy. Chromatographic neurochemical analysis of the mouse brain tissue revealed that the antidepressant effects of the compounds may be mediated by an increase in serotonin level.

Dose-dependent Enhancement of In Vivo  GABAA–Benzodiazepine Receptor Binding by Isoflurane

2001 ◽  
Vol 95 (3) ◽  
pp. 585-593 ◽  
Author(s):  
Ferenc E. Gyulai ◽  
Mark A. Mintun ◽  
Leonard L. Firestone
Keyword(s):  
Minimum Alveolar Concentration ◽  
Distribution Volume ◽  
T Test ◽  
Dependent Manner ◽  
Gamma Aminobutyric Acid ◽  
General Anesthetics ◽  
Gaba A ◽  
Site Density ◽  
Dose Dependent

Background Abundant in vitro and animal model data suggest the postsynaptic gamma-aminobutyric acid receptor type A (GABA(A)-R) is an important target for volatile general anesthetics, but the relevance of these models is untested in humans. Because benzodiazepines have also been shown to act via a specific GABA(A)-R site, they provide sensitive probes for the GABA(A)-R. Availability of the 11C-labeled benzodiazepine ligand, flumazenil, allowed us to quantitatively test in humans whether the volatile anesthetic isoflurane affects GABA(A)-Rs in vivo in a dose-dependent manner. Methods 11C-flumazenil positron emission tomography scans were obtained in 12 healthy subjects while awake (control condition) and anesthetized with either 1.0 or 1.5 minimum alveolar concentration isoflurane (n = 7 and 5, respectively; isoflurane conditions). Regions of interest included areas of high, intermediate, and low GABA(A)-benzodiazepine site density. For each subject and experimental condition, the binding of 11C-flumazenil, expressed as distribution volume (which linearly correlates to maximal binding site density and apparent ligand affinity), was obtained by curve fitting using a two-compartment model. Results The ratio of distribution volume increased significantly in each examined region during the isoflurane conditions compared with control conditions (P < 0.01, one-tailed t test). Furthermore, the increases in ratio of distribution volume during the 1.5-minimum alveolar concentration isoflurane condition were significantly greater than those measured during 1.0 minimum alveolar concentration isoflurane inhalation (P < 0.002, one-tailed t test). Conclusions Isoflurane exposure appeared to enhance receptor-specific 11C-flumazenil binding in a dose-dependent manner. The results suggest the possibility that a conformational change of the GABA(A)-R is involved in the mechanism of action of isoflurane in the living human brain.

scholarly journals Anticonvulsant Effects of Aerial Parts of Verbena officinalis Extract in Mice: Involvement of Benzodiazepine and Opioid Receptors

2017 ◽  
Vol 22 (4) ◽  
pp. 632-636 ◽  
Author(s):  
Amir Rashidian ◽  
Fatemeh Kazemi ◽  
Saeed Mehrzadi ◽  
Ahmad Reza Dehpour ◽  
Shahram Ejtemai Mehr ◽  
...  
Keyword(s):  
Anticonvulsant Activity ◽  
Hind Limb ◽  
Ethanolic Extract ◽  
Maximal Electroshock ◽  
Dependent Manner ◽  
Reference Drug ◽  
Mes Test ◽  
Aerial Parts ◽  
Tonic Extension ◽  
Dose Dependent

To evaluate the anticonvulsant activity of the aerial parts of Verbena officinalis used traditionally by local Iranians for the treatment of convulsion. The anticonvulsant activity of the extract was assessed in pentylenetetrazole (PTZ) and maximal electroshock (MES) induced seizures in mice. Diazepam was used as reference drug. In addition, for investigating the mechanism of V officinalis in PTZ model, flumazenil and naloxone were injected before V officinalis. The extract showed no toxicity and significantly increased the period taken before the onset and decreased the duration of the seizures induced by PTZ. In the MES test, V officinalis displayed significant reduction in hind limb tonic extension duration in a dose-dependent manner. The results propose that V officinalis ethanolic extract has anticonvulsant activity against seizure. It seems that these effects may be related to potentiating of GABAergic system. Moreover, this study supports the use of this plant by local Iranians in order to treat convulsion.

scholarly journals Efficacy and safety of the metformin-mazindol anorectic combination in rat

2021 ◽  
Vol 71 (2) ◽  
pp. 279-291
Author(s):  
Federico Argüelles-Tello ◽  
José Eduardo Roa-Coria ◽  
Ángel Zúñiga-Romero ◽  
Juan Carlos Huerta-Cruz ◽  
Geovanna Nalley Quiñonez-Bastidas ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Effective Dose ◽  
Elevated Plus Maze ◽  
Blood Chemistry ◽  
Dependent Manner ◽  
Interaction Index ◽  
Elevated Plus Maze Test ◽  
Plus Maze ◽  
Anorectic Effect ◽  
Dose Dependent

