scholarly journals A GROUP OF COMPOUNDS POSSESSING ANTICONVULSANT ACTIVITY IN THE MAXIMAL ELECTROSHOCK SEIZURE TEST

1957 ◽  
Vol 6 (2) ◽  
pp. 115-121 ◽  
Author(s):  
KIYOSHI TANAKA ◽  
YOSUKE KAWASAKI
Keyword(s):  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Maximal Electroshock Seizure Test

Synthesis and Anticonvulsant Activity of α-Amino Acid Amide Derivatives

2019 ◽  
Vol 15 (5) ◽  
pp. 547-561
Author(s):  
Valerie Currier ◽  
Maryam Molki ◽  
Katelyn Fryman ◽  
Lacey D. Rodgers ◽  
A. Michael Crider
Keyword(s):  
Amino Acid ◽  
Side Effects ◽  
Anticonvulsant Activity ◽  
Acid Amide ◽  
New Drugs ◽  
Seizure Threshold ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Maximal Electroshock Seizure Test ◽  
Amide Derivatives

Background: Epilepsy is a disease of the central nervous system that affects approximately 50 million individuals worldwide. Although several new drugs have been marketed in the last 25 years, almost one-third of patients are not protected. In many cases, currently available drugs produce undesirable side effects. As a result, a need exists for novel anticonvulsants with unique mechanisms of action and minimal side effects. Methods: A mixed anhydride coupling procedure and standard deprotection procedures were utilized to prepare 36 α-amino acid amides. All final products were evaluated in mice and rats utilizing a standard battery of anticonvulsant tests. Results: α-Amino acids containing a 2,6-dimethylanilide group exhibited anticonvulsant activity in the maximal electroshock seizure test and 6 Hz test in mice and rats. A small, branched-chain on the α- carbon generally maintained or enhanced anticonvulsant activity in the maximal electroshock seizure test. The (R)-α-amino acid amides were typically more potent and slightly more neurotoxic than the corresponding (S)-enantiomers. The valine dimethylanilide (R)-42 was highly active in the MES test in mice (ED50 = 3.6mg/kg) and rats (ED50 = 3.8 mg/kg). (R)-42 also demonstrated excellent anticonvulsant activity in the 6 Hz, picrotoxin, and corneal kindled mouse tests. Furthermore, (R)-42 did not lower seizure threshold when evaluated in the intravenous metrazol seizure test. Conclusion: α-Amino acid 2,6-dimethylanilides exhibited potent activity in a variety of anticonvulsant tests in mice and rats. The valine derivative (R)-42 represents a promising compound for potential use in complex partial seizures.

Evaluation of the Anticonvulsant Activity of Terpinen-4-ol

2009 ◽  
Vol 64 (1-2) ◽  
pp. 1-5 ◽  
Author(s):  
Damião P. de Sousa ◽  
Franklin F. F. Nóbrega ◽  
Liana C. S. L. de Morais ◽  
Reinaldo N. de Almeida
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Animal Models ◽  
Motor Activity ◽  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Aromatic Plants ◽  
Depressant Effect ◽  
Maximal Electroshock Seizure ◽  
The Central Nervous System

Terpinen-4-ol is a monoterpenoid alcohol and component of the essential oils of several aromatic plants. Similarly to terpinen-4-ol, other monoterpenoid alcohols have shown anticonvulsant activity in convulsion animal models. The present study aimed to investigate the anticonvulsant activity of terpinen-4-ol. Treatment of mice with terpinen-4-ol ( 200 mg/kg) caused a signifi cant decrease in the spontaneous motor activity at 30, 60 and 120 min after administration. Terpinen-4-ol (100 and 200 mg/kg) produced a significant dosedependent increase in the duration of sleeping in mice. Pretreatment of mice with terpinen-4- ol at doses of 100, 200 and 300 mg/kg significantly increased the latency of pentylenetetrazole -induced convulsions. Terpinen-4-ol (200 and 300 mg/kg) also inhibited the induced seizures of picrotoxin. In another model, maximal electroshock seizure, terpinen-4-ol decreased the tonic hind convulsions percentage at the dose of 300 mg/kg. From the overall results we can conclude that terpinen-4-ol showed a depressant effect on the central nervous system and significant anticonvulsant activity.

