• YAKHAK HOEJI
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• v.27 no.4
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• pp.283-287
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• 1983

In order to search more active and less toxic central nervous depressants, piperic acid amides were synthesized by condensation of piperonal with crotonic acid amides. The bioassay results revealed that, among the compounds synthesized, the piperonic acid methylamide and ethylamide exhibited potent protective activity against strychnine-induced convulsion.

• YAKHAK HOEJI
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• v.27 no.4
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• pp.289-293
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• 1983

Twelve new N-piperoyl amino acids were synthesized by acylation of amino acids with piperoylchloride in order to develop the new central nervous depressants. Silylation of the carboxylic group of amino acids not only precluded side reactions but-also facilitated acylation at room temperature without catalysts. The acute toxicity of all the synthesized compounds were lower than that of piperine itself, whereas they showed strong protective effect against the strychnine-induced mortality.

• YAKHAK HOEJI
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• v.29 no.5
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• pp.253-259
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• 1985

In order to search a more active and safer compound, piperine derivatives with substituents in piperidine residue were synthesized and evaluated on CNS depressant activity. N-Piperoyl-2-methylpiperidine (I) and N-piperoyl-3-methylpiperidine (II) were potent in strychnine-induced convulsion. Compound I and N-piperoyl-3-hydroxypiperidine (IX) exhibited a potent inhibitory effect againt pentetrazoleinduced convulsion and a significant prolongation effect of hexobarbital-induced sleeping time. The hydroxy derivatives were more toxic than the methyl derivatives.

• The Korean Journal of Pharmacology
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• v.18 no.1
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• pp.17-22
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• 1982

Zizyphus seed(Zizyphus vulgaris Lamark var. Spinosus Bunge) has long been used as hypnotics and sedatives in oriental medicine, and it is reported that the Zizyphus seed elicited a variety of pharmacologic actions besides CNS depression. Present study was undertaken to investigate the effects of Zizyphus seed on the central nervous system and on the blood pressure. The effect of Zizyphus seed on the central nervous system was measured by the influence of thiopental sleeping time and by inhibition of chemical convulsion (strychnine and pentylenetetrazol induced). Blood pressure changes by Zizyphus extract and its mode of action were investigated. The ground Zizyphus seed was extracted with hexane and methanol, consecutively and the supernatants were discarded. The precipitate was re-extracted with distilled water and the supernatant was evaporated to a dark-brownish sticky liquid, which was used as Zizyphus seed extract in this study after dissolving in saline prior to experiment. The results are as follows. 1) Zizyphus seed extract caused marked prolongation of the thiopental sleeping time in mice. 2) The chemical convulsion by strychnine and pentylenetetrazol, and the mortality by them in chicks were not affected by pretreatment of Zizyphus seed extract. 3) Zizyphus seed extract produced transient fall of blood pressure in the cat, and this hypotentive effect was blocked partially by atropine but not affected by bilateral vagotomy and/or hexamethonium, nor propranolol and, chlorpheniramine and/or cimetidine. With the above results, it may be suggested that the water extract of Zizyphus seeds contains components producing CNS depression and hypotension. Furthermore it is felt that the cholinergic effect, but not the adrenergic or histaminergic, is partly responsible for the hypotensive effect of Zizyphus seed extract.

• The Korean Journal of Zoology
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• v.32 no.1
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• pp.34-39
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• 1989

Ouabain, strychnine sulfate, caffeine sodium benzoate and chlorpromazine hydrochloride were introduced intraperitoneally into male mice for 7, 14 and 21 days to induce the changes in the relative percentages of lactate dehydrogenase isozymes. The five isozymes in brain, heart and kidney tissues were electrophoresed on cellulose acetate strip and subjected to densitometry. Ouabain caused a drastic increase of B$_4$isozymes only in brain tissues. The two stimulants altered the relative percentages of $A_4$and B$_4$isozymes conspicuously in brain tissues, whereas virtually no redistributions of five isozymes were occurred by the depressant except B$_4$isozymes in brain and heart tissues. On the basis of these observations, it might be suggested that the changes in intracellular concentration of sodium and calcium ions are not the cause of the isozyme redistributions and that Organization of plasma membrane could be one of the factors involved in the tissue specificity of lactate dehydrogenase isozymes in vertebrates.

