• Title/Summary/Keyword: inhibitor injection

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Role of Spinal Adenosine $A_2$ Receptor in the cardiovascular Regulation in Rats (흰쥐에서 실혈관 조절기전에 대한 척수의 Adenosine $A_2$수용체의 역할)

  • 문삼영;신현진;신인철;고현철;엄애선;박정로;김범수;강주섭
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.325-331
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    • 2000
  • The present study was designed to assess the role of spinal adenosine $A_2$ receptor in the regulation of cardiovascular functions such as mean arterial pressure (MAP) and heart rate (HR) in male Sprague-Dawley rats. Rats (250~300 g) were anesthetized with urethane and paralyzed with d-tubocurarine and artificially ventilated. blood pressure and HR were continuously monitored via a femoral catheter connected to a pressure transducer and a polygraph. Drugs were administered intrathecally using injection cannula through guide cannula which was inserted inthrathecally at lower thoracic level through a puncture of an atlantooccipital mombrane. Intrathecal injection of an adenosine $A_2$ receptor agonist, 5'-(N-cyclopropyl)-carboxamaidoadenosine (CPCA; 1, 2 and 3 nmol, respectively), produced a dose-dependent decrease in MAP and HR. Pretreatment with $N^{G}$-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor or 10 nmol of MDL-12,330, an adenylate cyclase inhibitor blocked significantly the depressor and bradycardic effect of 2 nmol of CPCA. But, Pretreatment with 3 nmol of bicuculline, gamma-aminobutyric acid A (GAB $A_{A}$) receptor antagonist, or 50 nmol of 5-aminovaleric acid, GAB $A_{B}$ receptor antagonist did not inhibit the depressor and bradycardic effect of 2 nmol of CPCA. These results indicate that adenosine $A_2$ receptor in the spinal cord plays an inhibitory role in the regulation of cardiovascular function and that the depressor and bradycardic action of adonosine $A_2$ receptor are mediated via the synthesis of nitric oxide and the activation of adenylate cyclase in the spinal cord of rats.s.s.s.

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Evaluation of Pharmacological Effect of Soybean Trypsin Inhibitor-Chondroitin Sulfate Conjugates (Soybean Trypsin Inhibitor와 황산 콘드로이친 포합체의 약리 효과 평가)

  • Choi, Youn-Lim;Nam, Hyun-Gu;Shin, Young-Hee
    • Journal of Pharmaceutical Investigation
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    • v.30 no.3
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    • pp.159-166
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    • 2000
  • Kunitz-type soybean trypsin inhibitor (SBTI) and chondroitin sulfate (A, and C type) were conjugated using sodium periodate method. And the physicochemical, pharmacokinetic properties and immunogenecity of the conjugates (Chon-A-SBTI or Chon-C-SBTI) were characterized. We expected the conjugation using chondroitin sulfate to reduce the immunogenecity and to improve the pharmacological effect. As the results, the mean molecular weight of the conjugate highly increased. After I.V. injection of the radiolabeled conjugates or native SBTI into mice, it was found that native SBTI showed rapid elimination from plasma, whereas Chon-A-SBTI and Chon-C-SBTI were slowly eliminated. Organ distribution of the two agents at 30 min after I.V. injection was different : Chon-A-SBTI or Chon-C-SBTI accumulated to a large extent in the liver (13% in Chon-A-SBTI and 16% in Chon-C-SBTI), whereas native SBTI was taken up more rapidly by the kidney (107% dose/g of tissue) and excreated into the urine (26%). In addition we evaluated the therapeutic value of the conjugates by using the sublethal septic shock model caused by pseudomonal elastase and tested the immunogenecity by passive cutaneous anaphylaxis shock (PCA). The conjugates were more effective than native SBTI against pseudomonal elastase induced septic shock in guinea pig. In case of the conjugates, the pharmacological and therapeutic effect lasted over 3 hours long. In immunogenecity test, both of the conjugates showed the reduction of their immunogenecity, especially Chon-A-SBTI looked most effective.