AbstractThe current study investigates the anorectic interaction and safety of the mazindol-metformin combination in rats. Isobologram and interaction index were used to determine anorectic interaction between mazindol and metformin in the sweetened milk model. The safety profile of the mazindol-metformin combination was determined by measuring anxiety, blood pressure, hematic biometry and blood chemistry. An acute dose of mazindol and metformin administered per os, individually or as a mixture, has reduced the milk consumption in rats in a dose-dependent manner. Theoretical effective dose 40 (ED40t) did not differ from the experimental effective dose 40 (ED40e) obtained with the mazindol-metformin mixture in the anorexia experiments, by Student′s t-test. In addition, the interaction index confirmed the additive anorectic effect between both drugs. A single oral dose of ED40e mazindol-metformin mixture induced anxiolysis in the elevated plus-maze test. Moreover, oral administration of mazindol-metformin combination for 3 months significantly decreased glycemia, but not blood pressure nor other parameters of hematic biometry and blood chemistry. Results suggest that mazindol-metformin combination exerts an additive anorectic effect, as well as anxiolytic and hypoglycemic properties. Mazindol-metformin combination might be useful in obese patients with anxiety disorders or diabetes risk factors.

ISOLATION OF TECOMINE FROM ALKALOID FRACTION, INVESTIGATION OF ADAPTOGENIC AND NEUROPSYCHOPHARMACOLOGICAL EFFECTSOF ETHANOLIC, ETHYL ACETATE AND HEXANE FLOWER EXTRACTS OF TECOMA GAUDICHAUDI

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (04) ◽  
pp. 63-74
Author(s):  
K. Ravishankar ◽  
◽  
G.V.N. Kiranmayi ◽  
Y. Rajendra Prasad
Keyword(s):  
Ethyl Acetate ◽  
Conditioned Avoidance ◽  
Vanillylmandelic Acid ◽  
Nootropic Activity ◽  
Dependent Manner ◽  
Spectrophotometric Methods ◽  
Plus Maze ◽  
Forced Swim Stress ◽  
Alkaloid Fraction ◽  
Dose Dependent

The present study aims to evaluate antistress and neuropharmacological parameters of ethanolic, ethyl acetate and hexane flower extracts of Tecoma gaudichaudi. Forced swim stress was used to evaluate antistress activity. The 24 h urinary excretion of vanillylmandelic acid (VMA) and ascorbic acid were determined by spectrophotometric methods in all groups under normal and stressed conditions. In the present study, the extracts (200 and 400 mg/kg, p.o.) were investigated for nootropic activity in rats with and without stress. Cook’s pole climbing apparatus measures conditioned avoidance response, elevated plus maze determines transfer latency and staircase test calculates the number of steps climbed and rearings in normal and stress induced rats to assess cognitive-improving activities. Cognition was enhanced by daily administration of Tecoma gaudichaudi extracts at doses of 200 and 400 mg/kg, p.o. in dose dependent manner in normal rats. Tecomine and its derivatives were isolated from alkaloidal fraction.

scholarly journals Evaluation of the Anxiolytic Activity of NR-ANX-C (a Polyherbal Formulation) in Ethanol Withdrawal-Induced Anxiety Behavior in Rats

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
L. Mohan ◽  
U. S. C. Rao ◽  
H. N. Gopalakrishna ◽  
V. Nair
Keyword(s):  
Drinking Water ◽  
Anxiolytic Activity ◽  
Ethanol Withdrawal ◽  
Ocimum Sanctum ◽  
Dependent Manner ◽  
Standard Drug ◽  
Polyherbal Formulation ◽  
Plus Maze ◽  
Anxiety Behavior ◽  
Dose Dependent

The present study investigates the anxiolytic activity of NR-ANX-C, a standardized polyherbal formulation containing the extracts ofWithania somnifera, Ocimum sanctum, Camellia sinensis, Triphala, and Shilajit in ethanol withdrawal- (EW-) induced anxiety behavior in rats. Ethanol dependence in rats was produced by substitution of drinking water with 7.5% v/v alcohol for 10 days. Then, ethanol withdrawal was induced by replacing alcohol with drinking water, 12 hours prior to experimentation. After confirming induction of withdrawal symptoms in the alcohol deprived animals, the anxiolytic activity of the test compound in graded doses (10, 20, and 40 mg/kg) was compared to the standard drug alprazolam (0.08 mg/kg) in the elevated plus maze and bright and dark arena paradigms. In our study, single and repeated dose administration of NR-ANX-C reduced EW-induced anxiety in a dose-dependent manner. Even though the anxiolytic activity was not significant at lower doses, NR-ANX-C at the highest dose tested (40 mg/kg) produced significant anxiolytic activity that was comparable to the standard drug alprazolam. Based on our findings we believe that NR-ANX-C has the potential to be used as an alternative to benzodiazepines in the treatment of EW-induced anxiety.

