• Biomolecules & Therapeutics
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• 제10권2호
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• pp.89-98
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• 2002

In this study general pharmacological profiles of KI-60606 on the central nervous system, the cardiovascular system and the other organs were investigated. The dosages given were 0,5, 10 and 25 mg/kg and drugs were administered intravenously. The animals used for this study were mice, rats, cats and guinea pigs. KI-60606 showed no effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital-induced hypnosis time, body temperature, analgesic activity, anticonvulsant activity and contraction of nictitating membrane in cats. Furthermore KI-60606 showed no effects on blood pressure, heart rate, LVP (left ventricular peak systolic pressure), LVEDP (left ventricular end diastolic pressure), LVDP (left ventricular developing pressure), DP(double product), CFR(coronary flow rate), smooth muscle contraction using guinea pig ileum and gastric secretion at all dosage tested except the increase of gastrointestinal transport and urinary $K^+$ excretion.

• 생약학회지
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• 제12권4호
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• pp.203-207
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• 1981

The acute toxicity and sedative activity of flavonoids and saponin isolated from Zizyphus seeds have been evaluated in mice. All the compounds elicited potentiation of hexobarbital-induced hypnosis, inhibition of ladder-climbing and caffeine-induced hyperactivity. Swertisin was the most potent of all flavonoids tested. The potency of saponin in these tests was found to be higher than that of swertisin. The activities in rotarod test and electroshock seizure test, on the other hand, were relatively weak or nil. From these findings it was suggested that flavonoids and saponin from Zizyphus seeds have neuroleptic activity without anticonvulsant or muscle relaxant activity accompanied by neurological deficit.

• Biomolecules & Therapeutics
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• 제7권2호
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• pp.170-177
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• 1999

PEG-hemoglobin SB1 (SB1), which is a hemoglobin-based oxygen carrier, is intended to use as a safe blood substitute against brain ischemia and stroke. The general pharmacological profiles of SB1 were studied. The doses given were 0, 5, 10, 20 ml/kg and drugs were administered intravenously. The animals used for this study were mouse, rat and guinea pig. SB1 showed no effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital sleeping time, anticonvulsant activity, analgesic activity, blood pressure and heart rate, left ventricular peak systolic pressure, left ventricular end diastolic pressure, left ventricular developing pressure, double product, heart rate, coronary flow rate, smooth muscle contraction using guinea pig ileum, gastrointestinal transport, gastric secretion, urinary volume and electrolyte excretion at all doses tested except the decrease of body temperature. These findings demonstrated that SB1 possesses no general pharmacological effects at all doses tested.

• Biomolecules & Therapeutics
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• 제10권4호
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• pp.258-267
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• 2002

In this study the general pharmacological profiles of AS6 on the central nervous system, cardiovascular and the other organs were investigated. The dosages given were 0, 250, 500 and 1000 mg/kg and drugs were orally administered. The animals used for this study were mice, rats and guinea pigs. Significant increases (p<0.01) in the charcoal transport capacity were observed at the high dose of 1000 mg/kg and significant increases in retardation of pain threshold were observed in the test using acetic acid in all dosed animals. However, AS6 showed no noticeable effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital-induced sleep time, body temperature, analgesic activity in the test using hot plate method and anticonvulsant activity. Furthermore no noticeable effects were observed in cardiovascular functions in the isolated rat heart, contraction and relaxation of the smooth muscle in the isolated guinea ileum, gastric secretion and renal function.

• 생약학회지
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• 제24권3호
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• pp.231-234
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• 1993

Neuropharmacological profile of Humulus lupulus (hop) extract was studied in mice. At doses above 100 mg/kg(i.p.), it decreased spontaneous locomotor activity and raised the nociceptive threshold in the hot-plate test. At doses above 250 mg/kg (i.p.), it increased pentobarbital-induced sleeping time and produced muscle relaxant effect. At the dose of 500 mg/kg, anticonvulsive effect against pentylenetetrazole-induced convulsion and hypothermic effect was observed.

• 동의신경정신과학회지
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• 제15권1호
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• pp.101-119
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• 2004

