• Title/Summary/Keyword: Channel Blocking

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Calcium Channel Blocking and Phosphodiesterase Inhibitory Action of GS386, a Dihydroisoquinoline Derivative, in Isolated Rat Trachea (흰쥐 기관평활근에 대한 GS 386의 칼슘억제 및 포스포디에스테라제 억제 작용)

  • Chang, Ki-Churl;Lee, Hoi-Young;Kang, Young-Jin;Koo, Eui-Bon
    • The Korean Journal of Pharmacology
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    • v.32 no.3
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    • pp.373-380
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    • 1996
  • Recently we reported that GS 386, 1-(4'-methoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinoline, inhibited amplitude of the $Ca^{2+}$ current by reducing the probability of $Ca^{2+}$ channel opening without changing channel kinetics in isolated rabbit atrial myocyte. In the present study, further investigation of the mechanism of action of GS 386 was performed using isolated rat trachealis. GS 386 concentration-dependently relaxed rat trachealis contracted by carbachol $(0.3{\mu}M)$ and high $K^+$(65.4 mM) with $IC_{50}$ 5.24 and 5.67 ${\mu}M$, respectively. Verapamil inhibited more effectively the high $K^+-contracted$ tissues than those with carbachol in the rat trachealis muscle. In $Ca^{2+}-free$ media, $Ca^{2+}-induced$ contraction was inhibited by GS 386. Furthermore, high concentration of GS 386 $(100{\mu}M)$ but not verapamil, attenuated a phasic contraction induced not only by carbachol but also caffeine, indicating that GS386 can enter into the cytoplasm where it may exert secondary actions on internal sites of the muscle, such as sarcoplasmic reticulum. Moreover, GS 386 showed verapamil-resistant component of relaxation and increased cAMP levels in rat trachal smooth muscle. These results suggest that the mechanism of action of GS 386 attributes to not only $Ca^{2+}$ antagonistic action but also weak phosphodiesterase inhibitory action.

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A Study on Stability of Levee Revetment in Meandering Channel (만곡수로 내의 호안 안정성 연구)

  • Kim, Sooyoung;Yoon, Kwang Seok;Kim, Hyung-Jun
    • Journal of Korea Water Resources Association
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    • v.48 no.12
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    • pp.1077-1087
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    • 2015
  • The levee protect lifes, houses, and properties by blocking overflow of river. The revetment is forced to be covered on the slope of levee in order to prevent erosion. The stability of revetment is very important enough to directly connected to the stability of levee. In this study, the weak points of revetment on meandering channel were found by movable revetment experiment and the velocity and the water surface elevation (WSE) were measured at main points. The 3-D numerical simulations were performed under same conditions with experiment. And unclear flow characteristics by the limit of measuring instruments were analyzed through numerical simulation. Consequently, the section of large wall shear stress and the failure section are almost the same. Despite of small wall shear stress, the revetments located at right bank were carried away because of circulation zone due to secondary flow by meandering. With existing riprap design formula, the sizes of riprap determined using maximum local velocity were 1.5~4.7 times greater than them using mean velocity. As a result of this study, it is necessary to calculate the size of riprap in other ways for meandering and straight channel. At a later study, if the weighted value considered the radius of curvature and shape of hydraulic structure is applied to riprap design formula, it is expected that the size of revetment was evaluated rationally and accurately.

The Antioxidant Activities and Hair-growth Promotion Effects of Tenebrio molitor Larvae Extracts (TMEs) (갈색거저리 유충 추출물의 항산화 활성 및 모발 성장 촉진 효과)

  • Baek, Minhee;Seo, Minchul;Kim, Mi-Ae;Yun, Eun-Young;Hwang, Jae-Sam
    • Journal of Life Science
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    • v.27 no.11
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    • pp.1269-1275
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    • 2017
  • Tenebrio molitor samples were investigated as novel biomaterials and sources of food in several recent studies. However, the insects' effects on hair growth were not sufficiently researched. To develop novel and natural materials for preventing alopecia and promoting hair growth, this study investigated the antioxidant activities and hair-growth promotion effects of TMEs. To determine the antioxidant activities, the TMEs' DPPH radical- and nitrite-scavenging activities were examined. To determine hair-growth promotion effects, proliferations of human dermal papilla cells (DPCs) and the murine fibroblast cell line NIH3T3 were evaluated by using an MTS assay. In addition, estimations were made for cell viabilities against cell death induced by dihydrotesterone (DHT) in DPCs and inhibitory effects against potassium channel blocking induced by tolbutamide (TBM) in NIH3T3 cells. The DPPH radical scavenging activity was 81.17%, and the nitrite scavenging activity was 43.69%; the activities were similar to the activities of blueberry extracts. Moreover, the TMEs promoted the proliferation of human DPCs and NIH3T3 cells, which were concentrated dependently. The TMEs prevented not only DHT-induced DPC cytotoxicity but also TBM's action as a potassium channel blocker in NIH3T3 cells. The results suggested that TME could be used as a functional therapeutic alopecia reagent, to prevent hair loss and to promote hair growth.