scholarly journals Pharmacological Evaluation of Naproxen Metal Complexes on Antinociceptive, Anxiolytic, CNS Depressant, and Hypoglycemic Properties

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Md. Sharif Hasan ◽  
Narhari Das ◽  
Zobaer Al Mahmud ◽  
S. M. Abdur Rahman
Keyword(s):  
Metal Complexes ◽  
Elevated Plus Maze ◽  
Zinc Complexes ◽  
Antinociceptive Activity ◽  
Tail Flick ◽  
Dependent Manner ◽  
Cns Depressant ◽  
Plus Maze ◽  
Dose Dependent ◽  
Parent Ligand

Purpose. The present study was designed to investigate the antinociceptive, anxiolytic, CNS depressant, and hypoglycemic effects of the naproxen metal complexes.Methods. The antinociceptive activity was evaluated by acetic acid-induced writhing method and radiant heat tail-flick method while anxiolytic activity was evaluated by elevated plus maze model. The CNS depressant activity of naproxen metal complexes was assessed using phenobarbitone-induced sleeping time test and the hypoglycemic test was performed using oral glucose tolerance test.Results. Metal complexes significantly (P<0.001) reduced the number of abdominal muscle contractions induced by 0.7% acetic acid solution in a dose dependent manner. At the dose of 25 mg/kg body weight p.o. copper, cobalt, and zinc complexes exhibited higher antinociceptive activity having 59.15%, 60.56%, and 57.75% of writhing inhibition, respectively, than the parent ligand naproxen (54.93%). In tail-flick test, at both doses of 25 and 50 mg/kg, the copper, cobalt, silver, and zinc complexes showed higher antinociceptive activity after 90 minutes than the parent drug naproxen. In elevated plus maze (EPM) model the cobalt and zinc complexes of naproxen showed significant anxiolytic effects in dose dependent manner, while the copper, cobalt, and zinc complexes showed significant CNS depressant and hypoglycemic activity.Conclusion. The present study demonstrated that copper, cobalt, and zinc complexes possess higher antinociceptive, anxiolytic, CNS depressant, and hypoglycemic properties than the parent ligand.

scholarly journals TO EVALUATE THE EFFECT OF MORUS ALBA LEAVES EXTRACT ON SLEEP AND ANXIETY IN RAT MODELS

2021 ◽  
pp. 100-102
Author(s):  
SRIHARSHA RAYAM ◽  
KUDAGI BL ◽  
RAMYA JONNALAGADDA ◽  
RAVEENDRA KUMAR NALLABOTHULA
Keyword(s):  
Elevated Plus Maze ◽  
Morus Alba ◽  
Control Group ◽  
Dependent Manner ◽  
Sleeping Time ◽  
Elevated Plus Maze Test ◽  
Plus Maze ◽  
The Mean ◽  
Mean Time ◽  
Dose Dependent

Objectives: The objectives of the study were to study the effect of Morus alba leaves extract (MAE) on sleep by phenobarbitone-induced sleeping time and the antianxiety effect by elevated plus maze apparatus model in rats. Methods: In this study, the effect of MAE on sleep was evaluated by the phenobarbitone-induced sleeping time of rats. The onset and the duration of sleep were recorded in minutes. The antianxiety effect was evaluated by the elevated plus maze apparatus model in rats. During 5 min test period, the number of entries into the open arm and closed arm and time spent in the open arm and closed arm were recorded in seconds. Results: MAE at the dose 200 and 400 mg/kg, highly significantly (p<0.001) decreased the onset of phenobarbitone-induced sleeping time. The duration of sleeping time was increased significantly (p<0.01) for 200 mg/kg and highly significantly (p<0.001) for 400 mg/kg as compared to the control group. M. alba has significant antianxiety activity in comparison with control in a dose-dependent manner. M. alba in a dose of 200 mg showed significant (p<0.01) and 400 mg/kg treated groups showed highly significant (p<0.001) anxiolytic activity by increasing the mean time spent in open arms as compared to control but less significant with standard (diazepam). Conclusion: Results indicate that the MAE has a significant dose-dependent effect on phenobarbitone- induced sleeping time and antianxiety effect in the elevated plus maze test.

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