• Title/Summary/Keyword: Central action

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In Vivo Antitumor Activities and Pharmacokinetics of DW2282 Depending on Vehicles (DW2282의 용매의존성 항암효과 및 약동력학)

  • Moon, Eun-Yi;Choi, Chung-Ha;Seong, Seung-Kyoo;Lee, Jin;Ryu, Jei-Man;Lee, Moon-Sun;Jung, Sang-Hun;Chung, Yong-Ho;Lee, Dog-Keun;Yoon, Sung-June
    • Biomolecules & Therapeutics
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    • v.6 no.4
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    • pp.395-399
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    • 1998
  • DW2282, (S)- (+)-4-phenyl -1-[N-(4-am mob enzoyl) -indolin-5- sulfonyl]-4,5- dihydro-2-imidazolone hydrochloride, is a novel anticancer agent thought to have an unique mechanism of action on the inhibition of tumor growth. In this study, we estimated in vivo antitumor activities and pharmacokinetics of Dw2282 depending on various vehicles. The inhibition rate of tumor growth was increased by 50, 100 and 200 mg/kg of Dw2282 in a dose-dependent manner. When Dw2282 dissolved in 4 sorts of vehicles was orally single dosed to rats at 50 mg/kg, Cmax of Dw2282 in 0.5% CMC.Na was a half as high as those in PG, PG+CP and PG+CP+DW. When Dw2282 was orally administered to mice for 5 days, antitumor activity of 130 mg/kg suspended in 0.5% CMC.Na was as effective as that of 65 mg/kg dissolved in the rest of vehicles. Taken together, it is thought that antitumor activities of Dw2282 are resulted from the absorption extent of it and related to the vehicle used.

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Effect of Ephedrine on the Levels of Biogenic Amines and Their Metabolites in Rat Brain (Ephedrine이 뇌내 Biogenic Amine 함량에 미치는 영향)

  • Lee, Kyung-Eun
    • The Korean Journal of Pharmacology
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    • v.31 no.2
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    • pp.153-164
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    • 1995
  • Sympathomimetic amines, especially ephedrine, are a major ingredient in proprietary medications for symptomatic treatment of upper respiratory infections. Their frequent uses can lead to occasional instances of abuse and habituation. The clinical symptoms of ephedrine abuse are similar to that of amphetamine psychosis and resemble closely that of schizophrenia. Because both amphetamine psychosis and schizophrenia are thought to be mediated primarily through the action on catecholamines, ephedrine-induced changes of the biogenic amines can be suspected. However, there were few studies about the central effects of ephedrine because of the milder central action than peripheral. Therefore, the present investigation was undertaken to elucidate the relations between the effects of single or repeated administration of ephedrine on the regional levels of biogenic amines in rat brain and ephedrine-induced CNS stimulation. The male Sprague-Dawley rats weighing $100{\sim}200\;g$ were used. After single or repeated administrations of ephedrine, blocks of tissue were obtained from frontal cortex, corpus striatum, hippocampus, thalamus, hypothalamus, substantia nigra and cerebellum. The concentration of biogenic amines(norepinephrine, epinephrine, dopamine, 5-hydroxytryptamine(5-HT)) and their metabolites (3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid(HVA), 5-hydroxyindoleacetic acid(5-HIAA)) were measured by means of high performance liquid chromatography-electrochemical detector(HPLC-ECD). The results obtained were as follows: 1) In the normal rat, the concentration of norepinephrine was the highest in hypothalamus. Dopamine, DOPAC and HVA were highest in corpus striatum, and 5-HT and 5-HIAA were highest in substantia nigra. Epinephrine was not detectable in any part of the brain tissue. 2) In a single administration of ephedrine, the concentration of DOPAC was decreased in corpus striatum. However, the other biogenic amines and their metabolites were not changed. 3) In repeated administration of ephedrine, the concentration of norepinephrine was decreased in all brain region checked. Dopamine was decreased in corpus striatum and substantia nigra and, increased in hypothalamus, and HVA was decreased in corpus striatum. 5-HT was decreased in all brain region except cerebellum and, 5-HIAA was decreased only in frontal cortex. The ratio of 5-HIAA/5-HT was increased in corpus striatum, thalamus, hypothalamus and substantia nigra. These data indicated that, although a single administration of ephedrine did not change the central neurotransmitters, repeated administration of ephedrine caused the decreases of norepinephrine and 5-HT in the most regions of brain, which may be responsible for the emergence of abnormal behavioral effect after ephedrine abuse.

