• Title/Summary/Keyword: 길항제

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Effect of GABA on the Contractility of Small Intestine Isolated from Rat (흰쥐 적출 소장의 수축성에 미치는 GABA의 영향)

  • Huh, Joon-Young;Kwon, Oh-Cheol;Ha, Jeong-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.8 no.2
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    • pp.95-105
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    • 1991
  • This study was designed to investigate the effect of GABA and related substances on the spontaneous contraction of rat small intestine. The rats(Sprague-Dawley), weighing 200-250g, were sacrificed by cervical dislocation, and the small intestine was isolated. Longitudinal muscle strips from duodenum, jejunum and ileum were suspended in Biancani's isolated muscle chambers and myographied isometrically. GABA and muscimol, a GABA A receptor agonist relaxed the duodenum and jejunum significantly, but baclofen-induced relaxation in those muscle strips was negligible. The effectiveness of GABA and muscimol in various regions were the greatest on duodenum, and greater on jejunum than on ileum The effect of GABA and muscimol was antagonized by bicuculline, a compeptitive GABA A receptor antagonist and picrotoxin, a noncomptitive GABA A receptor antagonist. Duodenal relaxation induced by GABA and muscimol was unaffected by hexamethonium, but was prevented by tetrodotoxin. These results suggest that GABA inhibit the contractility of smooth muscle with distinct regional difference of efficacy, and the site of inhibitory action is the GABA A receptor existing at the presynaptic membrane of postganglionic excitatory nerves.

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Design and Synthesis of Carbo Analog of Oxetanocin Bisphosphate Derivative as $P2Y_1$ Receptor Antagonist ($P2Y_1$ 수용체 길항제로서의 옥세타노신 카보 유도체의 설계 및 합성)

  • 김혜옥
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.328-333
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    • 1999
  • In order to develop selective and competitive and competitive antagonist at the $P2Y_1$ receptor a carbocyclic oxetanocin bisphosphate derivative (7) was synthesized as a bioisostere of the lead, MRS 2179. The synthesis was started from ketene diethylacetal (1) and completed in 6 steps.

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Effect of N-Methyl-D-Aspartate Glutamate Receptor Antagonist, Memantine, on Alcohol Intake in C57BL/6 Mice (N-methyl-D-aspartate glutamate 수용체 길항제 memantine의 투여가 C57BL/6형 생쥐의 알코올 섭취량에 미치는 영향)

  • Kim, Hyeun-Kyeung;Kim, Sung-Gon;Kim, Ji-Hoon;Shin, Su-Mi;Lee, Sang-Shin;Bae, So-Hyun;Kim, Ho-Chan
    • Journal of Life Science
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    • v.19 no.4
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    • pp.532-537
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    • 2009
  • Previous studies reported that the N-methyl-D-aspartate (NMDA) receptor is related to alcohol dependence in terms of developing withdrawal or tolerance, however, it is controversial whether NMDA receptor antagonists are effective in preventing relapse in alcohol-dependent patients or not. The purpose of this study was to investigate the effect of memantine, an NMDA receptor antagonist, on alcohol intake in C57BL/6 mice, which prefer drinking hereditarily. Using limited access procedures in C57BL/6 mice in the state of alcohol dependence, vehicle, naltrexone 1.0 mg/kg or, memantine 5, 25, or 50 mg/kg i.p. was administered respectively for twelve days. Medication effects on 2-hours alcohol, 22-hour water, and 24-hour food intake and body weight were studied. Using repeated measure ANOVA, the naltrexone 1 mg/kg, memantine 5, 25, or 50 mg/kg, and vehicle groups showed significant medication by day interaction (naltrexone, df=4, F=11.827, p<0.01, memantine 5 mg/kg, df=4, F=7.999, p<0.01; memantine 25 mg/kg, df=4, F=6.199, p<0.05; memantine 50 mg/kg, df=4, F=10.522, p<0.01) in 2-hour alcohol intake. In 3 memantine groups, there was no significant medication by day interaction with the vehicle group in 22-hour water intake, 24-hour food intake, or body weight. The naltrexone and vehicle groups showed significant medication by day interaction in body weight, but not in 22-hour water or 24-hour food intake. From these results, it is suggested that memantine treatment can affect alcohol intake in mice. Therefore, it is possible that a pure NMDA receptor antagonist is effective in preventing relapse in alcohol-dependent patients.

