• Title/Summary/Keyword: 길항제

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Effect of Opioid on Nicotinic Receptor-Mediated Catecholamine Secretion in the Rat Adrenal Gland (횐쥐 부신에서 Opioid가 니코틴 수용체를 통한 카테콜아민 분비작용에 미치는 영향)

  • Lim, Dong-Yoon;Lee, Jong-Jin;Choi, Cheol-Hee
    • The Korean Journal of Pharmacology
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    • v.28 no.2
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    • pp.181-190
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    • 1992
  • The present study was conducted to investigate the effect of opioids on catecholamine (CA) secretion evoked by a selective cholinergic nicotinic agonist, 1,1-dimethyl-4-phenyl piperazinium (DMPP) and acetylcholine from the retrogradely perfused rat adrenal glands. Methionine-enkephalin $(9.68{\times}10^{-6}\;M)$ caused a significant inhibition of CA secretion evoked by DMPP (100 uM) and $ACh\;(50\;{\mu}g)$, but had no effect on the spontaneous (basal) CA release. Morphine $(1.73{\times}10^{-5}\;M)$ attenuated considerablely the increase in CA release induced by DMPP and ACh. Morphine itself also did not affect the basal CA output. A 20 to 65% reduction of the DMPP- and ACh-evoked increase in CA release was observed after the pretreatment with methionine-enkephalin or morphine. The increase in CA release evoked by DMPP and ACh was reduced markedly by preloading with an opiate antagonist naloxone $(1.22{\times}10^{-7}\;M)$ while basal CA output was not affected by naloxone. These present experimental results suggest that the nicotinic stimulation-evoked CA release from the perfused rat adrenal gland is inhibited by endogenously released opioid peptides through activation of opiate receptors located in the adrenal gland.

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Temporal Changes of c-fos, c-jun, and Heat Shock Protein 25 mRNA in Rat Uterus following Estradiol Treatment (Estrogen 처리에 따른 흰쥐 자궁조직내 c-fos, c-jun, hsp25 mRNA 발현 변화)

  • Lee, Young-Ki;Kim, Sung-Rye
    • Clinical and Experimental Reproductive Medicine
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    • v.26 no.2
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    • pp.149-156
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    • 1999
  • Steroid hormone is known to cause the dynamic changes of mammalian uterus during reproductive cycle, which are modulated via hypothalamus-pituitary -gonad reproductive endocrine axis. Although there were so many studies about estrogenic regulation of uterine growth and differentiation. There is little information about the effect of estrogen on the expression of various transcription factors involved in gene expression. Thus the present study was designed to demonstrate E induced expression of c-fos, c-jun, hsp25 mRNA in rat uterus. Employing Northern blot analysis, we studied the temporal expressions of c-fos, c-jun, and hsp25 messenger RNAs (mRNAs) elicited by a single 17beta-estradiol (E) treatment in the uteri of bilaterally ovariectomized adult rats. c-fos, c-jun, and hsp25 mRNA levels were increased and peaked at 3h after E administration, and then c-fos and c-jun mRNA levels were rapidly decreased to basal control level while, increased hsp25 mRNA levels were sustained till 12h post E treatment. To test the estrogenic effect on the increase of c-fos, c-jun, and hsp25 mRNA levels, we also examined the effects of antiestrogen (tamoxifen). Pretreatment with tamoxifen effectively blocked the E-induced increase of c-fos, c-jun, and hsp25 mRNA levels at 3h post E treatment. Present results suggest that transient increase of c-fos and c-jun protooncogene mRNA at the early time and simultaneous expression of hsp25 mRNA contribute to the response of uterine tissues to E in adult female rats.

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Existence of Cholinergic and Purinergic Receptor on the Detrusor Muscle of Rat Urinary Bladder (흰쥐 적출 배뇨근에서 콜린성 및 퓨린성 수용체의 존재)

  • Choi, Tae-Su;Kwon, Oh-Cheol;Ha, Jeoung-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.138-149
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    • 1991
  • This study was aimed at investigation of the stimulatory innervations on the rat urinary bladder. Detrusor muscle strips of 15 mm long were suspended in isolated muscle chambers containing 1 ml of PSS maintained at $37^{\circ}C$ and aerated with 95% $O_2/5%CO_2$. Isometric myography was perfomed, and the results were as followings : Muscle strips showed "on-contraction" by electric field stimulation (EFS) frequency-dependently. The EFS-induced contraction was not affected by hexamethonium, a ganglion blocker, but abolished, by tetrodotoxin, a nerve conduction blocker. Physostigmine, a cholinesterase inhibitor enhanced the EFS-induced contraction which was inhibited by hemicholinium, an inhibitor of choline uptake at the cholinergic nerve ending. Such an EFS-induced contraction was antagonized by atropine only partially, and the atropine-resistant portion was completely abolished by the desensitization of purinergic receptors by prolonged incubatin of the strips in the presence of high concentratin of ATP. Bethanechol, a cholinergic agonist, elicited concentration-dependent contraction. Adenosine triphosphate (ATP), a purinergic agonist, induced a weak but concentration-dependent contraction of short duration. Bethanechol-induced contraction was not affected by ATP-desensitization, and ATP-induced contraction was not affected by tetrodotoxin. These results suggest that there are at least two main stimulatory components of innervations in the detrusor muscle, cholinergic muscarinic and purinergic ; and those receptors are independent each other.

