• 제목/요약/키워드: High $K^{+}$-induced contraction

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EFFECT OF A NEW POSITIVE INOTROPIC AGENT, YS-49, A NOVEL TETRAHYDROISOQUINOLINE COMPOUND

  • Lee, Y. S.;Park, H. S. Yoon-;K. C. Chang
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1995년도 춘계학술대회
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    • pp.88-88
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    • 1995
  • Tetrahydroisoquinoline (THI) compounds have various pharmacological actions in the cardiovascular system. Recently, we have synthesized 1-${\alpha}$-naphthylmethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, YS 49. In the present study, we evaluated the effect of YS-49 on positive inotropic and chronotropic action using isolated rat heart and on blood pressure and heart rate using anesthesized rabbit. Vasodilating action was also assessed in isolated rat thoracic aorta. YS 49, concentration-dependently relaxed rat aorta precontracted with phenylephrine (PE, 0.3 ${\mu}$M) and high potassium (high K$\^$+/, 65.4 mM). The 50% inhibitory concentration (IC$\sub$50/) of YS 49 in PE-induced and high K$\^$+/-induded contraction was 5.36 ${\mu}$M and 2.52 ${\mu}$M, respectively. In isolated rat atria, YS 49 increased both heart rate and force, and in anesthesized rabbit it decreased blood pressure but increased heart rate. In addition, to know the mechanism of action of the compound, propranolol, nonselective ${\beta}$-antagonist, and phentolamine, ${\alpha}$-blocker, were used. Furthermore, a comparison with the effect of higenamine, trimetoquinol on the vasodilating action in rat thoracic aorta was also made. The action of YS 49 was inhibited by the presence of propranolo, not pentolamine. These results indicate that cardiotonic and vasodilatory action of YS 49 is attributable, at least in part, for ${\beta}$-receptor stimulation.

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High Pressure Synthesis and Physical Properties of the Solid Solution, $SrLaAl_{1-x}Ni_xO_4(0

  • 변송호
    • Bulletin of the Korean Chemical Society
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    • 제16권11호
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    • pp.1084-1088
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    • 1995
  • A complete solid solution (SrLaAl1-xNixO4) between insulating SrLaAlO4 and metallic SrLaNi(Ⅲ)O4 oxides were prepared under high oxygen pressure (1.5 kbar, 800 ℃). They have tetragonal K2NiF4-type structure in all the solid solution range. Compared with lattice parameters of the same solid solution prepared under normal condition (1 bar, 1200 ℃), large decrease in the c-parameter was induced by high pressure treatment while no noticeable variation of the a-parameter was observed. Although marked changes of structural parameters, magnetic susceptibilities, and electron paramagnetic resonance spectra were consistently occurred before and after x=0.5, overall behaviors were essentially the same with those of solid solution prepared under normal condition. Such a phenomenon is explained by assuming the formation of partially filled narrow σ*x2-y2 band for x>0.5. Lattice contraction along the c-axis by high pressure treatment seems not to broaden this band. Particularly, the continuous absorption characteristic of a high free carrier concentration for x>0.5 and the absence of Ni-O in-plane stretching mode in the infrared absorption spectra supports this picture. However, the conductivities increasing with temperature for all solid solution suggest that some localization character, of probably Anderson type, remains for x>0.5.

전단 자극에 의한 심방 근세포 칼슘 웨이브의 발생: Phospholipase C-이노시톨 1,4,5-삼인산 수용체 신호전달의 역할 (Activation of a Ca2+ wave by Shear Stress in Atrial Myocytes: Role of Phospholipase C-inositol 1,4,5-Trisphosphate Receptor Signaling)

