• 제목/요약/키워드: Hill coefficient

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Open channel block of Kv1.4 potassium channels by aripiprazole

  • Park, Jeaneun;Cho, Kwang-Hyun;Lee, Hong Joon;Choi, Jin-Sung;Rhie, Duck-Joo
    • The Korean Journal of Physiology and Pharmacology
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    • 제24권6호
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    • pp.545-553
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    • 2020
  • Aripiprazole is a quinolinone derivative approved as an atypical antipsychotic drug for the treatment of schizophrenia and bipolar disorder. It acts as with partial agonist activities at the dopamine D2 receptors. Although it is known to be relatively safe for patients with cardiac ailments, less is known about the effect of aripiprazole on voltage-gated ion channels such as transient A-type K+ channels, which are important for the repolarization of cardiac and neuronal action potentials. Here, we investigated the effects of aripiprazole on Kv1.4 currents expressed in HEK293 cells using a whole-cell patch-clamp technique. Aripiprazole blocked Kv1.4 channels in a concentration-dependent manner with an IC50 value of 4.4 μM and a Hill coefficient of 2.5. Aripiprazole also accelerated the activation (time-to-peak) and inactivation kinetics. Aripiprazole induced a voltage-dependent (δ = 0.17) inhibition, which was use-dependent with successive pulses on Kv1.4 currents without altering the time course of recovery from inactivation. Dehydroaripiprazole, an active metabolite of aripiprazole, inhibited Kv1.4 with an IC50 value of 6.3 μM (p < 0.05 compared with aripiprazole) with a Hill coefficient of 2.0. Furthermore, aripiprazole inhibited Kv4.3 currents to a similar extent in a concentration-dependent manner with an IC50 value of 4.9 μM and a Hill coefficient of 2.3. Thus, our results indicate that aripiprazole blocked Kv1.4 by preferentially binding to the open state of the channels.

Oxomemazine의 Muscarinic Receptor Subtypes에 대한 결합성질 (Binding Profiles of Oxomemazine to the Muscarinic Receptor Subtypes)

  • 이신웅;김정구
    • 대한약리학회지
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    • 제30권1호
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    • pp.49-57
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    • 1994
  • Oxomemazine이 muscarinic receptor subtypes에 대하여 선택성을 가지는지에 관한 지견을 얻고자, 대뇌, 심실 및 회장 muscarinic receptor에 대한 oxomemazine의 결합성질을 조사, 비교하였다. $[^3H]QNB$ 포화결합실험 결과 세 조직의 muscarinic receptor는 $[^3H]QNB$에 대해서는 affinity가 약 60pM인 단일 receptor인 것으로 추정되었다. 대뇌에서 pirenzepine과 oxomemazine의 $[^3H]QNB$ 결합억제에 대한 Hill coefficient는 각각 0.67 및 0.8로서 대뇌에는 이들 약물에 대하여 affinity가 서로 다른 두 종류의 muscarinic receptor subtypes가 존재하는 것으로 나타났으며, pirenzepine에 대한 high $affinity(M_1)$$low affinity(M_2)$ receptor 및 oxomemazine에 대한 high $affinity(O_H)$$low\;affinity (O_L)$ receptor의 분포비는 약 60:40 및 40:60이었고, $M_1$$M_2$ receptor에 대한 pirenzepine의 $K_i$치는 16nM 및 431 nM, $O_H$$O_L$, receptor에 대한 oxomemazine 의 $K_i$치는 80nM 및 1350nM이었다. 그러나 심실과 회장에서 이들 약물의 $[^3H]QNB$ 결합억제에 대한 Hill coefficient는 1에 가까웠다. 심실과 회장 muscarinic receptor에 대한 pirenzepine의 $K_i$치는 850nM 및 250nM, oxomemazine의 $K_i$치는 1460nM 및 670nM로서 대피에서 이들 약물의 low affinity receptor에 대한 $K_i$치에 가까웠다. 즉, muscarinic receptor에 대한 affinity면에서 oxomemazine은 pirenzepine과 같이 대뇌에서 가장 높았으며, 회장에 대해서는 중등도였고, 심실에서 가장 낮았다. 이로 보아 oxomemazine은 $M_1\;receptor$에 선택성이 있는 것으로 추정된다.

