1. The anticonvulsant potency of a series of structurally-dissimilar compounds which possess nanomolar affinities for high-affinity sigma binding sites was examined in the Mg2+-free model of epileptiform activity in rat hippocampal slices. Extracellular field potential recordings in the CA1 region were employed to examine the effects of test compounds on spontaneous epileptiform activity and mu...

OBJECTIVE The present study was designed to investigate the anticonvulsant potential of nickel which is shown to selectively block t-type calcium channels by using nickel choride on pentylenetetrazole (80 mg/kg) induced seizure activity model in mice. MATERIALS AND METHODS Seizures were assessed in terms of onset of Straub's tail phenomenon and onset of jerky movements of the whole body, conv...

The alcoholic extract of Achyranthes bidentata (AAB) has been studied for analgesic, anticonvulsant and CNS depressant activities in animal models. Analgesic activity was studied using acetic acid-induced writing test for assessing peripheral analgesic effect and tail immersion test for central analgesic effect. Anticonvulsant activity was performed by maximal electroshock induced convulsions; ...

Eighteen new 5-benzylidene-3-(4-arylpiperazin-1-ylmethyl)-2-thioxo-imidazolidin-4-ones were designed as hybrid structures from previously reported anticonvulsant compounds, synthesized and tested for anticonvulsant activity. Initial anticonvulsant screening was performed using the strychnine (2 mg/kg IP) potent generalized-induced seizure and pentylenetetrazole (PTZ) (60 mg/kg IP) acute clonic-...

We report here the synthesis and in vivo anticonvulsant/neurotoxicity activities of a series of compounds belonging to 2-aryl-4-arylidene-1-phenyl-1H-imidazol-5(4H)-one. The scaffold is based on the commonality of 5-membered lactam ring structures as successful anticonvulsant agents. The present compounds exhibited a range of anticonvulsant activity in pentylenetetrazole (PTZ)-induced seizure t...

The anticonvulsant effect of cannabinoids has been shown to be mediated through activation of the cannabinoid CB(1) receptor. This study was initiated to evaluate the effects of endogenously occurring cannabinoids (endocannabinoids) on seizure severity and threshold. The anticonvulsant effect of the endocannabinoid, arachidonylethanolamine (anandamide), was evaluated in the maximal electroshock...

The pro- and anticonvulsant effects of phencyclidine (1-[1-phenylcyclohexyl]piperidine HCl, PCP), a number of its analogues, and SKF 10047 were investigated in rats. The PCP analogues were compounds produced by substitutions for the phenyl and piperidine rings of PCP and were selected to elucidate the structure-activity relationships existing between PCP and its pro- and/or anticonvulsant effec...

Two guinea pig models were used to study the anticonvulsant potency of diazepam, midazolam, and scopolamine against seizures induced by the nerve agents tabun, sarin, soman, cyclosarin, O-ethyl S-(2-(diisopropylamino)ethyl)methylphosphonothioate (VX), and O-isobutyl S-(2-diethylamino)ethyl)-methyl phosphonothioate (VR). Animals instrumented for electroencephalogram recording were pretreated wit...

OBJECTIVES This article will review current data on the metabolism, interactions, methods of analysis, and adverse effects observed with the use of new anticonvulsant drugs. The role of the laboratory in the provision of therapeutic drug monitoring for these drugs is discussed. CONCLUSION Certain of the newer anticonvulsant drugs require therapeutic drug monitoring for their optimal use in th...

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...