  • 김준철;우선희
    • 약학회지
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    • 제59권4호
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    • pp.158-163
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    • 2015
  • Cardiac myocytes are subjected to fluid shear stress during each contraction and relaxation. Under pathological conditions, such as valve disease, heart failure or hypertension, shear stress in cardiac chamber increases due to high blood volume and pressure. The shear stress induces proarrhythmic longitudinal global $Ca^{2+}$ waves in atrial myocytes. In the present study, we further explored underlying cellular mechanism for the shear stress-induced longitudinal global $Ca^{2+}$ wave in isolated rat atrial myocytes. A shear stress of ${\sim}16dyn/cm^2$ was applied onto entire single myocyte using pressurized fluid puffing. Confocal $Ca^{2+}$ imaging was performed to measure local and global $Ca^{2+}$ signals. Shear stress elicited longitudinally propagating global $Ca^{2+}$ wave (${\sim}80{\mu}m/s$). The occurrence of shear stress-induced atrial $Ca^{2+}$ wave was eliminated by the inhibition of ryanodine receptors (RyRs) or inositol 1,4,5-trisphosphate receptors ($IP_3Rs$). In addition, pretreatment of phospholipase C (PLC) inhibitor U73122, but not its inactive analogue U73343, abolished the generation of longitudinal $Ca^{2+}$ wave under shear stress. Our data suggest that shear-induced longitudinal $Ca^{2+}$ wave may be induced by $Ca^{2+}$-induced $Ca^{2+}$ release through the RyRs which is triggered by $PLC-IP_3R$ signaling in atrial myocytes.

Interaction of Antihistaminics with Muscarinic Receptor (III) - Relationship between binding and functional in vitro data -

  • Lee, Shin-Woong;Park, Young-Joo
    • Archives of Pharmacal Research
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    • 제14권2호
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    • pp.181-187
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    • 1991
  • The muscarinic antagonist 1-[benzilic 4, 4'-$[^3H]$ QUINUCLIDINYL BENZILATE $([^3H]$ QNB) bound to a single class of muscarinic receptors with high affinity in rabbit ileal membranes. The $K_D\;and\;B_{ max}$ values for $([^3H]$ QNB calculated from analysis of saturation isotherms were 52.5 pM AND 154 fmol/mg, respectively. Chlopheniramine (CHP), histamine $H_1$ blocker, increased $K_D$ vlue for $([^3H]$QNB without affecting the binding site concentrations and Hill coefficient. The $K_i$ value of CHP for inhibition of $([^3H]$QNB binding in ileal membranes was 1.44\mu{M}$ and the pseudo-Hill coefficient for CHP was close to unit. In the functional assay carbachol, muscarinic agonist, increased the contractile force of ileum with $ED_{50}$ value of $0.11\mu{M}$. CHP caused the rightward shift of the dose-response curve to carbachol. The $pA_2$ value of CHP determined from Schild analysis of carbacholinduced contraction was 5.77 and the slope was unity indicating competitive antagonism with carbachol. The dissociation constant $(K_i)$ of CHP obtained in competitive experiments with $([^3H]$ QNB was similar to the $K_A$ value (1.69 \mu{M)}$ of CHP as inhibitor of carbachol induced contraction in rabbit ileum. This result suggest that the binding of $H_i$ blocker. CHP, vs $([^3H]$QNB to muscarinic receptors in ileal membranes represents an interaction with a receptor of physiological relevance.

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Amiodarone의 투여로 야기된 간질성 폐 질환의 1례 (A Case of Amiodarone-induced Interstitial Lung Disease)

  • 김병훈;박종원;정진홍;이관호;김영조;심봉섭;이현우
    • Journal of Yeungnam Medical Science
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    • 제11권1호
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    • pp.186-192
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    • 1994
  • 저자들은 Lown grade IVa의 심실성 기외 수축으로 진단 받고, amiodarone을 약 7개월간 투여 받은 환자에서 amiodarone으로 야기된 간질성 폐질환의 1례를 경험하였기에 그 휘기성에 비추어 문헌 고찰과 함께 보고하는 바이다.

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황해에서 발생한 동계 고기압형 기상해일의 기상학적 원인분석: 2005년 12월 21일 사례를 중심으로 (Meteorological Analysis of a Meteo-tsunami caused by a High Pressure System during Winter on the Yellow Sea, South Korea: A Case Study of 21 December 2005)

  • 이호재;김유근;김현수;우승범;김명석
    • 한국환경과학회지
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    • 제25권6호
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    • pp.853-864
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    • 2016
  • Meteo-tsunamis are tsunamis that are typically caused by strong atmospheric instability (e.g., pressure jumps) in low pressure systems, but some meteo-tsunamis in winter can be caused by local atmospheric instability in high pressure systems (e.g., the Siberian High). In this study, we investigated a meteo-tsunami event related to a high pressure system that occurred during winter on the Yellow Sea in 2005. Sea level data from tidal stations were analyed with a high-pass filter, and we also performed synoptic weather analyses by using various synoptic weather data (e.g., surface weather charts) collected during the winter season(DJF) of 2005. A numerical weather model (WRF) was used to analyze the atmospheric instability on the day of the selected event (21 Dec. 2005). On the basis of the results, we suggest that the meteo-tsunami triggered by the high pressure system occurred because of dynamic atmospheric instability induced by the expansion and contraction of the Siberian High.