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Cytoprotective Effect of Zinc-Mediated Antioxidant Gene Expression on Cortisol-Induced Cytotoxicity (Cortisol 유발 세포독성에 대한 아연 관련 항산화 유전자 발현 증가에 의한 세포보호 효과)

  • Chung, Mi Ja;Kim, Sung Hyun;Hwang, In Min
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.5
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    • pp.649-656
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    • 2015
  • The protective effect of zinc against cortisol-induced cell injury was examined in rainbow trout gill epithelial cells. Cells exposed to cortisol for 24 h showed increased leakage of lactate dehydrogenase (LDH) as well as decreased cell viability in a dose-dependent manner. Treatment with zinc ($100{\mu}M$ $ZnSO_4$) reduced the severity of both LDH release and cell death as well as protected cells against cortisol-induced caspase-3 activation, indicating reduction of apoptosis. Cortisol-induced cell death, leakage of LDH, and caspase-3 activation were blocked by the glucocorticoid receptor antagonist Mifepristone (RU-486), suggesting that cell injury was cortisol-dependent. In addition, we studied the effect of zinc on the expression of antioxidant genes such as metallothionein A (MTA), metallothionein B (MTB), glutathione-S-transferase (GST), and glucose-6-phosphate dehydrogenase (G6PD) during cortisol-induced cell injury. MTA, MTB, GST, and G6PD mRNA levels increased after treatment with zinc or cortisol, separately or in combination. Higher mRNA levels of MTA, MTB, GST, and G6PD were detected when cells were treated with $100{\mu}M$ $ZnSO_4$ and $1{\mu}M$ cortisol in combination at the same time compared to treatment with zinc or cortisol separately. Cells treated with zinc showed increased intracellular free zinc concentrations, and this response was significantly enhanced in cells treated with cortisol and zinc. In conclusion, zinc treatment inhibited cortisol-induced cytotoxicity and apoptosis through indirect antioxidant action.

Effect of Vanadate and Ouabain on the Contractile Response of Cat Ileal Muscle (고양이 회장 평활근의 수축력에 미치는 Vanadate와 Ouabain의 작용)

  • Lee, Jae-Yang;Jung, Jin-Sup;Kim, Yong-Keun;Lee, Sang-Ho
    • The Korean Journal of Physiology
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    • v.18 no.2
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    • pp.139-150
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    • 1984
  • Vanadate is a potent inhibitor of Na-K-ATPase. Ouabain, the another specific inhibitor of Na-K-ATPase, induces the contraction in cardiac muscle and smooth muscle. But, some investigators observed the discrepancies between vanadate and ouabain-induced contraction in cardiac muscle. The difference of vanadate and ouabain-induced contraction was investigated in the cat ileal smooth muscle. The following results were obtained. 1) Ouabain-induced contraction was biphasic, but vanadate-induced contraction had one peak. 2) Atropine inhibited ouabain·induced contraction, but did not inhibit vanadate-induced contraction. 3) Changes in external $Ca^{++}$concentration or $Ca^{++}$ antagonists had a greater influence on the contraction induced hy vanadate than by ouabain. 4) Removal of $Na^+$ from incubation medium and high $K^+$ abolished ouabain-induced contraction, but had no effect on vanadate-induced contraction. 5) Vanadate-induced contraction was potentiated in the presence of ouabain. 6) After 3 hrs incubation with vanadate, there was no change in intracellular $Na^+$ concentrations in contrast with ouabain. These results suggest that vanadate contracts ileal smooth muscle through the mechanism different from ouabain, and this is independent of the inhibition of Na-K-ATPase activity.

