• YAKHAK HOEJI
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• v.48 no.3
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• pp.182-188
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• 2004

This study aimed to synthesize new anticonvulsive agents as potential dual acting prodrugs. For the synthesis of ester or amide prodrug types, p-hydroxybenzaldehyde or valproic acid was coupled with clinically usable anticonvulsants or GABAmimetics with use of DCC/DMAP coupling methods. Also their anticonvulsive activities were evaluated.

• Archives of Pharmacal Research
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• v.26 no.10
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• pp.785-795
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• 2003

For the development of new anticonvulsive agents, GABAmimetics such as nipecotic acid, isonipecotic acid, ${\gamma}-aminobutyric$ acid (GABA), ${\gamma}-vinyl$ GABA (vigabatrin) and valproic acid were covalently coupled through an ester bond by a two-carbon linker chain as potential prodrugs and evaluated for their anticonvulsive activities.

• YAKHAK HOEJI
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• v.34 no.3
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• pp.171-179
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• 1990

The recombinant gamma-interferon (LBD-001) which was produced by yeast as host system was investigated on the pharmacological activities. This gamma-interferon exhibited potent inhibitory effect on adjuvant induced arthritis, but no effect on carrageenin induced paw edema in rats. It did not show any sedative, anticonvulsive, analgesic and hypothermic activities in animals. It also had no influences on isolated tracheal muscle and ileum of guinea pig, isolated uterus and fundus strip of rats, and on blood pressure and respiration in situ experiments of rabbits.

• Journal of Sasang Constitutional Medicine
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• v.2 no.1
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• pp.177-188
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• 1990

In order to investigate experimentally the clinical effects of Soumin Kamikop'ungsan (少陰人 加味祛風散) that was prescribed to cure the Wisuhanrihanbyung (胃受寒裡寒病) of Sumin (少陰人) the author experimented various activities of mixed extract from the Sournin Kamikop'ungsan by the method prescribed in the experimental part. The results of the studies were summerized as follows: 1. Analgesic effects by acetic acid and Randall-Sellito experimental method were noted. 2. Anticonvulsive effect to strychnine was noted. 3. The sedation effects by the unbalanced effects of spontaneous momentum by wheel cage method, muscle relaxing action by Rotor rod method were noted. 4. A prolongation of anesthetic time by Thiopental-Na on the mice was noed. 5. The expansion of blood vessels by relaxation of smooth muscle was noted. According to the above results, results of Soumin Kamikop'ungsan on oriental medical references were consistent with the actual experimental results.

• Korean Journal of Pharmacognosy
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• v.18 no.1
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• pp.14-25
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• 1987

The effects of the water extract of 'Banhahubagtang', the combined herbal medicine, on the low esophageal sphincter, stomach, small intestine and CNS were investigated, and the results were as follows: The hexobarbital induced sleeping time was prolonged in female mice. The convulsion induced by electric shock was suppressed and analgesic action was recognized in mice. The extract inhibited intestinal propulsion of barium sulfate in mice. The extract inhibited free acid secretion and showed remarkable suppression of gastric ulcer in rats. Relaxation induced by isoproterenol and norepinephrine in low esophageal sphincter(L.E.S.) of rabbit was potentiated by addition of the extract. In conclusion, the Banhahubagtang exhibited anticonvulsive, sedative and L.E.S. inhibitory activities. These experimental results might indicate to be coincided with the indications for neuro-esophago-stenosis, esophagitis, esophagia, gastralgia, and neurosis which are well referred to the literature of oriental medicine.

• The Journal of Pediatrics of Korean Medicine
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• v.10 no.1
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• pp.245-263
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• 1996

In order to investigate the effects of Yangsymtang on the activities of central nervous system, we observed the effects on convulsions induced by pentylenetetrazole, strychnine and picrotoxin. The sedative those on spontaneous motor activity and by rota rod method, the those on sleeping time induced by barbiturate and the alleviative those on pain induced by acetic acid and hind limb pressure also were analyzed. The results were as follows: 1. The solid extracts of Yangsymtang showed no anticonvulsive effects on convulsions induced by pentylenetetrazole, strychnine and picrotoxin. 2. As to the sedative effects by rota rod method, th solid extracts of Yangsymtang were recognized as significance(P<0.01). 3. The sleeping time induced by thiopental sodium was not prolonged by the oral administration of the solid extracts of Yangsymtang. 4. The oral administration of Yangsymtang did not influenced the sleeping induced by pentobarbital sodium significantly. 5. As to the effects on spontaneous motor activity, the oral administration of Yangsymtang made spontaneous motor activity decrease significantly(P<0.05). 6. The oral administration of Yangsymtang was significant on pain induced by acetic acid(P<0.001). 7. As to alleviative effects on pain induced by hind limb pressure. The solid extracts of Yangsymtang were not significant.

