• 제목/요약/키워드: strychnine

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Piperine 유도체의 합성 및 중추억제작용에 관한 연구(I) 3,4-Methylenedioxycinnamic Acid 유도체 (Syntheses and Central Nervous Depressant Activity of Piperine Derivatives(I) 3,4-methylenedioxycinnamic Acid Derivatives)

  • 임중기;이동웅;이진영;김연순;우원식;이은방
    • 약학회지
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    • 제26권4호
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    • pp.189-196
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    • 1982
  • Piperine was reported to have a potential central nervous system (CNS) depressant activity in mice. In order to search a more active and less toxic compound than piperine and to elucidate the active group of piperine, the aromatic amides (10 compeunds) and aromatic esters (10 cempounds) of 3, 4-methylenedioxycinnamic acid were synthesized and evaluated on CNS depressant activity in comparison with piperine. The pharmacological tests conducted are as follows; (1) Acute, toxicity, (2) Antagonism against strychnine induced conduced convulsion, (3) Antagonism against maximal electrobhock seizure, (4) Rotarod test, (5) Potentiation of hexobarbital sleeping time. It was observed that 3, 4-methylendioxycinanamic acid derivatives were less toxic than piperine, and showed no significant CNS depressant activities. These facts indicate that the piperoyl group might be concerned with the pharmacological activity of piperine.

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Some pharmacological studies with Cycleanine, a diphenylbisbenzylisoquinoline alkaloid from Stephania hernandifolia

  • Maitra, Suparna;Seal, Tapan;Mallik, Sujit;Khasnobis, Arnab;Nandi, RP;Vedasiromoni, J. Rajan;Mukherjee, Biswapati
    • Advances in Traditional Medicine
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    • 제3권3호
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    • pp.123-128
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    • 2003
  • Stephania hernandifolia belonging to the family Menispermaceae is the biggest storehouse of diphenylbisbenzylisoquinoline (DBBI) alkaloids. Exhaustive chemical processing of the bulb of S. hernandifolia by the application of modern separation techniques yielded a DBBI alkaloid which was identified as cycleanine using spectroscopic methods (UV, IR, $^1HNMR$. $^{13}CNMR$, Mass). Cycleanine showed significant anti-inflammatory activity against carrageenin induced paw oedema, comparable to that produced by diclofenac sodium, used as standard drug. It exhibited potent analgesic effects against chemical and thermal noxious stimuli. It was also found to possess anticonvulsive activity in the strychnine induced convulsion model.

소음인(少陰人) 소합향원(蘇合香元)의 효능(效能)에 관(關)한 실험적(實驗的) 연구(硏究) (Experimental Studies on the Effects of Soeuminsohaphyangwon)

  • 전진상
    • 사상체질의학회지
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    • 제5권1호
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    • pp.157-173
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    • 1993
  • In order to investigate experimentally the clinical effects of Soeuminsohaphyangwon that was prescribed to cure the Wisunanrihanbyung of Soeum-In, the author experimented various activities of mixed extract from the Soeuminsohaphyangwon by the method prescribed in the experimental part. The results of the studies were summerized as follows : 1. Suppressive action was not shown on the convulsion induced by strychnine but significant effect was noted on the convulsion induced by picrotoxin and caffeine. 2. In acetic acid method experiment analgesic effect was noted. 3. A prolongation of anesthetic time by Pentobarbital sodium and antipyretic effect was observed. 4. Relaxing action was noted on the ileums of mice, also same effect was recognized on contraction of the ileums due to acetylcholine, barium chloride and histamine 2 HCl. 5. The expansion of blood vessels by relaxation of smooth muscle and fall of blood pressure were noted. According to the above results, effects based on oriental medical references were approximate to the actual experimental results.