Effects of Histamine, 5-Hydroxytryptamine and Their Antagonists on the Uterine Motility in the Rat (Histamine, 5-Hydroxytryptamine 및 이들 길항물질(拮抗物質)이 흰쥐의 자궁근(子宮筋) 운동성(運動性)에 미치는 영향)

  • Yoo, Kyu-yon
    • Korean Journal of Veterinary Research
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    • v.28 no.1
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    • pp.17-22
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    • 1988
  • 평골근(平滑筋)으로 된 자궁근(子宮筋)은 자동성(自動性)을 가지고 있어서 신경지배(神徑支配)와 관계(關係)없이 근자체(筋自體)로 운동(運動)을 하게 된다. 그러나 이러한 자궁근(子宮筋)의 형태적(形態的) 및 기능적(機能的) 정상상태유지(正常狀態維持)에는 estrogen의 작용(作用)이 불가결(不可缺)한 요소(要素)로 되어 있으며 이 estrogen의 작용(作用)에 의하여 histamine의 자궁근(子宮筋)에 대한 (작용)作用이 수용체(受容體)의 어떤 기전에 의한 것인지를 알기 위하여 본(本) 연구(硏究)는 histamine과 5-hydroxytryptamine 및 이들 길항물질(拮抗物質)들의 자궁근(子宮筋) 운동성(運動性)에 대한 수축(收縮) 및 이완작용(弛緩作用)을 조사(調査)하였다. 자궁근(子宮筋)의 운동성(運動性)은 physiograph를 통(通)해 자궁수축(子宮收縮)의 빈도(頻度)와 크기를 기록하여 아래와 같은 결론(結論)을 얻었다. 1. 5-hydroxytryptamine에 대한 phenoxybenzamine의 억제작용(抑制作用)은 phenoxybenzamine의 길항성(拮抗性)의 결과(結果)이다. 2. histamine은 $H_1$-receptor를 통해서 흰쥐의 자궁평활근(子宮平滑筋)의 운동성(運動性)은 증가(增加)한다. 3. 반면 histamine은 $H_2$-receptor를 통해서는 자궁평활근(子宮平滑筋)의 운동성(運動性)을 이완(弛緩)시켰다. 4. 흰쥐의 자궁근(子官筋)에서 $H_2$-receptor 차단제(遮斷劑)가 $H_1$-receptor 차단제(遮斷劑)의 작용(作用)보다 더욱 강하였다.

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Effects of RH 5849, an Ecdysone Agonist, against Feeding and Growth of Tobacco Cutworm(spodoptera litura Fabricius)Larvae (담배거세미나방(Spodoptera litura Fabricius) 유충의 섭식과 생장에 대한 곤충탈피호르몬길항제 RH 5849의 영향)

  • 박노중;장경수;조점래;조광연
    • Korean journal of applied entomology
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    • v.31 no.4
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    • pp.475-479
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    • 1992
  • The non-steroidal ecdysone agonist RH 5849 showed almost similar LC.o values( 18.1-26.5 ppm) at all stages of larval development of the tobacco cutworm, Spodoptera litura, when treated by a leaf-disk dipping method. The feeding-inhibition rate for the 4th instar larvae was dose-dependent, and simultaneously the weight gain of 3rd instar larvae ceased within 48 hour after feeding of the cabbage leafdisk dipped into RH 5849 4.2 ppm solution. The systemic larvicidal effect of RH 5849 was compared at cabbage and tobacco whole plant test. The $LC_{50}$ values below 20 ppm(mg/kg soil) was lasted for 15 days in cabbage, 30 days in tobacco respectively.

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Selection and Antagonistic Mechanism of Pseudomonas fluorescens 4059 Against Phytophthora Blight Disease (고추역병과 시들음병을 방제하는 토착길항세균 Pseudomonas fluorescens 4059의 선발과 길항기작)

  • Jeong, Hui-Gyeong;Kim, Sang-Dal
    • Microbiology and Biotechnology Letters
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    • v.32 no.4
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    • pp.312-316
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    • 2004
  • In oder to select the powerful rhizophere-dorminatable biocontrol agent, we had isolated an indigenous antagonistic bacterium which produced antibiotic and siderophore from a disease suppressive local field soil of Gyungsan, Korea. And we could select the Pseudomosp. 4059 which can strongly antagonize against Fusarium oxysporum and Phytophthora capsici by two kinds of antifungal mechanism that can be caused by the antibiotic of Phenazin, a siderophore and a auxin like subThe selected strain was identified as Pseudomonas fluorescens (biotype A) 4059 by biochemical tests, API $\textregistered$ test, MicroLog TM system and 16S rDNA analysis. The selected antagonistic microorganism, Pseudomosp. 4059 had an antifungal mechanism of antifungal antibiotic and sidrophore. And we were confirmed the antagonistic activity of P fluorescens 4059 with in vitro antifungal test against Phytophthora capsici and in vivo by red-pepper.

Selection and Characterization of Antagonistic Microorganisms for Biological Control of Acidovorax citrulli Causing Fruit Rot in Watermelon (수박에 과실썩음병을 유발하는 Acidovorax citrulli의 생물학적 방제를 위한 길항 미생물 선발과 특성 검정)