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Further Evidence in Support of Psychotropic Action on Red Ginseng

  • Yoshimura, Hiroyuki;Kimura, Naoto
    • Proceedings of the Ginseng society Conference
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    • 1990.06a
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    • pp.29-35
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    • 1990
  • Using an ethopharmacological technique, we demonstrated that saponin fraction from red ginseng root possessed a potent psychotropic actions on either intermale or maternal aggression models. A series of experiments clearly indicated that one of psychoactive ingredient is ginsenoside Rbl. Although a drug-induced debilitation of motor performance remains a possible cause of the antiaggressive effect of the drug, ginsenoside Rb 1 did not alter the locomotor activity of the mice during agonistic confrontations. Thus, one can eliminate the possibility that the psychoactive effect of ginsenoside Rbl might be concealed by a drugindulced impairment of motor performance. More recently, we developed a new model for copulatory disorder and introduced into the behavioral analysis of drug action. Male mice which has been housed individually from weaning for 5 weeks failed to manifest copulatory behavior when they encountered with the sexually-receptive females. Daily administration of crude ginseng saponin during isolation housing period prevented the development of copulatory disorder, whereas both ginsenoside Rbl and Rgl were ineffective. A further experiment may be needed to explore active ingredient of ginseng saponins. Keywords Panax ginseng, Korean red ginseng, psychotropic action, saponin, ginsenoside Rb1

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Effect of Glibenclamide, $K^+$ Channel Blocker, on Renal Function in Rabbit (토끼의 신장기능에 미치는 $K^+$ Channel 차단제인 Glibenclamide의 영향)

  • 고석태;나종학
    • Biomolecules & Therapeutics
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    • v.9 no.1
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    • pp.26-32
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    • 2001
  • This study was investigated about the effect of glibenclamide (GLY) which is $K^{+}$ channel blocker on renal function in rabbit, GLY, when given into the vein, produced the diuretic action accompanied with the increases of amounts of N $a^{+}$ and $K^{+}$ excreted into urine ( $E_{Na}$ , $E^{K}$), and then osmolar and negative free water clearances ( $C_{osm}$, $T^{C}$$_{H2O}$), fraction excretory rates of filtered N $a^{+}$ and $K^{+}$ ( $F_{Na}$ , $F_{K}$) and ratios of $E_{K}$ against $E_{Na}$ were augmented. Filtration fraction (FF) were reduced because renal plasma flow (RPF) were not changed but glomerular filtration rates (GFR) were diminished. GLY administered into a renal artery exhibited significant reduction of urine volume along with the decreases of GFR and RPF in only experimented kidney whereas changes of renal function was not observed in control kidney. GLY given intracerebroventricularly exhibited diuretic action along with the increase of $E_{Na}$ , $E_{K}$ and $F_{Na}$ , $F_{K}$ by small dose which was not affect on renal function when it given into the vein. Above results suggest that GLY given into the vein in rabbit produce the diuretic action by inhibition of electrolytes reabsorption in renal tubules through central function. function.n. function.ion.

