New derivatives of 2-[2-(2-Chlorophenoxy)phenyl]-1,3,4-oxadiazole as candidates for agonistic effect on benzodiazepine receptors were synthesized. Conformational analysis and superimposition of energy minima conformers of the novel compounds on estazolam, a known benzodiazepine agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. In pharmacological evaluatio...

Erythrophleum ivorense is used traditionally for many ailments such as convulsion, swellings, pain and emesis. Therefore, this study aimed to investigate the anticonvulsant and sedative activities of extracts of Erythrophleum ivorense stem bark in mice. Anticonvulsant effect of the extracts was assessed using picrotoxin, pentylenetetrazole and strychnine-induced convulsion and sedative effect w...

Epilepsy is a neurological condition which is characterized by unprovoked seizures resulting from abnormal discharge of cerebral neurons and affecting at least 50 million people worldwide. There is continuing demand for new anticonvulsant agents as it has not been possible to control every kind of seizure with existing antiepileptic drugs. Moreover, conventional antiepileptic drugs exhibited un...

New 3-[(2,4-dioxo-1,3,8-triazaspiro[4.6]undec-3-yl)methyl]benzonitrile derivatives 8-37 were synthesized and their pharmacological activities were determined with the objective to better understand their structure-activity relationship (SAR) for anticonvulsant activity. All the compounds were evaluated for their possible anticonvulsant activity by maximal electroshock seizure (MES) and pentylen...

BACKGROUND AND PURPOSE Phytocannabinoids in Cannabis sativa have diverse pharmacological targets extending beyond cannabinoid receptors and several exert notable anticonvulsant effects. For the first time, we investigated the anticonvulsant profile of the phytocannabinoid cannabidivarin (CBDV) in vitro and in in vivo seizure models. EXPERIMENTAL APPROACH The effect of CBDV (1-100 μM) on epile...

Two novel 3-amino-5-(4-choloro-2-phenoxyphenyl)-4H-1,2,4-triazole derivatives were prepared and their anticonvulsant activity was measured by evaluation of the ability of these compounds to protect mice against convulsion induced by lethal doses of pentylenetetrazole (PTZ). Diazepam (Sigma) was considered as a positive control drug with anticonvulsant effect [ED50 = 1.2 (0.5-1.9) mg/Kg]. Amongs...

There are no reports on the effect of 7-nitroindazole (7-NI) on chemically-induced convulsions. Hence, in the present study, its (100 and 200 mg/kg) action was tested alone and in combination with phenobarbitone (20 mg/kg) and diazepam (0.25 mg/kg) on picrotoxin (PCT)-induced convulsions in rats. The changes produced by 7-NI on nitric oxide synthase (NOS) activity and nitric oxide (NO) concentr...

Background: Enhancement of cerebrocortical GABAergic inhibition is postulated as the main mechanism by which anesthetics inhibit seizures; however this has not been directly tested under controlled conditions. In this study we utilized the isolated cerebral cortex slice preparation and tested the anticonvulsant properties of three anesthetics with differing specificities for GABAergic activatio...

A comparison of the anticonvulsant and neurotoxic effects of cannabidiol (CBD), delta 9tetrahydrocannabinol, cannabinol and antiepileptic drugs (phenytoin, phenobarbital, carbamazepine, chlordiazepoxide, clonazepam, ethosuximide and trimethadione) was made in rats. Median effective potencies (ED 50 values) for maximal electroshock, audiogenic seizures and TD50 values for a rotor rod neurotoxici...

     New derivatives of 2-[2-(2-Chlorophenoxy)phenyl]-1,3,4-oxadiazole as candidates for agonistic effect on benzodiazepine receptors were synthesized. Conformational analysis and superimposition of energy minima conformers of the novel compounds on estazolam, a known benzodiazepine agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. In pharmacological eval...