scholarly journals Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects

Marine Drugs ◽  
2019 ◽  
Vol 17 (7) ◽  
pp. 430 ◽  
Author(s):  
Qinghao Jin ◽  
Zhiyang Fu ◽  
Liping Guan ◽  
Haiying Jiang
Keyword(s):  
Forced Swimming Test ◽  
Antidepressant Activity ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Immobility Duration ◽  
Maximal Electroshock Seizure Test ◽  
Percentage Decrease ◽  
Swimming Test ◽  
Anticonvulsant Effects

Thirty-four new benzo[d]thiazol derivatives 2a–2i, 3a–3r, and 4a–4g were synthesized and investigated for their potential antidepressant and anticonvulsant effects. In a forced swimming test, 2c and 2d showed the highest antidepressant and anticonvulsant effects. 2c and 2d displayed a higher percentage decrease in immobility duration (89.96% and 89.62%, respectively) than that of fluoxetine (83.62%). In the maximal electroshock seizure test, 3n and 3q showed the highest anticonvulsant effect, with ED50 values of 46.1 and 64.3 mg kg−1, and protective indices of 6.34 and 4.11, respectively, which were similar to those of phenobarbital or valproate. We also found that the mechanism for the antidepressant activity of 2c and 2d may be via increasing the concentrations of serotonin and norepinephrine.

Captopril potentiates the anticonvulsant activity of carbamazepine and lamotrigine in the mouse maximal electroshock seizure model

2010 ◽  
Vol 117 (10) ◽  
pp. 1161-1166 ◽  
Author(s):  
Krzysztof Łukawski ◽  
Tomasz Jakubus ◽  
Grzegorz Raszewski ◽  
Stanisław J. Czuczwar
Keyword(s):  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Seizure Model

scholarly journals STUDY OF THE ANTICONVULSANT ACTIVITY OF ETHANOLIC EXTRACT OF ROOT OF ACORUS CALAMUS IN ALBINO RATS

2019 ◽  
Vol 12 (1) ◽  
pp. 185
Author(s):  
Shipra Kaushik ◽  
Kalpana Gohain
Keyword(s):  
Normal Saline ◽  
Anticonvulsant Activity ◽  
Ethanolic Extract ◽  
Albino Rats ◽  
Acorus Calamus ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Onset Of Action ◽  
Electrical Shock ◽  
Seizure Models

Objective: Root of Acorus calamus has been traditionally used as an anticonvulsant. The aim of the study is to assess the anticonvulsant activity of ethanolic extract of A. calamus (EEAC) by maximal electroshock seizure (MES) and pentylenetetrazol (PTZ)-induced seizure models on albino (Wistar strain) rats.Methods: Albino rats were taken and divided into five groups, each consisting of five rats both for MES and PTZ model. One group was used as control (normal saline 10 ml/kg), one as standard (phenytoin in MES model/diazepam in PTZ model), and three groups for the test drug (EEAC in the doses of 100, 200, and 400 mg/kg). In MES model, maximal electrical shock of 150 mA was passed for 0.2 s through earlobe electrodes after 30 min of giving the drugs and normal saline. Different stages of convulsions were noted down along with time spent by the animal in each phase of convulsions. In PTZ model, PTZ was injected 30 min after giving the drugs and normal saline, and onset of action and severity of convulsions were noted. Data were statistically analyzed by one-way analysis of variance followed by multiple Dunnett’s test.Results: EEAC dose dependently reduced the duration of tonic hind limb extension in MES model, and there was increase in latency and occurrence of convulsions in PTZ model.Conclusion: EEAC has anticonvulsant activity.

scholarly journals To evaluate the anticonvulsant activity of ethanolic extract of Moringa oleifera (drumstick leaves) in albino mice

