• Biomolecules & Therapeutics
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• 제11권1호
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• pp.51-57
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• 2003

General pharmacological properties of ADP, a new pharmaceutical composition, which contains a mixed water extract obtained from the mixture of Phellodendron cortex (Phellodendron amurense) and Anemarrhena rhizoma (Anemarrhena asphodeloides), as the active ingredients, were investigated in experimental animals administering orally and in vitro test system. ADP had no influences on general behavior, pentobarbital sleeping time, spontaneous motor activity, motor coordination of mice, normal body temperature, chemoshock produced by pentylenetetrazole and writhing syndromes induced by 0.8% acetic acid at the dose of 150 and 1500 mg/kg. Gastric secretion of rats and intestinal motility of mice were not also influenced by the administration of ADP at doses of 150 and 1500 mg/kg, with the exception of the significant decrease of free HCI concentration at a dose of 1500 mg/kg in rats. ADP (150 and 1500 mg/kg) did not alter mean arterial blood pressure and heart rate in conscious rats. ADP given to anesthetized rats showed no effect on respiratory rate at the same doses. In in vitro experiments, ADP at the concentration of 150 mg/L did not show direct effect and inhibitory or augmentative action on histamine- or acetylcholine-induced contractions in the isolated ileum of guinea-pig. Taken together, these results indicate that ADP does not induce any adverse effects in experimental animals.

• Journal of Ginseng Research
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• 제33권1호
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• pp.48-54
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• 2009

Epileptifrom discharges were induced in the telencephalon of the adult zebrafish via perfusion with pentylenetetrazole (PTZ), bicuculline methiodide, kainic acid-treated artificial cerebrospinal fluid (aCSF), and $Mg^{2+}$-free aCSF. Ginseng total saponin [GTS ($50{\mu}g/ml$)] was shown to attenuate the occurrence rate of epilpetiform discharges by 50-75%, compared to the control. Ginsenoside $Rg_1$ ($130{\mu}M$) reduced the epileptiform discharges in the isolated telencephalon and delayed the occurrence of behavioral seizures observed from the adult zebrafish placed in the PTZ (10 mM)-containing aquarium water. However, Re was not effective in the suppression of epileptiform discharges and behavioral seizures. These results indicate that $Rg_1$ may be useful in the control of epileptiform discharges and effective in controlling behavioral seizures, and that the zebrafish can be used as a model animal for the testing of potential anticonvulsant drugs.

• Bulletin of the Korean Chemical Society
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• 제32권2호
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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.

• 동의생리병리학회지
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• 제16권3호
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• pp.567-571
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• 2002

In order to prove the sedative, anticonvulsive effects of Incenses and to identify the effect of this medicine to cerebral glutamic acid and GABA density in experimental animal. we used Incense which was made of traditional herb medicines. We also examined what kind of material is to be involved in biosynthesis of these elements. In addition we experimented to find out synthesis of active GABA-T. Incenses were inhaled 8 hours a day for 4 weeks to mice. Finally we have following results. On the convulsion induced by pentylenetetrazole(PTZ), Incenses showed significant anticonvulsive effect. Density of glutamic acid in brain was significantly decreased. On the contrary, density of GABA was significantly increased. The Activity of GABA- T in brain was significantly reduced. The quantity of lipid peroxide in the brain was significantly decreased. Activity of xanthine oxidase and aldehyde oxidase were significantly reduced in brain. From the above results, we confirmed that Incenses decreased the density of glutamic acid, increased GABA density and decreased the activity of GABA- T in brain. For the convulsion which was induced by PTZ, Incenses showed significant anticonvulsive effect. With this we can recognize that Incenses had ability to control the quantity of lipid peroxide in brain. In the conclusion, Incenses has significant anticonvulsive effect, so I strongly recommend to prescribe Incenses to treat convulsive disorder like epilepsy.

• Biomolecules & Therapeutics
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• 제12권3호
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• pp.175-178
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• 2004

Rutaecarpine is one of quinazolinocarboline alkaloids found in Evodia rutaecarpa, a Rutaceous plant and it has shown various biological effects including antiinflammation. However, the effect of rutaecarpine on nervous system was not reported yet. In this study we investigated the general pharmacology of rutaecalpine on the central nervous system. Rutaecapine (4O and 400 mg/kg) did not change chemoshock induced by pentylenetetrazole. However, oral administration of rutaecarpine altered motor coordination examined by rotarod test, pentobarbital-induced sleeping time and acetic acid-induced writhing syndrome in mice at the doses of 40 and 400 mg/kg. Rutaecarpine also induced hypothermia in mice at both doses. The results suggest that rutaecapine possesses neuromodulating activities on central nervous system in addition to the various biological effects on the Periphery.

• Biomolecules & Therapeutics
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• 제4권4호
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• pp.385-390
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• 1996

General pharmacological properties of urinary trypsin inhibitor (UTI) following intravenous administration of 1,000,000 units/kg were examined in terms of effects on central nervous system, cardiovascular system, respiratory system, gastrointestinal system in mice, rats and rabbits. Administration of UTI (1,000,000 units/kg, iv) had no effect on central nervous system; no influences on pentobarbital sleeping time, spontaneous activity, normal body temperature, chemoshock produced by pentylenetetrazole solution, writhing syndromes induced by 0.6% acetic acid solution, and motor coordination of mice. The administration of UTI (1,000,000) units/kg, iv) in rats had no effect on systolic blood pressure and pulse rate. UTI (500,000 units/kg, iv) given to anesthetized rabbits showed no effect on respiratory rate. However, it showed significant elevation of respiratory rate at the concentration of 1,000,000 units/kg. Gastric secretion of rat and intestinal motility of mice were not influenced by the dose of 1,000,000 units/kg. In terms of autonomic nervous system, the material did not show direct effect and inhibitory or augmentative action of histamine- or acetylcholine-induced contraction at the concentration of 2,000 units/ml in the isolated ileum of guinea pig.