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Cholinergic Mechanisms on Cardiovascular Regulation in the Ventrolateral Medulla of the Rat (흰쥐 복외측 연수에서 심혈관 조절에 대한 Choline성 기전)

  • Kim, Seong-Yun;Koh, Taek-Lip;Lee, Sang-Bok
    • The Korean Journal of Pharmacology
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    • v.23 no.2
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    • pp.77-85
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    • 1987
  • This study was carried out to determine the role of cholinoceptors in the ventrolateral medulla on central control of blood pressure (BP) and heart rate (HR). In rats anesthetized with urethane and paralyzed, microinjections of the neuroexcitatory amino acid L-glutamate (300 ng/site) were performed to functionally identity the vasopressor area (VLPA) and the vasodepressor area (VLDA) in the ventrolateral medulla oblongata. 1. The bilateral microinjection of carbachol (300 ng/site) into the VLPA produced significantly an increase in BP and HR which was not blocked by bilateral pretreatment of hexamethoium ($4\;{\mu}g/site$). 2. The bilateral microinjection of physostigmine (200 ng/site) and oxotremorine (300 ng/site) into the VLPA produced significantly an increase in BP respectively. 3. The bilateral microinjection of atropine ($4\;{\mu}g/site$) into the VLPA produced significantly a decrease in BP and HR. 4. The bilateral micro injection of acetylcholine (500 ng/site) and dimethylphenylpiperazinium (500 ng/site) into the VLDA produced significantly a decrease in BP and HR respectively. 5. The depressor and bradycardiac responses elicited by the bilateral microinjection of acetylcholine (500 ng/site) into the VLDA were blocked by bilateral pretreatment of hexamethonium ($4\;{\mu}g/site$). The results suggest that the activation of cholinoceptors in VLPA produce hypertensive and tachycardiac responses which may be mediated by muscarinic receptors, and the activation of cholinoceptors in VLDA produce hypotensive and bradycardiac responses which may be mediated by nicotinic receptors.

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A clinical report of a patient with Tourett's disorder (뚜렛 장애(Tourett's disorder) 환자(患者) 1례(例)에 대한 증례보고(症例報告))

  • Sung, Woo-Yong;Lee, Seung-Hyun;Son, Ji-Hyung;Han, Seung-Hea;Jung, Hyo-Chang
    • Journal of Oriental Neuropsychiatry
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    • v.14 no.2
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    • pp.213-218
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    • 2003
  • This is a case report of a patient with Tourett's disorder treated by Ukgan-san. We evaluated the patient Tourett's disorder by behavior and sound. His tic behaviors like eye blinking, shoulder shrugging, head jerking, facial frimace have been shown frequently, and His phonic tic symptoms like coughing, throat clearing, sniffing have been presented frequently, too. We diagnosed his condition as Wind-syndrome Caused by Hyperactivity of Liver-yang by patient's redish face, taut pulse, Left umbilical throb. So we treated the patient with Ukgan-san. and the score of Yale Global Tic Severity Scale(YGTSS) was 30 at the start of treatment. and the score of YGTSS was 3 at the end. We found that Ukgan-san was effective for the patient with Tourett's disorder.

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The Effect of Intrathecal ACEA 2085, Highly Selective AMPA Receptor Antagonist on the Hyperalgesia Observed after Thermal Injury in the Rat (흰쥐에서 척수강내로 투여한 AMPA 수용체 길항제, ACEA 2085의 항통각과민 효과)

  • Jun, Jong-Hun;Yeom, Jong-Hoon;Kim, Yong-Chul;Shim, Jae-Chul;Kim, Kyoung-Hun;Suh, Jung-Kook;Yoo, Hee-Koo
    • The Korean Journal of Pain
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    • v.12 no.1
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    • pp.1-7
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    • 1999
  • Background: To study the role of spinal alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors in pain behaviors caused by mild burn, we examined the effect of intrathecal administered ACEA 2085, which has been recently characterized as a high potency competitive AMPA receptor antagonist, on the thermal hyperalgesia state induced by mild burn. Methods: A thermal injury was induced by applying the left hind paw to a thermal surface ($52.5^{\circ}C$) for 45 sec. Thermal escape latency of the hind paw was determined using an underglass thermal stimulus. Thirty min after thermal injury, the paw withdrawal latency (PWL) in injured paw of all groups fell from 10~12 sec to 5~7 sec. At that time, ACEA 2085 (0.01~0.1 mcg) and 6-cyano-7-nitroquinoxalinedione (CNQX, 1~30 mcg) were injected through intrathecal heters in rats with mild burn injury on the right hindpaw. And then, PWL were measured in the both hindpaw every 30 minutes for about three hours. Results: The intrathecal injection of ACEA 2085 produced a dose dependent reversal of the hyperalgesia in the right hindpaw and more potent than CNQX, but had no effect upon the response latency of the normal left hind paw even at the largest doses. All effects were observed at doses that had no significant effect upon motor function. Conclusions: Intrathecal ACEA 2085, highly selective AMPA receptor antagonist produce a dose- dependent reversal of the thermal hyperalgesia evoked mild burn injury. These results suggested that spinal AMPA receptor play an important role in the hyperalgesia induced by mild burn injury.