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Renal Action of $N^G$-Nitro-L-arginine, Nitric Oxide Synthase Inhibitor, in Dog and Rabbit (니트릭옥사이드의 합성 억제제인 $N^G$-니트로-L-아르기닌의 신장작용)

  • Ko, Suk-Tai;Yu, Kang-Jun;Hwang, Myung-Sung
    • YAKHAK HOEJI
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    • v.42 no.5
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    • pp.519-526
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    • 1998
  • This study was performed in order to investigate the effect of renal function of NG-nitro-L-arginine (L-NOARG), inhibitor of nitric oxide (NO) synthase, in dog and ra bbit. L-NOARG, when given intravenously in dogs, exhibited the decrease in urine flow (vol), renal plasma flow (RPF), osmolar clearance ($C_{osm}$) and amounts of sodium and potassium excreted in urine($E_{Na},\;E_K$). These renal functions of L-NOARG showed the same aspect in rabbit, too. L-NOARG, when administered into a renal artery, showed the same pattern as was obtained when given intravenously in both experimental and control kidney in dog. L-NOARG administered into the carotid artery showed the decrease in Vol, RPF, $E_{Na}$, in a low doses that did not show any effect when given intravenously. Above results suggest that L-NOARG produces antidiuretic action in dog and rabbit, and these antidiuretic actions may be mediated by central action.

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An Exploration of a Performer's Organic Action

  • BongHee, Son
    • International Journal of Advanced Culture Technology
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    • v.10 no.4
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    • pp.383-388
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    • 2022
  • This thesis explores the principle of a performer's organic action by means of his/her bodily responses on stage. This research has been developed to define the nature of a performer's central task in order to constitute empirical understanding of acting and the purpose of training in addressing the question of what sort of qualitative bodily training is necessary to be in a state of the full body involvement. This study investigates to articulate a performer's fundamental task at the most rudimentary level by utilizing those theatre artists' concepts with practical assumptions. In particular, the key terms, happen and change signifies the quality of a performer's body that has to fit into the given environment in which the performer's body can be subordinated through the moment on stage. Here, we argue that a performer's essential task parallel to make the following moment to happen and change by means of progressing a set of the next moment. In this manner, we also argue that a moment of displaying the performer's conscious effort, forceful and externalizing the visible elements under the use of erroneous language leads his/her body not to function on stage, a state of disengagement from his/her body. Finally, we provide a way to facilitate a performer's organic action by focused on his/her lived experience to create the functional moment which is opposite to the predominance of a representation, maintaining the performer's intellectual sense.

Diuretic Action of Vasopressin (바소프레신의 이뇨작용)

  • Go, Seok-Tae;Yun, Jae-Gyeong;Yu, Gang-Jun
    • YAKHAK HOEJI
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    • v.40 no.4
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    • pp.468-477
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    • 1996
  • Vasopressin which is an antidiuretic hormone in human body produced the diuretic action in dog. This study was investigated in order to certify the diuretic action and to search out the mechanism of the action on the vasopressin. Vasopressin, when given in a dose of 10.0mU/kg, bolus+1.0mU/kg/min intravenously, exhibited the increase of urine flow(Vol), renal plasma flow(RPF), osmolar clearance (Cosm) and amounts of sodium and potassium excreted in urine ($E_{Na},\;E_K$), the decrease of reabsorption rate of sodium and potassium in renal tubules ($R_{Na},\;R_K$), and then elevated the mean arterial pressure(MAP). Vasopressin given in a increased dose to 30.0mU/kg, bolus+1.0mU/kg/min intravenously elicited the same aspect with that exhibited by a small dose in changes of Vol. and all renal function and potentiated the change rates, whereas this time MAP did not change at all when compared with control value. Vasopressin, when administered into a renal artery, did not induce the changes of Vol and all renal function in experimental (administered) kidney, but increased slightly the Vol, glomerular filtration rate(GFR), $E_{Na},\;and\;E_K$ expected the no change of $R_{Na}\;and\;R_K$ in the control (not administered) kidney. Vasopressin, when infused into carotid artery, showed the increase of Vol. GFR, $E_{Na},\;and\;E_K$ and no change of $R_{Na}\;and\;R_K$ in a dose of 1/5 of intravenous dose. Diuretic action of vasopressin administered into carotid artery was not influenced by renal denervation. Above results suggest that vasopressin produced diuretic action by hemodynamic changes in dogs. These hemodynamic changes may be mediated by central endogenous substances not associated with renal nerve.