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Effect of Phosphate-based Inhibitors on Pipe Corrosion of Drinking Water Supply (상수도 배급수관망의 부식방지를 위한 인산염계 방청제 적용에 관한 연구)

  • 이윤진;남상호
    • Journal of Environmental Health Sciences
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    • v.29 no.3
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    • pp.65-71
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    • 2003
  • The injection concentration of corrosion inhibitor increases under the pH 7, temperature of 2$0^{\circ}C$, and alkalinity of 35 mg/l (as CaCO$_3$), the corrosion rate gradually decreased. When the corrosion inhibitor of 10 mg/l is injected, the corrosion rate for carbon steel pipe, galvanized steel pipe, and copper pipe reduces for 37, 66 and 61 % respectively that it is more efficient on galvanized steel pipe and copper pipe. As a result of examination of corrosion rate at pH 6, 7, and 8 when injecting 10 mg/l of corrosion inhibitor under the conditions of 2$0^{\circ}C$ in water temperature and 35 mg/l (as CaCO$_3$) in alkalinity, the efficiency of the corrosion inhibitor increases as the pH increases. For carbon steel pipe, it does not show much a difference with the change of the pH condition, but galvanized steel pipe and copper pipe clearly show the corrosion rate depending on the change of the pH condition. The efficiency of corrosion inhibitor is low as the concentration of residual chlorine is high, but it does not show a great influence at 0.4 mg/l or less. For each pipe type, in the case of carbon steel pipe, the range of increase of corrosion speed following the residual chloride is higher than the other pipe types. In the meantime, the effect following the residual chlorine in copper pipe is low.

Experimental Study on Injection Rate Effects during Gas Hydrate Production using Flue Gas Swapping Method (가스하이드레이트 배가스 치환 시 주입유속의 영향에 관한 실험적 연구)

  • Lee, Dong-Gun;Lee, Joo-Yong;Lee, Min-Hui;Lee, Jae-Hyung
    • 한국신재생에너지학회:학술대회논문집
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    • 2008.10a
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    • pp.196-199
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    • 2008
  • In this study, gas hydrate production has been followed using swapping method to investigate the effect of injection rate of flue gas and soaking period in unconsolidated artificial sand sample. The results shows that recovery factor of methane gas decreases with increasing the injection rate of flue gas. This indicates that the velocity of flue gas in porous media may act as kinds of inhibitor for production of hydrate. Also recovery factor increases with increasing the soaking time.

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A Blockade of the Central MAPK Pathway Attenuates Referred Pain in Rats with Complete Freund's Adjuvant -Induced Inflammation of the Temporomandibular Joint

  • Won, Kyoung-A.;Lim, Nak-H.;Lee, Min-K.;Park, Min-K.;Yang, Gwi-Y.;Park, Yoon-Yub;Ahn, Dong-K.;Bae, Yong-C.
    • International Journal of Oral Biology
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    • v.35 no.3
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    • pp.83-89
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    • 2010
  • We investigated the role of the central MAPK pathways in extra-territorial (referred) pain resulting from inflammation of the temporomandibular joint (TMJ). Experiments were carried out on male Sprague-Dawley rats weighing 220-280 g. Under anesthesia, these animals were injected with $50\;{\mu}L$ of complete Freund's adjuvant (CFA) into the TMJ using a Hamilton syringe. In the control group, saline was injected into the TMJ. To identify the extent of inflammation of the TMJ, Evans blue dye (0.1%, 5 mg/kg) was injected intravenously at 1, 3, 6, 9, 12 and 15 days after CFA injection. The concentration of Evans blue dye in the extracted TMJ tissue was found to be significantly higher in the CFA-treated animals than in the saline-treated group. Air-puff thresholds in the vibrissa pad area were evaluated 3 days before and at 3, 6, 9, 12, 15 and 18 days after CFA injection into the TMJ. Referred mechanical allodynia was established at 3 days, remained until 12 days, and recovered to preoperative levels at 18 days after CFA injection. This referred mechanical allodynia was observed in contralateral side area. To investigate the role of central MAPK pathways, MAPK inhibitors ($10\;{\mu}g$) were administrated intracisternally 9 days after CFA injection. SB203580, a p38 MAPK inhibitor, significantly attenuated referred mechanical allodynia, as compared with the vehicle group. PD98059, a MEK inhibitor, also reduced CFA-induced referred mechanical allodynia. These results suggest that TMJ inflammation produces extra-territorial mechanical allodynia, and that this is mediated by central MAPK pathways.

