• The Korean Journal of Physiology and Pharmacology
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• v.24 no.6
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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.

• The Korean Journal of Pharmacology
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• v.30 no.1
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• pp.49-57
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• 1994

The binding properties of oxomemazine to muscarinic receptors using the ability of oxomemazine to inhibit $[^3H]QNB$ binding in membrane fractions of rat cerebrum and guinea pig ventricle and ileum were investigated. $[^3H]QNB$ bound to a single class of muscarinic receptors with a dissociation constant of approximately 60 pM in three tissue preparations. Pirenzepine and oxomemazine inhibited $[^3H]QNB$ binding in cerebrum with a Hill coefficient lower than unity, and the inhibition data were best described by a two-site model. The relative densities of the high $(M_1)\;and\;low\;(M_2)$ affinity sites for pirenzepine were 60 and 40%, with corresponding Ki values of 16 and 431 nM, and those $(O_H\;and\;O_L)$ for oxomemazine 40 and 60%, with corresponding Ki values of 80 and 1350 nM. However, the inhibition data of both drugs vs $[^3H]QNB$ in ventricle and ileum appeared to obey the law of mass-action (Hill coefficient close to 1). The apparent Ki values of pirenzepine were 850 and 250 nM, and those of oxomemazine 1460 and 570 nM in ventricle and ileum, respectively. Thus, oxomemazine like pirenzepine has high affinity for cerebrum, moderate affinity for ileum and low affinity for ventricle. These results suggest that oxomemazine could recognize the muscarinic receptor subtypes with a high affinity for the $M_1$ sites.

• Structural Engineering and Mechanics
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• v.61 no.4
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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.

• BMB Reports
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• v.45 no.12
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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.

• Journal of The Korean Society of Grassland and Forage Science
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• v.35 no.3
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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.

• Journal of the Korean Chemical Society
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• v.28 no.3
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• pp.185-193
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• 1984

At the spermine concentration to cover the number of the binding site of spermine 0.016 per nucleotide, the Hill coefficient of the ethidium binding to the calf thymus DNA was 1.7, while the value was 0.38 in the absence of the spermine. On the basis of the data, together with other present data on the viscometric titration of the DNA with spermine and anomalous absorbance-temperature profile at 260nm and viscosity-temperature profile, it can be speculated that allosteric propagation of the conformational transition induced by the binding of the spermine may be involved in the monomolecular collapse of the DNA to a condensed structure.

• Structural Engineering and Mechanics
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• v.52 no.3
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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.

• Journal of The Korean Society of Agricultural Engineers
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• v.58 no.5
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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.

• Journal of the Korea Society of Computer and Information
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• v.24 no.10
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• pp.33-39
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• 2019

In this paper, we propose a parametric model for analyzing the motion information obtained from the acceleration sensors to measure the activity of the human body. The motion of the upper body and the lower body does not occur at the same time, and the motion analysis method using a single motion sensor involves a lot of errors. In this study, the 3-axis accelerometer is attached to the arms and legs, the body's activity data are measured, the momentum of the arms and legs are calculated for each channel, and the linear predictive coefficient is obtained for each channel. The periodicity of the upper body and the lower body is determined by analyzing the correlation between the channels. The linear predictive coefficient and the periodic value are used as data to measure the type of exercise and the amount of exercise. In the proposed method, we measured four types of movements such as walking, stair climbing, slow hill climbing, and fast hill descending. In order to verify the usefulness of the parameters, the recognition results are presented using the linear predictive coefficient and the periodic value for each motion as the neural network input.

• Transactions of the Korean Society of Mechanical Engineers
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• v.7 no.1
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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.