• Title/Summary/Keyword: CNS depressant

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Syntheses and Central Nervous Depressant Activities of Piperine Derivatives (V) (피페린 유도체의 합성 및 중추 억제작용에 관한 연구(V) -Methylenedioxyphenylalkenoic Acid Amide 유도체-)

  • 도경삼;임중기;우경식;이은방
    • YAKHAK HOEJI
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    • v.30 no.4
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    • pp.163-168
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    • 1986
  • Thirteen compounds were synthesized by condensing the N-heterocyclic amines (piperidine, pyrrolidine, morpholine) and secondary aliphatic amines (dimethylamine, diethylamine) with 3,4-methylenedioxyphenylalkenoic acid chlorides for developing CNS depressants. Among them, N, N-diethyl-3,4-methylenedioxycinnamamide (IX) and N, N-dimethyl-5-(3,4-methylenedioxyphenyl)-2, 4-pentadienoic acid amicle (XII) exhibited strong activity in antagonism against pentylenetetrazole-induced convulsion, strychnine-induced convulsion and maximal electroshock seizure. N, N-Dimethyl-3, 4-methylenedioxycinnamide (VIII) showed more potent activity in antagonism against strychnine-induced convulsion and maximal electroshock seizure and in the prolongation of hexobarbital sleeping time.

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Analgesic Effect of the Essential Oil from the Rhizomes of Cnidium officinale

  • Heo, Kyung-Hee;Lim, Jae-Chul;Choi, Jae-Woo;Ryu, Dong-Uk;Lee, Dong-Ung
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.387.2-387.2
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    • 2002
  • The rhizomes of Cnidium ollicinale Makino (Umbelliferae) has been used as sedatives and analgesics in the Traditional Medicine in Korea. The essential oil of this rhizomes has been reported to possess CNS depressant activity. however, its analgesic activity has not yet been investigated. (omitted)

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CNS Activities of the Aqueous Extract of Hydrilla verticillata in Mice

  • Pal, Dilipkumar;Balasaheb, Nimse Satish;Khatun, Samina;Bandyopadhyay, Pranab Kumar
    • 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.

Central nervous system activity of the methanol extracts of Caesalpinia bonducella and Bauhinia racemosa (Caesalpinaceae) in experimental animal model

  • Kumar Ramanathan Sambath;Sivakumar Thangavel;Sundaram Rajagopal Shanmuga;Gomathi Periyasamy;Kumar Mani Senthil;Mazumdar Upal Kanti;Gupta Malaya
    • Advances in Traditional Medicine
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    • v.6 no.3
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    • pp.221-231
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    • 2006
  • The aim of the present study is to investigate central nervous system (CNS) activity of the methanol extracts of leaves of Caesalpinia bonducella (MECB) and stem bark of Bauhinia racemosa (MEBR) (Caesalpinaceae) in Swiss albino mice and Wistar albino rats. General behavior, exploratory behavior, muscle relaxant activity and phenobarbitone sodium-induced sleeping time were studied. The results revealed that the methanol extracts of leaves of Caesalpinia bonducella at 100 - 200 mg/kg and stem bark of Bauhinia racemosa 100 - 200 mg/kg caused a significant reduction in the spontaneous activity (general behavioral profile), remarkable decrease in exploratory behavioral pattern (Y-maze and head dip test), a reduction in muscle relaxant activity (rotarod and traction tests), and also significantly potentiated phenobarbitone sodium-induced sleeping time. The results suggest that MECB and MEBR exhibit CNS depressant activity in tested animal models.

Pharmacological study of 'treenoponchomul'-an Ayurvedic diuretic preparation

  • Haque, Sabera;Hannan, JMA;Shahriar, Masum;Islam, M Naimul;Sattar, Mafruhi;Choudhuri, MSK
    • Advances in Traditional Medicine
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    • v.3 no.1
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    • pp.21-28
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    • 2003
  • The pharmacological effects of an Ayurvedic diuretic drug 'Treenoponchomul' (TPM) was investigated in animal model. The pharmacological actions of the test drug along with that of the components thereof, on the Central Nervous System (CNS) were studied. The drug under study TPM showed little effect on the CNS, the same can not be said about the components. The most prominent CNS depressant effect was observed with Saccharum officinarum Linn. (EE) in that it lowered the spontaneous motor activity as well the exploratory -behavior of the animals. An exploration retarding effect of moderate degree, was evident with Imperata cylindrica Beauv. (UU), and Phragmites maxima Blatter & McCann (NN). Although the test drug did not alter the normal locomotor and/ or exploratory behavior of the treated animals, it did significantly (p<0.01) lower the locomotion of the amphetamine induced hyperactive animals. TPM along with its components (especially Desmostachya bipinnata Stapf. Root, KU), significantly reduced the gastro-intestinal motility of the treated animals (p<0.01). The test drug and its components lowered the body weight of the treated animals, on being administered chronically (30 days), with EE being the only exception.