흰쥐 적출 자궁의 수축 작용과 흰쥐 장관에 있어 칼륨에 의해 활성화되는 칼슘 채널에 대한 Cyclobuxine D의 영향 (Effects of Cyclobuxine D on Drug-Induced Contractions of the Isolated Rat Uterine Muscle and Potassium-Activated Calcium Channels in an Intestinal Smooth Muscle)

  • 권준택;이종화;박영현;조병현;최규홍;김유재;김종배;김정목;김천숙;차영덕;김영석
    • 대한약리학회지
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    • 제24권1호
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    • pp.103-109
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    • 1988
  • Buxus microphylla var. koreana Nakai에 존재 하는 steroidal alkaloid인 cyclobuxine D는 흰쥐에 있어 심박동수 감소 작용, 적출 개구리 심장에서 수축력 감소작용, 토끼 적출 장관에서 acetylcholine과 $Ba^{++}$.에 유발되는 수축에 대한 억제작용 등을 나타낸다고 보고되었다. 본 연구에서는 흰쥐 적출 자궁에서 acetylcholine, oxytocin과 $Ba^{++}$에서 의해 나타나는 수축 작용에 대한 cyclobuxine D의 영향을 관찰하였으며, 또 흰쥐 적출장관에서 칼륨에 의해 활성화되는 칼슘채널에 대한 cyclobuxine D의 작용을 관찰하였다. Cyclobuxine D는 흰쥐 적출 자궁에서 acetylcholine, oxytocin과 $Ba^{++}$에 의해 증가되는 peak tension과 duration을 용량적으로 현저히 억제하였다. Cyclobuxine D는 oxytocin보다 acetylcholine에 의해 나타나는 수축작용에 대해 강하게 작용했다. 흰쥐 적출 장관(ileum)을 Ca을 고갈시킨 Tyrode's 용액에 $40{\sim}50$분 담그고 $Na^+$ 대신 $K^+$로 대체시킨 용액에 10분간 담근 후 1.8 mM $CaCl_2$를 가했을 때 이중적인 근육수축작용이 나타난다(Phasic and tonic increase in tension). Cyclobuxine D $(6.2{\times}10^{-5}\;M)$은 이 두 components를 유의하게 억제하였으며 tonic component가 최대치에 도달했을 때 cyclobuxine D $(3.1{\times}10^{-4}\;M)$을 가하면 근육은 긴장도를 빨리 상실했다. 이 결과는 적출 장관에 있어 칼륨에 의해 활성화되는 칼슘 채널이 cyclobuxine D에 의해 차단되고 있음을 나타낸다. 이상의 결과에서 cyclobuxine D의 흰쥐 적출 자궁에 대한 수축 억제 작용은 voltage-dependent calcium channel 차단에 밀접한 관련이 있는 것으로 사려된다.

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가토 위저에서 Nitric oxide에 의해 매개되는 비-아드레날린 비-콜린성 이완반응 (Non-adrenergic and Non-cholinergic Relaxation Mediated by Nitric Oxide in the Rabbit Gastric Fundus)

  • 홍승철;최지은;한석규;김영미;김남득;박미선;홍은주;김진보
    • 약학회지
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    • 제38권2호
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    • pp.149-157
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    • 1994
  • The role of nitric oxide(NO) as neurotransmitter in non-adrenergic non-cholinergic (NANC) relaxation induced by electrical stimulation has been studied in circular muscle strips of the rabbit gastric fundus. In the presence of atropine and guanethidine, low frequency$(1{\sim}20\;Hz)$ and short trains (5s) of electrical stimulation induced the frequency-dependent relaxations which were not affected by adrenergic and cholinergic blockage, but abolished by tetrodotoxin, a nerve conductance blocker. L-NNA, a stereospecific inhibitor of NO biosynthesis, inhibited the relaxations induced by electrical stimulation but not affected the relaxation to exogenous NO. The effect of L-NNA was prevented by L-arginine, the precursor of the NO biosynthesis, but not by its enantiomer, D-arginine. Exogenous administration of NO$(10{\sim}100\;{\mu}M)$ caused the concentration-dependent relaxation which showed a similarity to those obtained with electrical stimulation. Hemoglobin, a NO scavenger, abolished the NO-induced relaxations and also markedly inhibited those evoked by electrical stimulation. Application of adenosine triphosphate$(1{\sim}10\;{\mu}M)$ induced concentration-independent contractions, but in high dose caused temporary contraction followed by relaxation which was not affected by L-NNA. Exogenous vasoactive intestinal polypeptide$(10{\sim}100\;nM)$ induced the concentration-dependent relaxation, while its effects were slower in onset and more persistent than those induced by short trains and low frequencies of electrical stimulation. Based on above results, it is suggested that NO is the principal neurotransmitter of NANC nerve at relaxation induced by short trains and low frequencies of electrical stimulation in the rabbit gastric fundus.