Ginseng Radix Alba and Cyperi Rhizoma were investigated for their anti-depressant effects. For this purpose, forced-swimming test, tail suspension test, hot plate test, reserpine-induced hypothermia, aggressive behavior test were performed. In addition, the brain content of 5-hydroxyindoleacetic acid(a metabolite of serotonin), the monoamine oxidase activity, anticonvulsant effect, sleep enhancement effect were determined. The results are as follows: In the forced swimming test, Ginseng Radix diminished the duration of immobility by 45.5% compared to the control group, while Cyperi Rhizoma showed weaker effect (12.4% reduction) at 2g/kg. In the tail suspension test, the effect of Ginseng Radix(43.7% reduction) are also better than that of Cyperi Rhizoma(15.6% reduction) at 2g/kg. In the hot plate test, Ginseng Radix showed no difference as compared to control, while Cyperi Rhizoma increased the jump latency time by about 25% after administration for 10 days. In the reserpine-induced hypothermia test, both drugs slowly dropped the body temperature compared to the control group, especially the rate of hypothermia of Ginseng Radix was 24.0% at 1g/kg. In the aggressive behavior test, both drugs delayed the onset time, decreased the duration and frequency, of which effects were better in Cyperi Rhizoma. The content of 5-hydroxyindoleacetic acid in mice brain was slightly increased in Ginseng Radix, while Cyperi Rhizoma increased its level almost to the control group. Both drugs inhibited the monoamine oxidase activity in a dose-dependent manner, but the effect(51.2%) of Cyperi Rhizoma was more potent than the effect(11.8%) of Ginseng Radix. In the pentobarbital-induced sleep test, Cyperi Rhizoma exhibited no significant difference against the control group, while Ginseng Radix showed about two-fold enhancement at 2g/kg. The anticonvulsant effect of both drugs delayed the onset time, shortened the duration of convulsion and diminished the lethality, but Ginseng Radix were better than Cyperi Rhizoma.

• Biomolecules & Therapeutics
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• 제5권4호
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• pp.325-330
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• 1997

Methanol extract of G. elata inhibited the binding of [/sup 3/H]Rol5-1788, a selective benzodiazepine receptor antagonest, to benzodiazepine receptor of rat cortices. Saturation experiments followed by Scatchard analysis of the results showed that the inhibition of [sub 3/H]Ro15-1788 binding by G. dlata. appeared to be com-petitive. These competitive inhibiton of the butanol fraction was observed to be higher than the methanol extract. Methanol extract of G. efara inhibited a [sub 3/H]flunitrazepam, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of [/sub 3/H]flunitrazepam binding by G. elata, and these "positive GABA shift" supported the strong possibility of agonestic activity to benzodiazepine receptor Butanol fraction was observed to be higher than crude extract by methanol in an agonistic activity to benzodiazepine receptor, furthermore enhanced the binding of [sub 3/H]SR95531 to GABA receptor. Butanol fraction of G. elata significantly diminished the pentylenetetrazole-induced lethality of mice. From these results, it can be concluded that substance or substances with neurochemical properties characteri- stic of a benzodiazepine receptor agonist may be important components, and contribute to the anticonvulsant property of G. elata.

• Archives of Pharmacal Research
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• 제22권2호
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• pp.219-224
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• 1999

In our search for the anticonvulsant consitutent of Gastrodia elata repeated column chromatographies guided by activity assay led to isolation of an active compound, which was identified as gastrodin on the basis of spectral data. Brain succinic semialdehyde dehydrogenase (SSADH) was inactivated by preincubation with gastrodin in a time-dependent manner and the reaction was monitored by absorption and fluorescene spectroscopic methods. The inactivation followed pseudo-first-order kinetics with the second-rate order constant of $1.2{\times}10^{3} M^{-1} min^{-1}$. The time course of the reaction was significantly affected by the coenzyme NAD^{+}$, which affected complete protection against the loss of the catalytic activity, whereas substrate succinic semialdehyde failed to prevent the inactivation of the enzyme. It is postulated that the gastrodin is able to elevate the neurotransmitter GABA levels in central nervous system by inhibitory action on one of the GABA degradative enzymes, SSADH.

• Toxicological Research
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• 제13권4호
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• pp.349-352
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• 1997

Scopoliae rhizoma is a perennial herb which has a similar effect with atropine on the cardiovascular system. It is also known to have a seditive and anticonvulsant activity on the central nerve system. In order to evaluate an acute toxicity of Scopoliae rhizoma, the present study was performed after administration the Scopoliae rhizoma prepared by both decoctional and frozen dried extract through three different routes (oral; 5,000 mg/kg, intraperitoneal; 2,000 mg/kg, subcutaneous; 5,000 mg/kg) to the female ICR mice. In the group treated intraperitoneally with a frozen dried extract, abnormal clinical signs such as decreased activity, crouch, potosis and abnormal walking were observed for 40 rain after administration. With regard to WBC, decreased number of lymphocyte and increased number of monocyte and granulocyte were also observed in the animals received intraperitoneally with Scopoliae rhizoma extract. Taken together, what toxicity of Scopoliae rhizoma was shown differently depending on its type for administration may be resulted in the differency of administered dose. The results provided here support a pharmacological and toxicological consideration for its clinical use in the regard of oriental medicine.

• Journal of Life Science
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• 제9권1호
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• pp.81-83
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• 1999

2,4-Disubstituted nortropinone derivatives anticipated anticonvulsant activity were respectively synthesized by the reaction of N-substituted nortropinones, ethanol, 5N-NaOH and benzaldehyde ({TEX}$R_{1}${/TEX}CHO)