Effect of ATP on Calcium Channel Modulation in Rat Adrenal Chromaffin Cells (흰쥐 부신 크로마핀 세포 칼슘통로 조절에 미치는 ATP의 효과)

  • Kim, Kyung Ah;Goo, Yong Sook
    • Progress in Medical Physics
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    • v.25 no.3
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    • pp.157-166
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    • 2014
  • ATP in quantity co-stored with neurotransmitters in the secretory vesicles of neurons, by being co-released with the neurotransmitters, takes an important role to modulate the stimulus-secretion response of neurotransmitters. Here, in this study, the modulatory effect of ATP was studied in $Ca^{2+}$ channels of cultured rat adrenal chromaffin cells to investigate the physiological role of ATP in neurons. The $Ca^{2+}$ channel current was recorded in a whole-cell patch clamp configuration, which was modulated by ATP. In 10 mM $Ba^{2+}$ bath solution, ATP treatment (0.1 mM) decreased the $Ba^{2+}$ current by an average of $36{\pm}6%$ (n=8), showing a dose-dependency within the range of $10^{-4}{\sim}10^{-1}mM$. The current was recovered by ATP washout, demonstrating its reversible pattern. This current blockade effect of ATP was disinhibited by a large prepulse up to +80 mV, since the $Ba^{2+}$ current increment was larger when treated with ATP ($37{\pm}5%$, n=11) compared to the control ($25{\pm}3%$, n=12, without ATP). The $Ba^{2+}$ current was recorded with $GTP{\gamma}S$, the non-hydrolyzable GTP analogue, to determine if the blocking effect of ATP was mediated by G-protein. The $Ba^{2+}$ current decreased down to 45% of control with $GTP{\gamma}S$. With a large prepulse (+80 mV), the current increment was $34{\pm}4%$ (n=19), which $25{\pm}3%$ (n=12) under control condition (without $GTP{\gamma}S$). The $Ba^{2+}$ current waveform was well fitted to a single-exponential curve for the control, while a double-exponential curve best fitted the current signal with ATP or $GTP{\gamma}S$. In other words, a slow activation component appeared with ATP or $GTP{\gamma}S$, which suggested that both ATP and $GTP{\gamma}S$ caused slower activation of $Ca^{2+}$ channels via the same mechanism. The results suggest that ATP may block the $Ca^{2+}$ channels by G-protein and this $Ca^{2+}$ channel blocking effect of ATP is important in autocrine (or paracrine) inhibition of adrenaline secretion in chromaffin cell.

Analysis of abnormal traffic controller based on prediction to improve network service survivability (네트워크 서비스의 생존성을 높이기 위한 예측기반 이상 트래픽 제어 방식 분석)

  • Kim Kwang sik
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.30 no.4C
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    • pp.296-304
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    • 2005
  • ATCoP(Abnormal traffic controller based on prediction) is presented to securely support reliable Internet service and to guarantee network survivability, which is deployed in Internet access point. ATCoP is a method to control abnormal traffic that is entering into the network When unknown attack generates excessive traffic, service survivability is guaranteed by giving the priority to normal traffic than abnormal traffic, that is reserving some channels for normal traffic. If the reserved channel number increases, abnormal traffic has lower quality service by ATCoP system and then its service survivability becomes worse. As an analytic result, the proposed scheme maintains the blocking probability of normal traffic on the predefined level in the specific interval of input traffic.

Shape Selective Catalysis of Cation-Exchanged Pentasil Zeolites (양이온 교환된 펜타실 제올라이트의 형상 선택적 촉매작용)

  • Byoung Joon Ahn;Byung Woo Hwang;Hakze Chon
    • Journal of the Korean Chemical Society
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    • v.28 no.1
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    • pp.62-69
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    • 1984
  • The reaction of toluene with ethanol was studied over various cation-exchanged pentasil zeolite catalysts. The toluene disproportionation reaction to produce xylenes increased with increasing reaction temperature and the activity of alkylation of toluene with ethanol showed maximum at around $400^{\circ}C$. Only Cs-ZSM-5 catalyst showed pronounced p-ethyltoluene selectivity increasing to 96% with increasing degree of Cs-exchange. The sorption rate of m-xylene was lower for Cs-exchanged ZSM-5 than H-ZSM-5 catalyst. These phenomena were interpreted in terms of shape selectivity arising from the partial blocking of channel intersections by large cesium ions.