• Biomolecules & Therapeutics
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• 제5권4호
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• pp.412-418
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• 1997

General pharmacological properties of AG 60 (mixture of acriflavine and guanosine (1:1, w/w)), which has anticancer effect, following intramuscular administration were examined in terms of effects on central nervous system, gastrointestinal system, cardiovascular system, respiratory system and autonomic nervous system in mice, rats, guinea-pigs and rabbits. AG 60 at the dose of 15 mgtg had no influences on pentobarbital sleeping time, spontaneous motor activity, chemoshock produced by pentylenetetrazole solution, writhing syndromes induced by 0.8% acetic acid solution, and motor coordination of mice. However, AG 60 at the dose of 7.5 and 15 mg/kg caused significant decrease of normal body temperature 1 and/or 2 h after the administration. No influence on body temperature was observed at 3.75 mg/kg in mice. Gastric secretion of rat and intestinal motility of mice were not influenced by the dose of 15 mg/kg. In terms of autonomic nervous system, AG 60 did not show direct effect and inhibitory or augmentative action of histamine- or acetylcholine-induced contractions at the concentration of 5 mg/L in the isolated ileum of guinea-pig. The administration of 15 mg/kg of AG 60 did not affect mean arterial blood pressure and heart rate in rat. AG 60 (15 mg/kg) given to anesthetized rabbits showed no effect on respiratory rate.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.495-501
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• 2004

A series of N-substituted-1,3-isoindolinedione derivatives (2-16) were synthesized for the purpose of defining the effect of N-substitution on the anticonvulsant activity of these derivatives. The target compounds (2-16) were obtained by condensation of phthalic anhydride with the corresponding amine derivative. The structures of the synthesized derivatives (2-16) were confirmed by means of IR, $^1$H-NMR, $^{13}$ C-NMR, MS and elemental analyses. The anticonvulsant activity of all compounds (2-16) were evaluated by subcutaneous pentylenetetrazole seizure threshold test at doses of 0.2, 0.4 and 0.8 mmol/kg compared with sodium valproate as a positive control. Their neurotoxicity were determined by the rotorod test. Many of the present series of compounds showed good anticonvulsant activity at the tested doses, as compared to sodium valproate. Three of them (4, 6 and 11) exhibited 100 % protection against convulsions, neurotoxicity and death at all tested doses. Out of the series, two compounds (12 and 13) were completely inactive with 100% mortality. 3-(p-chlorophenyl)-4-(1 ,3-dioxo-2,3-dihydro-1 H-2-isoindolyl) butanoic acid derivative (11) has emerged as the most active compound which is 20 times more active than valproate with ED$_{50}$ 8.7, 169 mg/kg; TD$_{50}$ 413, 406 mg/kg and PI 47.5, 2.4. The results revealed the importance of the combination of baclofenic and phthalimide moieties (compound 11) as a promising anticonvulsant candidate.

• Journal of Ginseng Research
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• 제18권3호
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• pp.165-174
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• 1994

To investigate the significant indicators Improving the undisturbed memory in animal behavior, we employed several behavioral methods (learning, relearning in radial maze, and active avoidance) with ginseng components. Results showed that the repeated intranasal administration of $Rb_1$ and total saponins from Korean red ginseng induced direct effects on the brain mechanisms in rats, and improved the spatial memory during the learning, relearning and retention in the 12-arm radial maze test. The intranasal treatment of the total saponins also effectively improved the disturbed memory (amnesia) by pentylentetrazole, and simultaneously protected the brain by decreasing the severity of motor epileptic seizures. The intraperitonial administration of polysaccharide fraction of Korean red ginseng could improve avoidance behavior (amount of the total ecapes) in the active-avoidance test. In addition, local changes of the temperature and resistance of skin observed after Rb, administration were suggested to reflect some action of sympathetic nerve Key words Memory, intranasal administration, pentylenetetrazole, Korea red ginseng.

• 생명과학회지
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• 제16권1호
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• pp.156-161
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• 2006

The essential oil of Nardostachys jatamansi (Valerianaceae), which has been used for a long time in aroma therapy, was investigated after inhalation or oral administration for its analgesic effect, anticonvulsant action, hypnotic effect and in vitro inhibitory activity on monoamine oxidase. This fragrance oil showed a significant analgesic effect in the phenylquinone-induced .writhing test, suppressed the convulsion induced by pentylenetetrazole and lengthened the pentobarbital-induced sleeping time in a time-dependent manner after fragrance inhalation or dose-independently by oral administration. Its inhibitory activity on monoamine oxidase was remarkable, showing $49.4\%$ inhibition at a concentration of 5.0 mg/ml. Six new terpenes with seven known compounds were detected by our GC-MS analytical conditions used. As a result, the essential oil fragrance of Nardostachys jatamansi would be clinically useful for a sedative by either inhalation or oral administration.