Intravenous administration of piceatannol, an arginase inhibitor, improves endothelial dysfunction in aged mice

  • Nguyen, Minh Cong;Ryoo, Sungwoo
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.1
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    • pp.83-90
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    • 2017
  • Advanced age is one of the risk factors for vascular diseases that are mainly caused by impaired nitric oxide (NO) production. It has been demonstrated that endothelial arginase constrains the activity of endothelial nitric oxide synthase (eNOS) and limits NO generation. Hence, arginase inhibition is suggested to be vasoprotective in aging. In this study, we examined the effects of intravenous injection of Piceatannol, an arginase inhibitor, on aged mice. Our results show that Piceatannol administration reduced the blood pressure in aged mice by inhibiting arginase activity, which was associated with NO production and reactive oxygen species generation. In addition, Piceatannol administration recovered $Ca^{2+}$/calmodulin-dependent protein kinase II phosphorylation, eNOS phosphorylation and eNOS dimer stability in the aged mice. The improved NO signaling was shown to be effective in attenuating the phenylephrine-dependent contractile response and in enhancing the acetylcholine-dependent vasorelaxation response in aortic rings from the aged mice. These data suggest Piceatannol as a potential treatment for vascular disease.

The Status of the Development of Production Technology of the Gas Hydrate (가스하이드레이트 생산기술 개발동향 분석)

  • An, Seung-Hee;Park, Seoung-Soo;Shin, Hoon-Chang;Kim, Byung-Joo;Lee, Jeong-Hwan
    • 한국신재생에너지학회:학술대회논문집
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    • 2008.10a
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    • pp.216-219
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    • 2008
  • As a future clean substitute energy, the Gas hydrate development projects are world widely carried out to prepare the shortage of petroleum and natural gas resources. The OIIP of gas hydrate is estimated approximately 10 Trillion LNG equivalent ton and it reaches almost the amount of 5 thousand years use for the world people. To develop the commercial production technology, several research projects like Malik and Alaska project have been carried by several advanced countries and teams, but nobody have succeeded it yet due to the technical problems and the high risks. The technologies developed up to now for the hydrate production are categorized to four methods, such as depressurization method, thermal recovery method, inhibitor injection method and replacement method. As these methods are highly related to the costs and the environmental problems, many other researches including the safety, environment and disaster prevention are actively fulfilled as well.

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Computational Estimation of Process Parameters in Structural Reaction Injection Molding (SRIM/RIM을 위한 공정 인자의 수치 해석적 평가)

  • ;R.J. Duh
    • Journal of the Korean Society for Precision Engineering
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    • v.13 no.11
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    • pp.143-151
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    • 1996
  • Structural reaction injection molding을 이용한 복합재료의 제품 셩형을 위한 모델링 전략을 설명하였다. 사용된 모델은 두 평행한 원판형 mold에 있는 불 균일한 온도조건의 fiber preform을 통과하는 reactive srsin의 방사형 유동을 시뮬레이션 한다. 이러한 모델은 중요한 작동인자와 공정인자(주입온도, mold의 온도, 유량, cavity의 두께와 섬유의 조밀도)등이 유동속도, 변화(monomer, radical, inhibitor) 및 온도분포 등에 미치는 영향을 예견한다. 열전달과 질량전달 및 화학반응을 고려하여 모델을 개발하였다. 중요한 공정인자를 평가하기 위한 효울적인 공정창( process window)을 제공하는데 본 연구의 목적을 두었다. 2차원적인 Lagrangian 방식에 1차원적인 유동과 제한적인 2차원 열전달을 가정하여 모델을 유도하였고, 방정식은 implicit difference scheme에 의해 전개하였다. 이 모델은 Gonzalez-Romero의 실험 결과와 비교함에 의해 확인되었고, 실험결과가 잘 일치함을 보였다.