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Inhibitory Effects of the Korean Red Ginseng Extract on the Content of Neurotransmitter-Related Components of the Mouse Brain in Convulsion-induced Model

  • Choi, Jong-Won;Yoo, Yeong-Min;Park, Hee-Juhn
    • Natural Product Sciences
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    • 제13권4호
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    • pp.384-389
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    • 2007
  • Treatment of mice with Korean Red Ginseng (KRG) changed glutamic acid and GABA content in the mouse brain tissue with pentylenetetrazole (PTZ)-induced convulsion. KRG were orally administered at a dose of 50, 100 mg/kg for two weeks. The electroconvulsions (MES) and PTZ-induced convulsion were reduced but those induced by strychnine, bicuculine and picrotoxin were not. PTZ-induced convulsion decreased the $\~{a}$-aminobutyric acid (GABA) content in brain compared to control group while the content was increased in KRG-treated group compared to PTZ group. In the PTZ-treated group, the GABA-transaminase (GABA-T) activity was increased by 59.6%, while no effect was observed on glutamate decarboxylase (GAD) activity. These results support that the KRG decreased the GABA contents and modulated the glutamic acid contents in the brain.

생약복합제(生藥複合劑)의 약효연구(藥效硏究) 제4보(第4報) -황연해독탕(黃連解毒湯)의 중추신경계(中樞神經系) 작용(作用)에 대(對)하여- (Studies on the Efficacy of Combined Preparations of Crude Drugs (IV) -Effect of ‘Whangryonhaedok-Tang’ on the Central Nervous System-)

  • 홍남두;김종우;두호경;김남재
    • 생약학회지
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    • 제13권1호
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    • pp.20-25
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    • 1982
  • In order to investigate the pharmacological action of combined preparation of crude drugs, 'Whangryonhaedok-Tang' were studied. Pharmacological studies of the water extract, methanol insoluble fraction and methanol soluble fraction obtained from 'Whangryonhaedok-Tang' were conducted. The results of this investigation were summarized as follows; Central convulsions induced by strychnine, picrotoxine and caffeine were depressed in mice. Analgesic effect was observed in mice and rats. Antipyretic effect was observed in rats and rabbits. Sedative effect was observed.

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Effects of Psoralen and Angelicin on Hepatic Drug-Metabolizing Enzyme Activities

  • Shin, Kuk-Hyun;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • 제11권2호
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    • pp.122-126
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    • 1988
  • The effects of psoralen and angelicin on hepatic microsomal drug-metabolizing enzyme (DME) activities were investigated to elucidate the mode of the interaction of furanocoumarins with DME system. A single administration (30 mg/kg,i. p.) of both coumarins to mice cased a significant prolonagation of hexobarbital-induced hypnosis as well as an increase in strychnine toxicity. The inhibitory potencies of both coumarins as measured by rat hepatic microsomal aminopyrine N-demethylase and hexobarbital hydroxylase activities in vitro were considerably weaker than those of other furanocoumarins which possess a side chain moiety. Both coumarins were found to have significant inducing effects of DME system, with repeated treatments of them. The activities of an angular coumarin were stronger than those of a linear coumarin.

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$^1$H-NMR Studies of Chiral Solvating Agent Induced - Chemical Shift Differences of Ibuprofen Enantiomers

  • Lee, Jae-Yong;Seo, Sang-Hun;Hong, Seon-Pyo;Kim, Kyeong-Ho
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.223.3-224
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    • 2003
  • Chiral discrimination of ibuprofen by $^1$H-NMR using several chiral solvating agents such as (-)-brucine, (-)-cinchonidine, (1R, 2S)-(-)-ephedrine, (S)-(-)-${\alpha}$- methylbenzylamine, (-)-strychnine and L-(-)-tryptophane was investigated. Racemic ibuprofen treated with one equivalent of chiral solvating agent was preferentially crystallized. Chiral purity of each precipitates was measured by chiral HPLC and chemical shift differences(ΔΔ$\delta$) was calculated. Eventhough (S)-(-)-${\alpha}$-methylbenzylamine was most effective for the preferential recrystalization of (S)-(+)-ibuprofen, chemical shift differentiation ability was weak. (omitted)

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The Effects of KR-10876, a new Quinolone Antimicrobial Agent, on the Central Nervous System

