Anticonvulsant activity of N-(p-aminobenzoyl)-1,2,3,4- tetrahydro-quinoline (NTQ), a newly synthesized ameltolide analog, was investigated with regards to efficacy and toxicity in mice. Additionally, its effect on NMDA receptors was also performed on NR1a/NR2B expressed in Xenopus oocytes. NTQ, given intraperitoneally, was able to protect the animals in both maximal electroshock seizure and pen...

GABA-potentiating neuroactive steroids such as pregnanolone have potent protective effects in the pentylenetetrazol seizure test. We sought to determine if tolerance develops to the anticonvulsant activity of pregnanolone with chronic administration. Mice were treated with two daily injections of a 2 x ED50 dose of pregnanolone (25 mg/kg, i.p.) for 7 days. On the day after the chronic treatment...

introduction: jugulans regia (jugulandaceae), astragaus hamosus (papilionaceae), crocus pallasii subsp. haussknechtii boiss. (iridaceae) and cassia angustifolia vahl. (caesalpinaceae) have been suggested as antiepileptic remedies in traditional medicine of iran. the possible anticonvulsant effect of the hydroalcoholic extract of the leaves of j. regia, fruits of a. hamosus, corm of c. haussknec...

Some novel fluorinated quinazolines (5a-j) were designed and synthesized to be evaluated for their anticonvulsant activity and their neurotoxicity. Structures of all newly synthesized compounds were confirmed by their infrared (IR), mass spectrometry (MS) spectra, ¹H nuclear magnetic resonance (NMR), 13C-NMR, and elemental analysis (CHN). The anticonvulsant activity was evaluated by a subcutane...

     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...

     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...

Isatin derivatives are one of most potent anticonvulsant agent of natural origin. It has display potent anticonvulsant effect in a wide variety of preclinical anticonvulsant models. Till date various isatin derivatives have been synthesized and evaluated for anticonvulsant activity. This review is an attempt to compile the medicinal chemistry of various synthesized isatin analogs. Isatin and it...

In the recent years there has been an increased interest in the pyridazinone ring system. Many investigations indicated that the presence of at least one aryl group, one or two electron donor atoms and/or an NH group in a special spatial arrangement is necessary for anticonvulsant activity. Many investigations indicated that the presence of at least one aryl group, one or two electron donor ato...

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...

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...