• Bulletin of the Korean Chemical Society
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• v.32 no.2
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• pp.576-582
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• 2011

Various 2-amino-6-[3-(substituted phenyl)-5-phenyl-4,5-dihydropyrazol-1-yl]-4-(substituted phenyl)nicotinonitriles (3a-t) were designed and synthesized by clubbing two active anticonvulsant pharmacophores pyrazole and pyridine. All the synthesized compounds possessed the pharmacophoric elements essential for good anticonvulsant activity. The anticonvulsant screening was performed by maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) tests. Two compounds 3i and 3s showed significant anticonvulsant activity in both the screens with $ED_{50}$ values 17.5 mg/kg and 22.6 mg/kg respectively in MES screen and 154.1 mg/kg and 242.6 mg/kg respectively in scPTZ screen. They were also found to have no acute toxic effects in mice when tested at elevated doses.

• The Journal of Korean Medicine
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• v.25 no.1
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• pp.188-197
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• 2004

Objective and Methods : This study was performed to evaluate the anticonvulsant, antioxidant effect of modified formulas Korean traditional medicine Cheongsinhwadam-Jeon(CSHDJ). The extract of CSHDJ was administered (p.o.) to mice for 14 days in anticonvulsant and antioxidant tests. Results : The pretreatment of CSHDJ extract prohibited pentylenetrazol (PTZ)-induced convulsion. In PTZ-induced convulsion, lowered level of brain ${\gamma}$-aminobutyric acid(GABA) was restored normal state by the pretreatment of CSHDJ. Increased level of brain glutamic acid was lowered to normal state by CSHDJ, and increased activity of brain ${\gamma}-aminobutyric$ acid transaminase(GABA-T) was reduced to normal state by CSHDJ. In PTZ-induced convulsion, increased level of brain lipid peroxide was lowered to normal state by the pretreatment of CSHDJ. Increased activity of brain xanthine oxidase(XOD) was lowered by CSHDJ, and increased activity of brain aldehyde oxidase lowered to normal state by CSHDJ. In PTZ-induced convulsion, increased activities of superoxide dismutase(SOD) and catalase in brain were lowered by the pretreatment of CSHDJ, whereas increased level of glutathione and increased activity of gluthathione peroxidase in brain were not changed significantly. Conclusions : Above results suggest that CSHDJ has anticonvulsant, antioxidant effect. That seems to be strongly related with the levels of GABA, glutamate, lipid peroxide and the activities of GABA-T, XOD, aldehyde oxidase, SOD, catalase in brain tissue. From these results, CSHDJ could be applied to various convulsive disorders.

• Korean Journal of Pharmacognosy
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• v.23 no.1
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• pp.34-42
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• 1992

The analgesic, anticonvulsant and anti-inflammatory actives of leaves of Hedera rhombea Bean were evaluated. The methanol and butanol fractions showed considerable analgesic activity, but no anticonvulsant activities. Anti-inflammatory activity was found in the methanol, butanol and ether fractions by carrageenin induced edema test.

• Korean Journal of Pharmacognosy
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• v.27 no.1
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• pp.53-57
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• 1996

To elucidate the activities of Uncaria Ramulus et Uncus, which has been used as anticonvulsant and antihypertensive in oriental region, the methanolic extract and its fractions were applied to inhibition of convulsion onset. The ethyl acetate fraction showed dose-dependent inhibitory activity against pentylenetetrazole-induced seizure.

• Advances in Traditional Medicine
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• v.7 no.1
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• pp.46-50
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• 2007

Callus cultures of Convolvulus microphyllus Sieb. was induced on Murashige and Skoog's medium supplemented with 2,4-dichloro phenoxy acetic acid, 6-benzyl adenine, indole acetic acid and kinetin (1 ppm each). Methanolic extracts of whole plant, leaf, stem and leaf and stem calli were tested for anticonvulsant activity against standard drug phenytoin using maximal electroshock model on mice. It was observed that the animals treated with methanolic extracts of stem callus, leaf callus and whole plant (200 mg/kg, oral) showed significant protection against tonic convulsions induced by transcorneal electroshock. Anticonvulsant activity of methanolic extract of stem callus was comparable to that of standard drug phenytoin.

• The Journal of Pediatrics of Korean Medicine
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• v.18 no.2
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• pp.263-271
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• 2004

Objective : Epilepsy is a brain condition which causes a person to suddenly lose consciousness and sometimes to have fits. The etiologic factors of epilepsy are various, but most of cases are idiopathic. The purpose of this study is to report a pediatric patient with idiopathic epilepsy. Method : We treated him with herb medicine, acupucture and anticonvulsant. Then, we stopped administering anticonvulsant, and observed the progress of his condition. Result : We had good effect with oriental medical treatment on an epileptic who quitted taking anticonvulsant. Conclusion : We report the good results of oriental medicine on a pediatric patient with idiopathic epilepsy. And the further study is needed with more cases, longer duration and other tools.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1194-1201
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• 2004

Michael addition of certain nucleophiles on ${\alpha}$ , ${\beta}$-unsaturated ketones 1 led to the formation of adducts 2-7 as well as the reaction of arylidene derivatives with secondary amines afforded the amino compounds 9 and 11. Also, dialkylmalonates were treated with ${\alpha}$-cyano cinnamide to afford 13. On the other hand, double Michael cycloaddition of ethylcyanoacetate or tetrachlorophthalic anhydride to the suitable divinylketone were synthesized to produce 15-17. Selected compounds (13 and 6) were screened for muscle relaxant, anticonvulsant, and sedative activities using established pharmacological models. Their activities were compared with that of phenobarbital sodium taken as standard. Compound 6 was the most potent muscle relaxant while compounds 13a and 13c offered the highest anticonvulsant activity. Meanwhile compound 13c showed the highest potentiation of phenobarbital induced sleep in mice.

• YAKHAK HOEJI
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• v.32 no.1
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• pp.40-49
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• 1988

There is evidence that brain norepinephrine may play a role in experimentally induced seizures in animals. Thus the present experiments were undertaken in an attempt to explore the role of brain norepinephrine in anticonvulsant activity of clonazepam. 6-Hydroxydopamine was given to newborn rats and PTZ-induced seizures were tested $70{\sim}90$ days after birth and the rats were killed for determination of brain norepinephrine 8 days after the seizure test. Depletion of norepinephrine in the rat brain significantly potentiated the PTZ-induced convulsions and antagonized the effect of clonazepam on clonic seizures, tonic seizures and the number of seizures, but the latency to the seizure and the mortality has not been altered. However the 6-hydroxydopamine-induced antagonism of anticonvulsant action was surmountable by increasing the dose of clonazepam. These results show that brain norepinephrine may play an important role in seizure susceptability as well as in the anticonvulsant activity of clonazepam in rats.

• Bulletin of the Korean Chemical Society
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• v.32 no.3
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• pp.1011-1016
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• 2011

A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].

• Bulletin of the Korean Chemical Society
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• v.23 no.6
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• pp.917-921
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• 2002