• The Korean Journal of Physiology and Pharmacology
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• v.24 no.5
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• pp.433-440
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• 2020

The substantia gelatinosa (SG) of the trigeminal subnucleus caudalis (Vc) is the first relay site for the orofacial nociceptive inputs via the thin myelinated Aδ and unmyelinated C primary afferent fibers. Borneol, one of the valuable time-honored herbal ingredients in traditional Chinese medicine, is a popular treatment for anxiety, anesthesia, and antinociception. However, to date, little is known as to how borneol acts on the SG neurons of the Vc. To close this gap, the whole-cell patch-clamp technique was applied to elucidate the antinociceptive mechanism responding for the actions of borneol on the SG neurons of the Vc in mice. In the voltage-clamp mode, holding at -60 mV, the borneol-induced non-desensitizing inward currents were not affected by tetrodotoxin, a voltage-gated Na⁺ channel blocker, 6-cyano-7-nitro-quinoxaline-2,3-dione, a non-N-methyl-ᴅ-aspartate (NMDA) glutamate receptor antagonist and DL-2-amino-5-phosphonopentanoic acid, an NMDA receptor antagonist. However, borneol-induced inward currents were partially decreased in the presence of picrotoxin, a γ-aminobutyric acid (GABA)_A receptor antagonist, or strychnine, a glycine receptor antagonist, and was almost suppressed in the presence of picrotoxin and strychnine. Though borneol did not show any effect on the glycine-induced inward currents, borneol enhanced GABA-mediated responses. Beside, borneol enhanced the GABA-induced hyperpolarization under the current-clamp mode. Altogether, we suggest that borneol contributes in part toward mediating the inhibitory GABA and glycine transmission on the SG neurons of the Vc and may serve as an herbal therapeutic for orofacial pain ailments.

• YAKHAK HOEJI
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• v.43 no.2
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• pp.251-262
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• 1999

In order to investigate pharmacological properties of New Wonbang Woohwangchungsimwon Pill (NSCH) and Wonbang Woohwangchungsimwon Pill (SCH), the effects of NSCH and SCH on cerebral ischemia and central nervous system were compared. Cerebral ischemia insult was performed using unilateral carotid artery occlusion in mongolian gerbils. The histological observations showed preventive effects of NSCH and SCH treatments with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by SCH treatment. In contrast to what was inhibited by NSCH and SCH treatments. While NSCH and SCH had no effects on the hexobarbital-induced sleeping time, they prevented the seizures induced by electric shock and strychnine. NSCH and SCH showed sedative effect in rotarod and spontaneous activity test. Furthermore, NSCH and SCH showed anti-stress effect. Our findings suggest that the pharmacological profiles of NSCH on cerebral ischemia and central nervous system are similar to those of SCH.

• Journal of Oriental Neuropsychiatry
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• v.10 no.2
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• pp.85-103
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• 1999

In order to prove the anticonvulsive effect of the fragrance of Magnoliae Flos in convulsion-induced mice, experiments were performed on anticonvulsive effect, GABA level, glutamic acid level, GABA-T activity and GAD activity. The results were obtained as follows: 1. As far as anticonvulsive effect was concerned, on the convulsion induced by such as maximal electric seizure, strychnine, bicuculline, or picrotoxin it was not significant, but the convulsion induced by pentylenetetrazole it was significant comparing to the control group. 2. GABA level was increased significantly in mice. 3. Glutamic acid level was decreased significantly in mice. 4. GABA-T activity was decreased by the fragrance of Magnoliae Flos. 5. The fragrance of Magnoliae Flos was not effective in GAD activity. From above result, the fragrance of Magnoliae Flos had significant effects on convulsion induced by pentylenetetrazole, so it is expected to clinical application on convulsive diseases such as epilepsy.

• Natural Product Sciences
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• v.12 no.1
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• pp.44-49
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• 2006

The aqueous extract of Hydrilla verticillata (AEHV) was tested for possible pharmacological effects on experimental animals. AEHV significantly potentiated the sleeping time of mice induced by standard hypnotics viz. pentobarbitone sodium, diazepam, and meprobamate in a dose dependent manner. AEHV showed significant analgesic properties as evidenced by the significant reduction in the number of writhes and stretches induced in mice by 1.2% acetic acid solution. It also potentiated analgesia induced by morphine and pethidine in mice. Pretreatment with AEHV caused significant protection against strychnine and leptazol-induced convulsions. The behavioral studies on mice indicate CNS depressant activity of the aqueous extract of H. verticillata.

• Korean Journal of Pharmacognosy
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• v.13 no.2
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• pp.79-86
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• 1982

In order to investigate pharmacological actions of combined preparations of crude drugs, 'Jakyakgamcho-Tang' were studied. The 'Jakyakgamcho-Tang' using abdominal pain and convulsion of pediatric diseases are composed of Glycyrrhizae Radix and Paeoniae Radix alba. This study was undertaken to investigate the effect of 'Jakyakgamcho-Tang'(S-I) and parched 'Jakyakgamcho-Tang'(S-II) on anticonvulsive, analgesic, antipyretic and sedative actions. The results of this study were summarized as follows; Both 'Jakyakgamcho-Tang' and parched 'Jakyakgamcho-Tang' showed anticonvulsive effects against convulsions induced by strychnine, picrotoxine and caffeine. 'Jakyakgamcho-Tang' and parched 'Jakyakgamcho-Tang' also showed analgesic and antipyretic effects. Parched 'Jakyakgamcho-Tang' only prolonged the duration of hypnosis induced by sodium pentobarbital.