• Animal cells and systems
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• v.13 no.4
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• pp.357-362
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• 2009

Hesperidin, the most abundant polyphenolic compound found in citrus fruits, has been known to possess neuroprotective, sedative, and anticonvulsive effects on the nervous system. In a recent electrophysiological study, it was reported that hesperidin induced biphasic change in population spike amplitude in hippocampal CA1 neurons in response to both single spike stimuli and theta-burst stimulation depending on its concentration. However, the precise mechanism by which hesperidin acts on neuronal functions has not been fully elucidated. Here, using whole-cell patch-clamp recording, we revealed that hesperidin did not affect excitatory synaptic activities such as basal synaptic transmission and theta-burst LTP. Moreover, in a current injection experiment, spike number, resting membrane potential and action potential threshold also remained unchanged. Taken together, these results indicate that the effects of hesperidin on the neuronal functions such as spiking activity might not be attributable to either modification of excitatory synaptic transmissions or changes in membrane excitability in hippocampal CA1 neuron.

• Biomolecules & Therapeutics
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• v.19 no.3
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• pp.342-347
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• 2011

In the present study, the anticonvulsant effects of Artemisia capillaris Herba (AC) and its major constituent, esculetin (ECT), were tested and the mechanism studied. Locomotion, Myorelaxation, motor coordination and electroshock seizure experiment were conducted in mice. To identify the anticonvulsant mechanism effect of this drug, chemical-induced seizure in mice and the ionic movement in neuroblastoma cells were also observed. The ethanol extract of AC was orally administered to mice 30 min. prior to testing and ECT was intraperitoneally injected. AC and ECT treatment did not change locomotor activities as well as activities on the rota-rod, which indicates that they did not cause a sedative and myorelaxation effect. AC and ECT treatment increased threshold of convulsion induced by electroshock. AC treatment also inhibited convulsion induced by pentylenetetrazole. In the case of strychnine however, only high dose of AC treatment inhibited convulsion. AC and ECT treatment increased the $Cl^-$ influx into the intracellular area in a dose-dependent manner. On the other hand, bicuculline, a GABA antagonist, inhibited the $Cl^-$ influx induced by AC and ECT. These results indicate that ECT induces the anticonvulsive effect of AC extract through the GABAergic neuron.

• Journal of Oriental Neuropsychiatry
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• v.13 no.2
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• pp.195-211
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• 2002

Gagamguibitang, a composite Korean medicinal drug prescribed by us, was evaluated for its sedative effects by measurements of potentiation on pentobarbital-induced sleeping time, anticonvulsive activities in animal model, inhibitory effect on GABA transaminase activity, and antioxidative activities in vitro- and/or in vivo assay. The results were summerized as follows : 1. Gagamguibitang showed about 2-fold prolongation of pentobarbital-induced sleeping time compared to the control group after administration(p.o) with 2.0g/kg of mice body weight. 2. Gagamguibitang strongly lengthened onset time of pentylenetetrazole-induced convulsion, shortened the duration of convulsion and diminished the lethality after treatment(p.o) with 1.0g/kg of mice body weight. 3. Gagamguibitang inhibited dose-dependently the brain GABA transaminase activity in vitro compared to the control group and in vivo compared to the pentylenetetrazole-treated group. 4. Gagamguibitang inhibited effectively brain lipid peroxidation by 45.8% at a dose of l0mg/ml in vitro and by 47.5% after oral treatment with 0.5g/kg of mice body weight in vivo assay. 5. Gagamguibitang exhibited a potent scavenging activity on DPPH radical in a dose-dependent manner with ca. 92% activity at l0mg/ml. As a result, Gagamguibitang can be useful for the effective sedative drug in clinical application.

• The Korean Journal of Physiology and Pharmacology
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• v.3 no.3
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• pp.237-244
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• 1999

Magnesium ion is known to selectively block the N-methyl-D-aspartate (NMDA)-induced responses and to have anticonvulsive action, neuroprotective effect and antinociceptive action in the behavioral test. In this study, we investigated the effect of $Mg^{2+}$ on the responses of dorsal horn neurons to cutaneous thermal stimulation and graded electrical stimulation of afferent nerves as well as to excitatory amino acids and also elucidated whether the actions of $Ca^{2+}$ and $Mg^{2+}$ are additive or antagonistic. $Mg^{2+}$ suppressed the thermal and C-fiber responses of wide dynamic range (WDR) cell without any effect on the A-fiber responses. When $Mg^{2+}$ was directly applied onto the spinal cord, its inhibitory effect was dependent on the concentration of $Mg^{2+}$ and duration of application. The NMDA- and kainate-induced responses of WDR cell were suppressed by $Mg^{2+}$, the NMDA-induced responses being inhibited more strongly. $Ca^{2+}$ also inhibited the NMDA-induced responses current-dependently. Both inhibitory actions of $Mg^{2+}$ and $Ca^{2+}$ were additive, while $Mg^{2+}$ suppressed the EGTA-induced augmentation of WDR cell responses to NMDA and C-fiber stimulation. Magnesium had dual effects on the spontaneous activities of WDR cell. These experimental findings suggest that $Mg^{2+}$ is implicated in the modulation of pain in the rat spinal cord by inhibiting the responses of WDR cell to noxious stimuli more strongly than innocuous stimuli.