2017 ◽  
Vol 6 (10) ◽  
pp. 2491
Author(s):  
Sushma V. Naidu ◽  
Harsha R. ◽  
Jyothsnya S.
Keyword(s):  
Anticonvulsant Activity ◽  
Hind Limb ◽  
Moringa Oleifera ◽  
Ethanolic Extract ◽  
P Value ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Isolation And Identification ◽  
Standard Drug ◽  
Albino Mice

Background: To evaluate the anti-convulsant activity of ethanolic extract of Moringa oleifera (Drum stick leaves) in seizure induced albino mice and to compare it with standard drug Sodium valproate.Methods: Swiss albino mice of either sex weighing around 25-30g were randomly selected and divided into four groups of six mice each. Group 1: control- treated with gum acacia. Group 2: Standard - Valproic acid 40mg/kg body weight. Group 3: T1- ethanolic extract of Moringa oleifera (150mg/kg). Group 4: T2 - ethanolic extract of Moringa oleifera (300mg/kg). All drugs were administered orally one hour prior to induction of seizure. The anticonvulsant activity was screened using maximal electroshock seizure (MES) model and pentylenetetrazole (PTZ) model.Results: Results were analysed by ANOVA followed by Bonferroni’s post hoc test. Abolition of Tonic hind limb extension was taken as the protective end point against MES induced seizures and prolongation of seizure latency in PTZ model.At both the doses the ethanolic extract of Moringa oleifera significantly (p value <0.05) reduced the duration of hind limb extension in MES test and also significantly (p value <0.05) delayed the onset of clonic seizures in PTZ induced convulsion when compared with control group.Conclusions: On comparing the percentage protection offered by Moringa oleifera leaves against both MES and PTZ model, it possesses significant anticonvulsant activity at both doses, with more efficacy at 300mg/kg BW indicating that the test drug can prove a very promising drug for treatment of epilepsy. Further studies are required for isolation and identification of the active constituent.

Synthesis and Pharmacological Evaluation of New Indolyl-oxadiazoles as Anticonvulsant Agents

2009 ◽  
Vol 2 (3) ◽  
pp. 661-666
Author(s):  
Harish Rajak ◽  
Ravichandran Veerasamy ◽  
Arun Kumar Gupta ◽  
Murli Dhar Kharya ◽  
Pradeep Mishra
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Anticonvulsant Activity ◽  
Anticonvulsant Drug ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Anticonvulsant Agents ◽  
Pharmacological Evaluation ◽  
Anticonvulsant Activities

The search for better anticonvulsant drug and the importance of 2,5-disubstituted 1,3,4-oxadiazoles and indole as anticonvulsant pharmacophores, prompted us to design, synthesize and evaluate a series of differently substituted 1,3,4-oxadiazoles for their potential anticonvulsant activity. The structures of the compounds were elucidated by elemental and spectral (IR, 1H NMR, 13C NMR and MS) analyses. Most of the test compounds demonstrated appreciable anticonvulsant activities in maximal electroshock seizure (MES) and subcutaneous pentylenetrtrazole (scPTZ) models.

scholarly journals Design, synthesis and anticonvulsant-analgesic activity of new N-[(phenoxy)alkyl]- and N-[(phenoxy)ethoxyethyl]aminoalkanols

MedChemComm ◽  
2017 ◽  
Vol 8 (1) ◽  
pp. 220-238 ◽  
Author(s):  
Anna Rapacz ◽  
Anna M. Waszkielewicz ◽  
Katarzyna Pańczyk ◽  
Karolina Pytka ◽  
Paulina Koczurkiewicz ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Anticonvulsant Activity ◽  
Seizure Threshold ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Design Synthesis ◽  
Electroshock Seizure Threshold

New aminoalkanols have been synthesized and evaluated for their anticonvulsant activity in maximal electroshock (MES), maximal electroshock seizure threshold (MEST) and pentylenetetrazol (PTZ) tests, and show promising activity.

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