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Development of a Synthetic Multi-Agent System;The KMITL Cadence 2003 Robotic Soccer Simulation Team, Intelligent and AI Based Control

  • Chitipalungsri, Thunyawat;Jirawatsiwaporn, Chawit;Tangchupong, Thanapon;Kittitornkun, Surin
    • 제어로봇시스템학회:학술대회논문집
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    • 2004.08a
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    • pp.879-884
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    • 2004
  • This paper describes the development of a synthetic multi-agent called KMITL Cadence 2003. KMITL Cadence 2003 is a robotic soccer simulation team consisting of eleven autonomous software agents. Each agent operates in a physical soccer simulation model called Robocup Soccer Server which provides fully distributed and real-time multi-agent system environment. All teammates have to cooperate to achieve the common goal of winning the game. The simulation models many aspects of the football field such as noise in ball movements, noisy sensors, unreliable communication channel between teammates and actuators, limited physical abilities and restricted communication. This paper addresses the algorithm to develop the soccer agents to perform basic actions which are scoring, passing ball and blocking the opponents effectively. The result of this development is satisfactory because the successful scoring attempts is increased from 11.1% to 33.3%, successful passing ball attempts is increased from 22.08% to 63.64%, and also, successful intercepting attempts is increased from 88% to 97.73%.

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Anti-interference Methods using Vector-based GPS Receiver Mode

  • Viet, Hoan Nguyen;Lee, Suk-Hwan;Kwon, Ki-Ryong
    • Journal of Korea Multimedia Society
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    • v.21 no.5
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    • pp.545-557
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    • 2018
  • The Global Positioning System (GPS) has become popular and widely used in many fields from military to civilian applications. However, GPS signals are suffered from interference due to its weak signal over wireless channel. There are many types of interference, such as jamming, blocking multipath, and spoofing, which can mislead the operation of GPS receiver. In this paper, vector-based tracking loop model with integrity check is proposed to detect and mitigate the harmful effect of interference on GPS receiver operation. The suggested methods are implemented in the tracking loop of GPS receiver. As a first method, integrity check with carrier-to-noise ratio (C/No) monitoring technique is applied to detect the presence of interference and prevent contaminated channels out of tracking channels to calculate position. As a second method, a vector-based tracking loop using Extended Kalman Filter with adaptive noise covariance according to C/No monitoring results. The proposed methods have been implemented on simulated dataset. The results demonstrates that the suggested methods significantly mitigate interference of Additive White Gaussian Noise (AWGN) and improve position calculation by 44%.

Enhancement of Nitrendipine Bioavailability in Rats by its Solid Dispersion with $Hydroxypropyl-{\beta}-Cyclodextrin$ after Oral Administration (흰쥐에 경구 투여시 히드록시프로필-베타-시클로덱스트린과 니트렌디핀 고체분산에 의한 생체이용률 증가)

  • Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.27 no.4
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    • pp.295-301
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    • 1997
  • Nitrendipine, a slightly soluble calcium channel blocking agent forms a solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$, which exhibits better dissolution characteristics than the uncomplexed drug. The dissolution rate of nitrendipine was markedly increased in solid dispersion system in pharmacopeial disintegration media at pH 1.2 and pH 6.8. Four different dosage forms of nitrendipine were administered to rats: (a) nitrendipine in the solution of PEG 400; (b) nitrendipine solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 by solvent evaporation method and administered in capsule form; (c) physical mixture of nitrendipine with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 and administered in capsule form; (d) nitrendipine alone administered in capsule form. Relative bioavailability after the oral administration of various dosage forms to rats with a dose of 10 mg/kg equivalent to nitrendipine was compared with that of nitrendipine in the solution of PEG 400. The AUC of solid dispersion was significantly bigger than that of nitrendipine powder. $T_{max}$ of solid dispersion was significantly shorter and $C_{max}$ was higher than that of nitrendipine powder. These results indicate that the bioavailability of nitrendipine could be improved markedly by inclusion complexation. An interesting correlation also appears to exist between the in vitro dissolution data and the area under the plasma concentration-time curves.

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Distributed Subchannel ON/OFF Scheduling by using Load Distribution for Cellular Femto Systems (셀룰러 펨토 시스템에서 부하 분산을 통한 분산적 부채널 ON/OFF 스케쥴링 기법)

  • Yoon, Kang-Jin;Kim, Young-Yong
    • Journal of Advanced Navigation Technology
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    • v.16 no.3
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    • pp.471-479
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    • 2012
  • In cellular femto systems, femto Base stations(f-BSs) can be installed unnecessarily and overcrowded in small areas. This will cause an interference problem and it can impact on the capacity, blocking probability, and coverage of femtocells in the shared channel systems. In this paper, we propose a load distribution scheme by using forced handover and probabilistic subchannel scheduling policy to resolve the problem. The proposed scheme operates in distributed manner though communication with neighboring f-BSs, and includes self-detection of overcrowded area and radio resource management based on measurements. We evaluate the performance of the proposed scheme in terms of average cell throughput and average throughput per users.