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Masculinization in juvenile longtooth grouper, $Epinephelus$ $bruneus$, with aromatase inhibitor: changes in GtH subunit mRNA expression and steroids hormone levels

  • Hur, Sung-Pyo;Lim, Bong-Soo;Hwang, In-Joon;Kim, Se-Jae;Ryu, Yong-Woon;Hur, Sang-Woo;Song, Young-Bo;Jeong, Hyung-Bok;Baek, Hae-Ja;Takemura, Akihiro;Lee, Young-Don
    • Animal cells and systems
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    • v.16 no.2
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    • pp.127-134
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    • 2012
  • We investigated the effects of fadrozol, an aromatase inhibitor (AI), and $17{\alpha}$-methyltestosterone (MT) on the induction of sex change in juvenile longtooth grouper $Epinephelus$ $bruneus$, via histological observation of gonads. Changes in the mRNA expression of GtH subunits (FSH-${\beta}$ and LH-${\beta}$) in the pituitary, and estradiol-$17{\beta}$ (E2) and 11-ketotestosterone (11-KT) levels in the blood were also surveyed after AI and MT treatment. Juvenile longtooth groupers ($113{\pm}17g\;body\;weight$; $16.2{\pm}1.2cm\;body\;length$) received intramuscular injections of AI at 3 (3-AI) and 5 (5-AI) mg/kg BWdoses and MT at a 5 mg/kg BW (5-MT) dose. At week 7 post-injection, 3-AI and 5-MT oocytes were degenerated, and gonads of the 5-AI group initiated spermatogenesis. At week 21 post-injection, 3-AI- and 5-MT-treated gonads contained spermatogonia and spermatocytes, while 5-AI treatment induced advanced stages of spermatogenesis. The serum E2 level showed no significant differences throughout the experimental period, whereas that of 11-KT was significantly elevated in the 5-AI group at weeks 7 and 21 post-injection. A significant increase in the expression of FSH-${\beta}$ mRNA was evident in the 5-AI group at week 21 post-injection. In contrast, LH-${\beta}$ mRNA expression did not significantly differ among groups during the experimental period. These results imply that sex change has two stages in the longtooth grouper. In the first stage, oocytes are degenerated by the stimulation by 11-KT, and in the second stage spermatogenesis occurs, owing to the co-effects of 11-KT and FSH-${\beta}$.

Histone deacetylase inhibitor, CG200745, attenuates cardiac hypertrophy and fibrosis in DOCA-induced hypertensive rats

  • Lee, Eunjo;Song, Min-ji;Lee, Hae-Ahm;Kang, Seol-Hee;Kim, Mina;Yang, Eun Kyoung;Lee, Do Young;Ro, Seonggu;Cho, Joong Myung;Kim, Inkyeom
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.5
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    • pp.477-485
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    • 2016
  • CG200745 is a novel inhibitor of histone deacetylases (HDACs), initially developed for treatment of various hematological and solid cancers. Because it is water-soluble, it can be administered orally. We hypothesized that the HDAC inhibitor, CG200745, attenuates cardiac hypertrophy and fibrosis in deoxycorticosterone acetate (DOCA)-induced hypertensive rats. For establishment of hypertension, 40 mg/kg of DOCA was subcutaneously injected four times weekly into Sprague-Dawley rats. All the rats used in this study including those in the sham group had been unilaterally nephrectomized and allowed free access to drinking water containing 1% NaCl. Systolic blood pressure was measured by the tail-cuff method. Blood chemistry including sodium, potassium, glucose, triglyceride, and cholesterol levels was analyzed. Sections of the heart were visualized after trichrome and hematoxylin and eosin stain. The expression of hypertrophic genes such as atrial natriuretic peptide A (Nppa) and atrial natriuretic peptide B (Nppb) in addition to fibrotic genes such as Collagen-1, Collagen-3, connective tissue growth factor (Ctgf), and Fibronectin were measured by quantitative real-time PCR (qRT-PCR). Injection of DOCA increased systolic blood pressure, heart weight, and cardiac fibrosis, which was attenuated by CG200745. Neither DOCA nor CG200745 affected body weight, vascular contraction and relaxation responses, and blood chemistry. Injection of DOCA increased expression of both hypertrophic and fibrotic genes, which was abrogated by CG200745. These results indicate that CG200745 attenuates cardiac hypertrophy and fibrosis in DOCA-induced hypertensive rats.