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Auto-parametric resonance of framed structures under periodic excitations

  • Li, Yuchun;Gou, Hongliang;Zhang, Long;Chang, Chenyu
    • Structural Engineering and Mechanics
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    • 제61권4호
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    • pp.497-510
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    • 2017
  • A framed structure may be composed of two sub-structures, which are linked by a hinged joint. One sub-structure is the primary system and the other is the secondary system. The primary system, which is subjected to the periodic external load, can give rise to an auto-parametric resonance of the second system. Considering the geometric-stiffness effect produced by the axially internal force, the element equation of motion is derived by the extended Hamilton's principle. The element equations are then assembled into the global non-homogeneous Mathieu-Hill equations. The Newmark's method is introduced to solve the time-history responses of the non-homogeneous Mathieu-Hill equations. The energy-growth exponent/coefficient (EGE/EGC) and a finite-time Lyapunov exponent (FLE) are proposed for determining the auto-parametric instability boundaries of the structural system. The auto-parametric instabilities are numerically analyzed for the two frames. The influence of relative stiffness between the primary and secondary systems on the auto-parametric instability boundaries is investigated. A phenomenon of the "auto-parametric internal resonance" (the auto-parametric resonance of the second system induced by a normal resonance of the primary system) is predicted through the two numerical examples. The risk of auto-parametric internal resonance is emphasized. An auto-parametric resonance experiment of a ${\Gamma}$-shaped frame is conducted for verifying the theoretical predictions and present calculation method.

Rationalization of allosteric pathway in Thermus sp. GH5 methylglyoxal synthase

  • Zareian, Shekufeh;Khajeh, Khosro;Pazhang, Mohammad;Ranjbar, Bijan
    • BMB Reports
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    • 제45권12호
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    • pp.748-753
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    • 2012
  • A sequence of 10 amino acids at the C-terminus region of methylglyoxal synthase from Escherichia coli (EMGS) provides an arginine, which plays a crucial role in forming a salt bridge with a proximal aspartate residue in the neighboring subunit, consequently transferring the allosteric signal between subunits. In order to verify the role of arginine, the gene encoding MGS from a thermophile species, Thermus sp. GH5 (TMGS) lacking this arginine was cloned with an additional 30 bp sequence at the 3'-end and then expressed in form of a fusion TMGS with a 10 residual segment at the C-terminus ($TMGS^+$). The resulting recombinant enzyme showed a significant increase in cooperativity towards phosphate, reflected by a change in the Hill coefficient (nH) from 1.5 to 1.99. Experiments including site directed mutagenesis for Asp-10 in TMGS and $TMGS^+$, two dimentional structural survey, fluorescence and irreversible thermoinactivation were carried out to confirm this pathway.

Mapping Herbage Biomass on a Hill Pasture using a Digital Camera with an Unmanned Aerial Vehicle System

  • Lee, Hyowon;Lee, Hyo-Jin;Jung, Jong-Sung;Ko, Han-Jong
    • 한국초지조사료학회지
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    • 제35권3호
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    • pp.225-231
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    • 2015
  • Improving current pasture productivity by precision management requires practical tools to collect site specific pasture biomass data. Recent developments in unmanned aerial vehicle (UAV) technology provide cost effective and real time applications for site specific data collection. For the mapping of herbage biomass (BM) on a hill pasture, we tested a UAV system with digital cameras (visible and near-infrared (NIR) camera). The field measurements were conducted on the grazing hill pasture at Hanwoo Improvement Office, Seosan City, Chungcheongnam-do Province, Korea on May 17 and June 27, 2014. Plant samples were obtained from 28 sites. A UAV system was used to obtain aerial photos from a height of approximately 50 m (approximately 30 cm spatial resolution). Normalized digital number (DN) values of Red and NIR channels were extracted from the aerial photos and a normalized differential vegetation index using DN ($NDVI_{dn}$) was calculated. The results show that the correlation coefficient between BM and $NDVI_{dn}$ was 0.88. For the precision management of hilly grazing pastures, UAV monitoring systems can be a quick and cost effective tool to obtain site-specific herbage BM data.

Spermine에 依한 Ethidium의 Calf Thymus DNA와의 結合 Cooperativity 變化 (Change in the Binding Cooperativity of Ethidium with Calf Thymus DNA, Induced by Spermine Binding)

  • 고동성;허준;이찬용
    • 대한화학회지
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    • 제28권3호
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    • pp.185-193
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    • 1984
  • 송아지 胸線 DNA의 nucleotide 당 spermine 0.016 분자의 비율로 結合되는 spermine 濃度에서 그 DNA와 ethidium과의 結合에 對한 Hill 係數는 1.7인 反面에 spermine이 存在하지 않는 條件에서는 그 Hill 係數가 0.38이었다. Spermine에 依한 DNA의 viscometric titration data, 260nm에서의 anomalous absorbance-temperature profile 및 粘性度-溫度 樣相과 더불어 이 data를 基礎로 하여 spermine 結合에 依하여 誘發되는 conformational transition의 allosteric propagation이 DNA의 凝縮된 構造로의 單分子的 collapse에 관여됨을 豫測할 수 있다.