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MC-CDMA 시스템에서 실수 고정점 반복 기반의 전치왜곡기를 이용한 비선형 왜곡 보상 (Compensation of Nonlinear Distortion Using a Predistorter Based on Real-Valued Fixed Point Iterations in MC-CDMA Systems)

  • 전재현;신요안;임성빈
    • 대한전자공학회논문지TC
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    • 제37권1호
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    • pp.1-11
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    • 2000
  • 본 논문에서는 다중 반송파 부호 분할 다원 접속 (multi-carrier-code division multiple access; MC-CDMA) 시스템 내의 고출력 증폭기에 의해 발생하는 비선형 왜곡의 보상을 위한 전치왜곡기를 제안한다. 제안된 방법은 contraction mapping 정리와 이에 따른 고정점 반복에 기반하고 있다. 우리가 이미 다른 논문에서 제안하였던 고정점 반복 기반의 전치왜곡기가 복소수 변조 신호 자체에 적용되는 것에 반해, 여기서 제안하는 전치왜곡기는 변조 신호의 진폭에 고정점 반복을 적용하여 실수 연산을 수행하므로써 계산량을 감소시킨다. 송신기에서 traveling wave tube amplifier를 고출력 증폭기로 사용하고, BPSK 변조와 64개의 부반송파를 이용하는 동기식 MC-CDMA 기저대역 시스템에 대한 컴퓨터 시뮬레이션 결과, 제안된 전치왜곡기를 사용하는 경우 그렇지 않은 경우에 비해 비트오율 및 total degradation의 측면에서 월등한 성능 향상이 가능함을 알 수 있었다. 또한, 작은 output back-off 레벨에 대해 제안된 전치왜곡기는 복소수 연산을 수행하는 기존의 공점점 반복 기반의 전치왜곡기보다 우수한 성능을 보임을 역시 확인하였다.

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SB-31$\circledR$의 일반약리작용 (General Pharmacology of SB-31$\circledR$)

  • 박우규;천혜경;권경자;윤여생;신화섭;공재양
    • Biomolecules & Therapeutics
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    • 제5권4호
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    • pp.369-375
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    • 1997
  • General pharmacological effects of SB-31$^{R}$, the extracts of Pulsatilla koreana, were investigated in mice, rats and guinea-pigs. Intravenous injection of SB-31 (3 and 6 ml/kg) produced almost no effect on central nervous system no effects on the general symptom and behaviors of mice, spontaneous locomotor activity, pentobarbital- induced sleeping time , rotared performance , electroshock and pentylenetertrazole -induced seizures, acetic acid-induced writhing and normal body temperature in mice. SB-31 showed little effects on the spontaneous movement of the isolated ileum and contraction induced by agonists in isolated ileum, suggesting no influence on autonomic nervous system. Administration of SB-31 also did not show any effect on blood pressure in conscious rats. However, a slight decrease in heart rate was observed at high doses (6 and 10 ml/kg) of SB-31 in conscious rats. Similarly, a slight increase in respiratory rate was observed at 6 m1/kg of SB-31 in anesthetized rats. SB-31 did not produce any effect at the dose of 3 ml/kg, but showed a tendency to increase the urinary volume at 6 ml/kg, and produced a decrease in urinary excretions of N $a_{+}$and $K_{+}$at 6 ml/kg. However, transport capacity within the gastrointestinal tract and the secretion of the gastric juice were not influenced by 6 ml/kg of SB-31. In conclusion, these results suggest that SB-31 did not pro-duce any acute effects on the central nervous system, autonomic nervous system, respiratory and circulatory systems, digestive system and kidney function at the dose of below 3 ml/kg.ml/kg.

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