Xylazine-induced depression and its antagonism by α-adrenergic blocking agents (Xylazine의 진정효과와 α-adrenergic 수용체 봉쇄약물의 길항효과)

  • Kim, Chung-hui;Hah, Dae-sik;Kim, Yang-mi;Kim, Jong-shu
    • Korean Journal of Veterinary Research
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    • v.33 no.1
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    • pp.71-80
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    • 1993
  • The central nervous system depressant effect of xylazine and xylazine-ketamine was studied in chicken and mice. Intraperitoneal injection of xylazine(1~30 mg/kg) and xylazine(1~30 mg/kg)-ketamine(100 mg/kg) induced a loss of the righting reflex in chicken and mice, respectively. These effects of xylazine were dose-dependent. The results obtained were as follows; 1. The effect of xylazine-induced depression was antagonized by adrenergic antagonists having ${\alpha}_2$-blocking activity(yohimbine, tolazoline, piperoxan and phentolamine). 2. Yohimbine was most effective in the reduction of the CNS depression by xylazine. 3. Phenoxybenzamine and prazosin did not reduced CNS depression by xylazine in both species. 4. Labetalol (${\alpha}_1$, ${\beta}_1$-adrenergic antagonist) and propranolol(${\beta}$-adrenergic blocking agent) were not effective in reducing xylazine induced depression. 5. Cholinergic blocking agents (atropine and mecamylamine), a dopaminergic antagonist (Haloperidol), a histamine $H_1$-antagonist(chlorpheniramine), a histamine $H_2$-antagonist(cimetidine), a serotonergic-histamine $H_1$ antagonist(cyproheptadine) were not effective in reducing xylazine-induced depression. 6. Xylazine-induced depression is mediated by ${\alpha}_2$-adrenergic receptors and appears not to be involved in cholinergic, dopaminergic, serotonergic or histaminergic pathways.

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Central nervous system depressant activity of Leucas aspera root

  • Rahman Shafiur;Sarder Mokaddez;Ali Yusuf;Rashid Abdur
    • Advances in Traditional Medicine
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    • v.6 no.3
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    • pp.174-178
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    • 2006
  • The ethanolic extract of Leucas aspera root was studied for its effect on the central nervous system (CNS) using pentobarbitone induced sleeping time test, the open field test and the hole cross test in Swiss albino mice. The present investigation revealed that the extract at the doses of 250 and 500 mg/kg, significantly prolonged the pentobarbitone induced sleeping time in mice though the onset of sleep was delayed as compared to control. In open field test the depressing effect was prominent from the second observation period (30 min) and persisted throughout the entire experimental period (240 min). In the hole cross test, the depressing effect was observed significant from the third observation period (60 min) and persisted up to the seventh observation period (240 min) except at fourth observation (90 min) for 250 mg dose group and depressing effect was significant from second observation (30 min) up to seventh observation period (240 min) for 500 mg dose group. These results support the finding that Leucas aspera root may contain biologically active constituent(s) having CNS activity.

Neuropharmacological study of some Ayurvedic medicinal plants

  • Hannan, JMA;Shahriar, Masum;Islam, M Naimul;Sattar, Mafruhi;Haque, Sabera;Choudhuri, MSK
    • Advances in Traditional Medicine
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    • v.3 no.1
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    • pp.8-17
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    • 2003
  • Water extract (kwath) of six different widely used Ayurvedic medicinal plants were tested in mice for possible neuropharmacological efficacy. In the present experiments it was observed that a number of plant tested causes a significant level of Central Nervous System (CNS) depression, in that it significantly decreased the spontaneous Motor activity, and also lowered the exploratory behavior of the treated animals. Terminalia chebula (HAA), Terminalia bellerica (BHA), Emblica officinalis (AA), Piper longum 1. (PP). exhibited depressant action of on the CNS. Apart from them a mild to moderate degree of depression was evident as a consequence of administration of Zingiber officinale Rosc (SUT), Piper nigrum L. (MRC). However, none of the plant tested did not exhibit significant effects on pentobarbital induced narcosis, and this indicated that the sedating effects of the drug was not associated with the risk of fatal consequences on overdose.

Isolation of Hepatic Drug Metabolism Inhibitors from the Seeds of Myristica fragrans

  • Shin, Kuk-Hyun;Kim, Ok-Nam;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • v.11 no.3
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    • pp.240-243
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    • 1988
  • The hexane extract from Nutmeg, the seed of Myristica fragrans significantly inhibited hepatic drug-metabolizing enzyme activity. Through systematic fractionation by $SiO_2$ column and vacuum liquid chromatography monitoring by bioassay, three components, myristicin, (I), licarin-B (II) and dehydrodiisoeugenol (III) were isolated as active principles. Compounds II and III, with a single treatment (200mg/kg, i.p.) showed not only a significant prolongation of hexobarbital-induced sleeping time but also a significant inhibition of aminopyrine N-demethylase and hexobarbital hydroxylase activities in mice. Compounds I and II provoked a sleep episode at a subhypnotic dose of HB, suggesting that they possess CNS-depressant properties.

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Pharmacological Activities of Sesquiterpenes from the Rhizomes of Curcuma zedoaria (아출(莪朮)의 Sesquiterpene 성분의 약물활성)

  • Shin, Kuk-Hyun;Yoon, Ki-Young;Cho, Tae-Soon
    • Korean Journal of Pharmacognosy
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    • v.25 no.3
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    • pp.221-225
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    • 1994
  • Pharmacological activities of two sesquiterpenes, curzerenone(I), and curcumenol(II) isolated from the rhizomes of Curcuma zedoaria being used as an aromatic stomachic in Chinese medicines were evaluated in rats and mice. Curzerenone (I), at 100mg/kg, p.o. showed a potent protective effect against HCl-ethanol induced gastric lesion in rats, and curcumenol(II), at the same dose level showed a CNS depressant action characterized by a potentiation of hexobarbital(HB)-induced narcosis. Both compounds showed a moderate analgesic action but did not exhibit a hypothermic action even at 200mg/kg dose level.

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