  • Kim, Ki Young;Park, Hyo Bin;Adhikari, Mahesh;Kim, Hyun Seung;Byeon, Eun Jeong;Lee, In Kyu;Lee, Youn Su
    • Research in Plant Disease
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    • v.28 no.2
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    • pp.69-81
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    • 2022
  • This study was performed to screen the efficacy of antagonistic bacterial isolates from various sources against the bacterial fruit blotch (BFB) causing pathogen (Acidovorax citrulli) in cucurbit crops. In addition, plant growth promoting traits of these antagonistic bacterial isolates were characterized. Two thousand seven hundred ninety-four microorganisms were isolated from the collected samples. Molecular identification revealed two A. citrulli out of 2,794 isolates. In vitro antagonistic results showed that, among the 28 antagonistic bacterial isolates, 24 and 14 bacterial isolates exhibited antagonism against HPP-3-3B and HPP-9-4B, respectively. Antagonistic and growth promotion characterization of the antagonistic bacterial isolates were further studied. Results suggested that, 4 antagonistic bacteria commonly showed both antagonism and growth promotion phenotypes. Moreover, 3 isolates possessed growth promoting activities. Overall results from this study suggests that BFB causing bacterial pathogen (A. citrulli) was suppressed in in vitro antagonism assay by antagonistic bacterial isolates. Furthermore, these antagonistic bacterial isolates possessed growth promotion and antagonistic enzyme production ability. Therefore, data from this study can provide useful basic data for the in vivo experiments which ultimately helps to develop the eco-friendly agricultural materials to control fruit rot disease in cucurbit crops in near future.

The Effect of a Potent Oxytocin Antagonist, Antag I, on In Vitro Uterine Contractions in Response to Exogenous Oxytocin and on Uterine Oxytocin Receptor Number and Affinity (옥시토신 길항제, Antag I이 옥신토신 투여에 따른 자궁수축과 자궁의 옥시토신 수용체 수 및 친화력에 미치는 영향)

  • ;C. Warnell;G. Flouret;L. Wilson Jr.
    • Korean Journal of Animal Reproduction
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    • v.18 no.2
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    • pp.95-99
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    • 1994
  • The purpose of the present study was to determine the in vivo effect of oxytocin antagonist-I(Al) on uterine oxytocin receptor number (Rn) and/or binding affinity (Kd) in the estrous rat. Anesthetized rats were given a bolus infusion of control or 5${\mu}\textrm{g}$ of AI and sacri-ficed 0.5 and 4 hours later. The uterine tissue was removed, trimmed and frozen. Membrane oxytocin receptors were isolated after homogenization of uterine tissue and differential ultracentrifugation. The oxytocin receptor assay was performed by saturation with cold oxytocin competion with a high specific activity oxytocin antagonist. Rn and Kds were determined by nonlinear curve fitting methods. No differences(p>0.05) between the AI and control treated animals in either oxytocin receptor number or binding affinity was detected in this study. These data suggest that the major mode of action of AI is via competitive inhibition at the uterine oxytocin receptor and not by altering receptor number or binding affinity.

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A Study on Cerebral Ischemia-Reperfusion Injury: Involvement of Platelet-Activating Factor (뇌의 허혈-재관류손상에 대한 연구: 혈소판활성인자의 관련)

  • Lee, Won-Suk;Rhim, Byung-Yong;Hong, Ki-Whan
    • The Korean Journal of Pharmacology
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    • v.29 no.1
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    • pp.1-8
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    • 1993
  • To elucidate involvement of platelet-activating factor (PAF) in cerebral ischemia-reperfusion injury, male Sprague-Dawley rats and albino mice of either sex were subjected to a 10-min bilateral carotid artery occlusion and 6-hr recirculation. The McGraw stroke index in mice was markedly inhibited by PAF antagonists, BN 52021 and CV 6209 (1 mg/kg, i.p., each) When they were administered 10 min before bilateral carotid artery occlusion or 1 hr after reperfusion. The increases in brain water content were significantly attenuated by treatment with BN 52021 or CV 6209 in both animals. BN 52021 exhibited a significant improvement in the postischemic blood pressure change in association with a beneficial effect on the delayed dilatation of pial arterioles after 10 min of ischemia. Thus it is suggested that PAF plays an important role as an endogenous mediator in development of cerebral ischemia-reperfusion injury, and further, specific antagonists to PAF will be able to prevent or reverse the pathological sequelae of cerebral ischemia.

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흰쥐의 실험적 건망모델에 있어 항치매 효과물질의 약효검색에 관한연구(I)

  • 이영근;류항목;양지선;김옥희;최병천;이숙영
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.43-43
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    • 1992
  • 최근 수년 전부터 학습(learning), 기억(memory)의 분자약리학적 기전과 치매(dementia)의 신경생리학적 원인 규명에 대한 연구가 사회적 요구에 부응하여 증가하고 있다. 이에 본 연구에서는 횐쥐를 이용하여 실험실적 건망모델을 설정하여 항치매 물질의 효력 screening을 시도하였다. 실험실적 건망모델은 다음 두 가지 방법으로 설정하였다. 첫째, Acetylcholine 길항제인 Scopolamine을 사용하여 중추신경계중 기억, 학습기전과 관련된 것으로 알려진 cholinergic신경계률 차단하여 유발한 실험적 건망모델과, 둘째, 단백질합성 저해제인 cycloheximide를 사용하여 기억, 학습경로에 관여하는 수종의 중추 단백질듈을 비선택적으로 저해하여 유발한 실험적 건망모델을 이용하여 인삼, 오미자등의 항치매 효과를 검색하고자 수동적 회피학습능, 능동적 회피학습능, 자발운동량을 측정하여 기억, 학습, 행동의 상관 관계를 고찰하였다.

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