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Genetic Transformation of Biocontrol Agent Bacillus sp, YBL-7 by Plasmid pE194 (생물방제균 Bacillus sp. YBL-7의 형질전환조건)

  • 한길환;정병곤;김상달
    • Microbiology and Biotechnology Letters
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    • v.20 no.4
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    • pp.384-389
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    • 1992
  • Bacillus sp. YBL-7 which had been isolated from ginseng root-rot suppressive soil was able to antagonize Fusarium solani causing ginseng root-rot by their antibiotic substance. In order to develop multifunctional antagonist on Bacillus sp. YBL-7 as a biocontrol agent against Fusarium salam', optimal conditions for protoplast transformation system of Bacillus sp.YBL-7 by the vector plasmid pE194 were investigated. The protoplasts of Bacillus sp. YBL-7 were obtained at best efficiency by treatment with 200${\mu}g$/ml of lysozyme in the pH 7.0 of SMM buffer for 90 minutes at $40^{\circ}C$. The cell wall of the protoplast was regenerated on the agar plate containing 1.2% agar and 0.7 M mannitol. Under the best condition for protoplast formation and regeneration, the optimal transformation was achieved with 40% polyethylene glycol (M.W. 4000) treatment for 10minutes. The vector plasmid pE194 showed the best transformation frequency at 5$\mu$g/ml of final concentration. The pE194 was very stable over 80% in the transformants.

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EFFECTS OF ELECTROACUPUNCTURE AND NALOXONE ON MOUTH OPENING REFLEX (전기침과 Naloxone이 개구반사에 미치는 영향)

  • Park, Min-Gap;Seo, Young-Ah;Song, Hyung-Geun;Lee, Sang-Ho
    • Journal of the korean academy of Pediatric Dentistry
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    • v.25 no.2
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    • pp.467-475
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    • 1998
  • 악안면 영역에 동통이 가하여지면 회피반사의 일종인 개구반사가 유발되며, 개구반사의 크기는 뇌간의 중추에 전달된 동통의 크기에 비례한다. 따라서 동통의 정도를 악이복근의 근전도를 이용하여 정량화 할 수 있고 동통의 지표로 이용할 수 있다. 본 실험은 악안면동통에 의하여 유발된 개구반사의 크기가 침점(족삼리) 전기자극으로 감소되는지와 이러한 전기침의 효과가 나타나는데 opioid 물질이 관여하는지에 대하여 연구하고자 하였다. 8주 이상, 150g이상의 Sprague-Dawley계 쥐 34 마리를 암수 구별없이 이용하여 실험하였다. 복강 내 Urethane용액(1.5g/kg)을 주입 전신마취하고 악이복근을 노출시켜 근전도 기록을 위한 한쌍의 선전극을 삽입하였다. 동통유발을 위하여 구강내 하악 이공주변에 0.1mm의 선전극을 한쌍 삽입하고 전기자극기에 연결하였다. 유해자극 조건은 duration $100{\mu}sec$, interval 5sec의 pulse로 정하고 자극의 크기는 개구반사를 일으키는 역치의 2배 크기로 하며 매 측정시마다 동일 자극을 10회식 가하여 평균하였다. 침점의 전기자극을 위하여 침점의 하나인 족삼리(Zusanli)에 표면전극(넓이 $0.4cm^2$ 정도)을 부착하고 자극부위가 약한 근수축을 일으키는 강도인 $100{\mu}sec$, 5V, 2Hz의 자극을 20분간 가하였다. 악이복근의 근전도는 교류증폭기 (Dam80, WPI, USA) 에서 1000배 증폭하여 유해자극이 가해진 순간 oscilloscope 에서 관찰하여 그 크기를 측정하였다. 침점의 전기자극으로 나타나는 진통효과가 opioid의 분비와 관련있는지 알아보기 위하여 opioid 의 길항제인 naloxone(0.2mg/kg)을 복강 내로 투여하였다. 실험군을 4군(group I - IV)으로 분류하였고 각 군에서 근전도를 측정한 단계는 다음과 같다. group I : control 침점에 전기자극 20 분간 가한후(EA), 20분후(EA20) group II : control 침점에 전기자극 20분간 가한후(EA), naloxone 투여 20분후(NX) group III : control naloxone 투여 5분후 침점에 전기자극 20분 가한후(NxEA20) group IV : control naloxone 투여 20분후(NX20) 구강내에 가해진 유해자극에 의하여 발생하는 악이복근 근전도는 족삼리 침점의 전기자극으로 그 크기가 감소하였고 이러한 침점자극의 효과는 naloxone의 투여로 인하여 억제되었다. 이와 같은 결과는 침점자극으로 진통작용이 나타나는데에 opioid 물질이 관여하고 있음을 시사한다.

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