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Elastic solutions for shallow tunnels excavated under non-axisymmetric displacement boundary conditions on a vertical surface

  • Wang, Ling;Zou, Jin-Feng;Yang, Tao;Wang, Feng
    • Geomechanics and Engineering
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    • v.19 no.3
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    • pp.201-215
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    • 2019
  • A new approach of analyzing the displacements and stress of the surrounding rock for shallow tunnels excavated under non-axisymmetric displacement boundary conditions on a vertical surface is investigated in this study. In the proposed approach, by using a virtual image technique, the shear stress of the vertical ground surface is revised to be zero, and elastic solutions of the surrounding rock are obtained before stress revision. To revise the vertical normal stress and shear stress of horizontal ground surface generated by the combined action of the actual and image sinks, the harmonic functions and corresponding stress function solutions were adopted. Based on the Boussinesq's solutions and integral method, the horizontal normal stress of the vertical ground surface is revised to be zero. Based on the linear superposition principle, the final solution of the displacements and stress were proposed by superimposing the solutions obtained by the virtual image technique and the stress revision on the horizontal and vertical ground surfaces. Furthermore, the ground settlements and lateral displacements of the horizontal and vertical ground surfaces are derived by the proposed approach. The proposed approach was well verified by comparing with the numerical method. The discussion based on the proposed approach in the manuscript shows that smaller horizontal ground settlements will be induced by lower tunnel buried depths and smaller limb distances. The proposed approach for the displacement and stress of the surrounding rocks can provide some practical information about the surrounding rock stability analysis of shallow tunnels excavated under non-axisymmetric displacement boundary conditions on a vertical surface.

Effect of the increased sympathetic outflow on the changes of muscle tone and central nervous system excitability in chronic stroke patients (만성 편마비 환자에 대한 교감신경 활동 강화가 근 긴장도와 중추신경흥분성 변화에 미치는 영향)

  • Kang, Byeong-Kil;Nam, Ki-Won
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.12 no.11
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    • pp.5019-5026
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    • 2011
  • The purpose of this study was to investigate the effect of the increased sympathetic outflow on the changes of muscle tone and central nervous system excitability in the chronic stroke patients. This study was conducted from October 12th 2009 to December 4th 2009. 30 patients with chronic hemiplegia for at least 6 months were participated. Before and during the mental arithmetic, static handgrip and post-handgrip ischemia tasks, the central nervous system action potentials and global synkinesis level were compared. The central nerve action potentials were measured with H/Mmax ratio and V/Mmax ratio. To obtain global synkinesis level, surface electromyography data were digitized, processed to root mean square. In our study, The global synkinesis level during knee flexion and extension was decreased in the mental arithmetic and in the post-handgrip ischemia task(p<.05) but not in the grip task. Also, V/Mmax ratio was decreased all in the three task(p<.05). In conclusion, we know that the central nervous system excitability and the muscle tone in chronic hemiplegic patients were decreased by the increased sympathetic outflow.

Field survey of 1983 central East Sea Tsunami : Imwon Port (1983년 동해 중부 지진해일 현장조사 : 임원항)

  • Kim, Sung-Min;Lee, Seung-Oh;Choi, Moon-Kyu;Cho, Yong-Sik
    • Journal of the Korean Society of Hazard Mitigation
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    • v.7 no.4
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    • pp.97-105
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    • 2007
  • This study has been focus to certify the run-up heights, losses of human lives and property damages due to the 1983 Central East Sea tsunami. We have conducted the interview with indigenous inhabitant and field surveying at the Imwon port, East sea in Korea in order to inquire into the state of things occurred during that period. It is also investigated how much well they are aware of the emergency action plan including the evacuation system. Base on the reliable interviews, we selected and surveyed 10 places at the Imwon port, where the historical maximum overflowing occurred due to the 1983 Central East Sea tsunami. The measured run-up heights are approximately $3.3m{\sim}4.0m$ at the selected 10 places and it is found that the sea water ran over the banks in Imwon stream about 700m upstream from the Imwon port. From this study we can suggest supplementing the present emergency action plan and supply the state-of-the-art inundation map.