  • Kim, Eun-Joo;Cha, Shin-Woo;Shin, Hwa-Sup;Roh, Jung-Koo;Park, Myoung-Whan;Kim, Wan-Joo
    • Archives of Pharmacal Research
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    • 제16권1호
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    • pp.6-12
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    • 1993
  • To evaluate KR-10876, a new fluoroquinolone antibacterial agent, its effects on the central nervous system(CNS) were investigated in mmice as part of phamacological study, and the results were compared with those for ciprofloxacin and ofloxacin, two prototypes of quinolone antiabctrial agents. All the parameters indicative of CNS function and acute toxicity were measured by close observation of the animals at regular time intervals after oral treatment of test compounds. KR-10876 did not have any effect on the parameters measured at lower does (100, 300 mg/kg, p.o.), it caused ptosis, suppressed spontaneous locomotor activity, hypothemia, and prolonged hexobarbital-induced sleeping time. KR-10876 also had a slight effect on motor coordination only at high dose. Simialr to ciprofloxacin, KR-10876 did not protect mice from pentylenetetrazol-strychnine-, and electroshock-inducedl convulsions at doses tested. These findings demonstrate that KR-10876 affects CNS functions only at high doses. The rank order for effects is ofloxacin$\le$KR-10876>ciprofloxacin.

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생약(生藥) 복합제제(複合製劑)의 약효(藥效) 연구(硏究)(제25보)(第25報) -소음인소합원(小陰人蘇合元)이 항경련(抗痙攣), 진통(鎭痛), 해열(解熱), 진정(鎭靜), 적출장관(摘出腸管), 혈관(血管) 및 혈압(血壓)에 미치는 영향(影響)- (Studies on the Efficacy of Combined Preparation of Crude Drug (XXV) -Effects of Soeuminsowhapwon on Anticonvulsion, Analgesic, Antipyretic, Sedative, Isolated Ileum, Blood Vessels and Blood Pressure-)

  • 전진상;김남재;원도희;송일병;홍남두
    • 생약학회지
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    • 제16권4호
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    • pp.199-205
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    • 1985
  • In order to investigate experimentally the clinical effects of Soeuminsohapwon that was prescribed to cure cerebral hemorrhage, palpitation etc, the author tested various activities of extract from the Soeuminsohapwhangwon by the method prescribed in the experimental part. The results of the studies were summarized as follows: Suppressive action was not shown on the convulsion induced by strychnine, but significant effect was noted on the convulsion induced by picrotoxin and caffeine. In acetic acid method, analgesic effect was noted. A prolongation of anesthetic time by pentobarbital sodium and antipyretic effect was observed. Relaxing action was noted on the ileum of mice, also same effect was recognized on contraction of the ileum due to acetylcholine, barium chloride and histamine. The expansion of blood vessels by relaxation of smooth muscle and hypotensive action were noted. According to the above results, effects based on oriental medical references were approximate to the actual experimental results.

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$\imath$-Muscone의 뇌허혈 및 중추신경계에 관한 약효연구 (Pharmacological Actions of $\imath$--Muscone on Cerebral Ischemia and Central Nervous System)

  • 조태순;이선미;이은방;조성익;김용기;신대희;박대규
    • Biomolecules & Therapeutics
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    • 제5권3호
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    • pp.306-315
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    • 1997
  • In order to investigate pharmacological properties of ι -muscone, effects of ι-muscone and musk 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 a preventive effect of the ι-muscone treatment with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by the ι-muscone treatment. In contrast to what was seen with ATP, the lactate and lipid peroxide were both elevated in vehicle-treated ischemic gerbils.˙ This elevation was prevented by the ι-muscone treatment. While ι-muscone had no effects on the hexobarbital-induced sleeping time and the convulsions induced by electric shock, pentetrazol and strychnine, it had effect on rotarod test and spontaneous activity test. Respiration rate and depth were increased by the ι-muscone treatment. Furthermore, ι-muscone showed anti-stress effect. Our findings suggest that the pharmacological profile of ι-muscone on cerebral ischemia and central nervous system are similar to that of musk.

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