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Moment Lyapunov exponents of the Parametrical Hill's equation under the excitation of two correlated wideband noises

  • Janevski, Goran;Kozic, Predrag;Pavlovic, Ivan
    • Structural Engineering and Mechanics
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    • 제52권3호
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    • pp.525-540
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    • 2014
  • The Lyapunov exponent and moment Lyapunov exponents of Hill's equation with frequency and damping coefficient fluctuated by correlated wideband random processes are studied in this paper. The method of stochastic averaging, both the first-order and the second-order, is applied. The averaged $It\hat{o}$ differential equation governing the pth norm is established and the pth moment Lyapunov exponents and Lyapunov exponent are then obtained. This method is applied to the study of the almost-sure and the moment stability of the stationary solution of the thin simply supported beam subjected to time-varying axial compressions and damping which are small intensity correlated stochastic excitations. The validity of the approximate results is checked by the numerical Monte Carlo simulation method for this stochastic system.

노지 작물의 적정 관개계획을 위한 토양수분의 공간변이성 분석 (Spatial Variability of Soil Moisture and Irrigation Scheduling for Upland Farming)

  • 최용훈;김민영;김영진;전종길;서명철
    • 한국농공학회논문집
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    • 제58권5호
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    • pp.81-90
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    • 2016
  • Due to droughts and water shortages causing severe damage to crops and other vegetations, much attention has been given to efficient irrigation for upland farming. However, little information has been known to measure soil moisture levels in a field scale and apply their spatial variability for proper irrigation scheduling. This study aimed to characterize the spatial variability and temporal stability of soil water contents at depths of 10 cm, 20 cm and 30 cm on flat (loamy soil) and hill-slope fields (silt-loamy soil). Field monitoring of soil moisture contents was used for variogram analysis using GS+ software. Kriging produced from the structural parameters of variogram was applied for the means of spatial prediction. The overall results showed that the surface soil moisture presented a strong spatial dependence at the sampling time and space in the field scale. The coefficient variation (CV) of soil moisture was within 7.0~31.3 % in a flat field and 8.3~39.4 % in a hill-slope field, which was noticeable in the dry season rather than the rainy season. The drought assessment analysis showed that only one day (Dec. 21st) was determined as dry (20.4 % and 24.5 % for flat and hill-slope fields, respectively). In contrary to a hill-slope field where the full irrigation was necessary, the centralized irrigation scheme was appeared to be more effective for a flat field based on the spatial variability of soil moisture contents. The findings of this study clearly showed that the geostatistical analysis of soil moisture contents greatly contributes to proper irrigation scheduling for water-efficient irrigation with maximal crop productivity and environmental benefits.

Extraction of Motion Parameters using Acceleration Sensors

  • Lee, Yong-Hee;Lee, Kang-Woo
    • 한국컴퓨터정보학회논문지
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    • 제24권10호
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    • pp.33-39
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    • 2019
  • 본 논문에서는 인체의 활동량을 측정하기 위해 가속도 센서로 부터 얻은 운동신호를 파라미터로 모델링 하는 방법을 제안한다. 상체와 하체의 움직임이 동시에 일어나지 않는 경우, 현재의 단체널 방식의 운동량 분석방법은 많은 오차를 수반하게 된다. 본 연구에서는 3축 가속도 센서를 팔과 다리에 부착하고 인체의 활동을 측정한 후, 각 채널 별로 팔과 다리의 운동량을 계산하고, 채널별로 선형예측계수를 얻는다. 또한, 상체와 하체운동간의 교차상관도를 측정함으로써 상체와 하체의 주기성을 판단하게 된다. 선형예측계수와 주기 값은 운동의 종류와 이에 따른 운동량을 측정하는 자료로 이용하게 된다. 결과에서 제안한 방법의 유효성을 확인하기 위해 계단내려가기, 계단오르기, 언덕오르기, 언덕내려가기 등의 4가지 운동을 측정하여, 제시한 파라미터 모델의 유용성을 확인한다.

알루미늄薄板 의 Stretch Forming 에 관한 硏究 (A Study on the Pure Stretch Forming Of Al Sheet)

  • 김동원;권인소
    • 대한기계학회논문집
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    • 제7권1호
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    • pp.64-72
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    • 1983
  • A method of numerical analysis is proposed for the pure stretch forming of A1 sheet by hemi-spherical punch. The analysis is performed by Woo's general method under the condition of variable friction and plastic yielding is based on the new anisotropic yield function proposed by Hill. A comparison of the calculated results with experiment shows good agreement for various lubrication when the initial values of the coefficient of coulomb friction at pole are less than 0.4.