• 제목/요약/키워드: Source-receptor

검색결과 196건 처리시간 0.026초

Rat Liver $AT_1$ Receptor Binding Analysis for Drug Screening

  • Lee, Sunghou;Lee, Buyean;Hwasup Shin;Jaeyang Kong
    • Biomolecules & Therapeutics
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    • 제3권1호
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    • pp.21-27
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    • 1995
  • The only compounds with antagonistic activity via AT$_1$receptor, one of two subtypes of angiotensin II (AII) receptor, have been demonstrated to block the vasoconstriction effects of AII and thereby provide therapeutic potential. This initiated the search for compounds with high specific affinity to AT$_1$receptor and their effective screening methods. The radioligand binding assay for the AII receptor is regarded as the primary method for the evaluation of AT$_1$receptor antagonists for their activity. In this paper, we characterized the liver AT$_1$receptor and describe the efficient method of the radioligand binding assay using rat liver as a source of AT$_1$receptor. Equilibrium binding studies with rat adrenal cortex, adrenal medulla, liver and bovine adrenal showed that the specific bindings of [$^3$H] AII were saturable in all tissues and the Scatchard plots of those data were linear, suggesting a single population of binding sites. Hill slopes were very near to the unity in all tissues. Kinetic studies of [$^3$H) AII binding in rat liver homogenates yielded two association rate constants, 4.10$\times$10$^{7}$ M$^{-1}$ min$^{-1}$ and 4.02$\times$10$^{9}$ M$^{-1}$ min$^{-1}$ , with a single dissociation rate constant, 7.07$\times$10$^{-3}$ min-$^{-1}$ , possibly due to the partial dissociation phenomenon. The rank order of inhibition potencies of [$^3$H] AII binding in rat liver was AII>Sarile>Losartan>PD 123177. Rat liver homogenates revealed to have very high density of homogeneous population of the AT$_1$receptor subtype, as the specifically bound [$^3$H] AII was not inhibited by PD 123177, the nonpeptide antagonist of AT$_2$. The results of this study demonstrated that the liver homogenates from rats could be the best receptor preparation for the AT$_1$receptor binding assay and provide an efficient system for the screening of newly synthesized candidate compounds of AT$_1$receptor antagonist.

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Action of Mitochondrial Substrates on Neuronal Excitability in Rat Substantia Gelatinosa Neurons

  • Lee, Hae In;Chun, Sang Woo
    • International Journal of Oral Biology
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    • 제42권2호
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    • pp.55-61
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    • 2017
  • Recent studies indicate that mitochondria are an important source of reactive oxygen species (ROS) in the spinal dorsal horn. In our previous study, application of malate, a mitochondrial electron transport complex I substrate, induced a membrane depolarization, which was inhibited by pretreatment with ROS scavengers. In the present study, we used patch clamp recording in the substantia geletinosa (SG) neurons of spinal slices, to investigate the cellular mechanism of mitochondrial ROS on neuronal excitability. DNQX (an AMPA receptor antagonist) and AP5 (an NMDA receptor antagonist) decreased the malate-induced depolarization. In an external calcium free solution and addition of tetrodotoxin (TTX) for blockade of synaptic transmission, the malate-induced depolarization remained unchanged. In the presence of DNQX, AP5 and AP3 (a group I metabotropic glutamate receptor (mGluR) antagonist), glutamate depolarized the membrane potential, which was suppressed by PBN. However, oligomycin (a mitochondrial ATP synthase inhibitor) or PPADS (a P2 receptor inhibitor) did not affect the substrates-induced depolarization. These results suggest that mitochondrial substrate-induced ROS in SG neuron directly acts on the postsynaptic neuron, therefore increasing the ion influx via glutamate receptors.

PMF모델을 이용한 용인.수원 경계지역에서 PM10 오염원의 확인과 상대적 기여도의 추정 (Identification of Atmospheric PM10 Sources and Estimating Their Contributions to the Yongin-Suwon Bordering Area by Using PMF)

  • 이형우;이태정;양성수;김동술
    • 한국대기환경학회지
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    • 제24권4호
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    • pp.439-454
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    • 2008
  • The purpose of this study was to extensively identify $PM_{10}$ sources and to estimate their contributions to the study area, based on the analysis of the $PM_{10}$ mass concentration and the associated inorganic elements, ions, and total carbon. The contribution of $PM_{10}$ sources was estimated by applying a receptor method because identifying air emission sources were effective way to control the ambient air quality. $PM_{10}$ particles were collected from May to November 2007 in the Yongin-Suwon bordering area. $PM_{10}$ samples were collected on quartz filters by a $PM_{10}$ high-volume air sampler. The inorganic elements (Al, Mn, V, Cr, Fe, Ni, Cu, Zn, Cd, Pb, Si, Ba, Ti and Ag) were analyzed by an ICP-AES after proper pre-treatments of each sample. The ionic components of these $PM_{10}$ samples ($Cl^_$, $NO_3^-$, $SO_4^{2-}$, $Na^+$, $NH_4^+$, $K^+$, $Ca^{2+}$, and $Mg^{2+}$) were analyzed by an IC. The carbon components (OC1, OC2, OC3, OC4, OP, EC1, EC2 and EC3) were also analyzed by DRI/OGC analyzer. Source apportionment of $PM_{10}$ was performed using a positive matrix factorization (PMF) model. After performing PMF modeling, a total of 8 sources were identified and their contribution were estimated. Contributions from each emission source were as follows: 13.8% from oil combustion and industrial related source, 25.4% from soil source, 22.1% from secondary sulfate, 12.3% from secondary nitrate, 17.7% from auto emission including diesel (12.1%) and gasoline (5.6%), 3.1% from waste incineration and 5.6% from Na-rich source. This study provides information on the major sources affecting air quality in the receptor site, and therefore it will help us maintain and manage the ambient air quality in the Yongin-Suwon bordering area by establishing reliable control strategies for the related sources.

Near Fields around Metallic Walls due to a Nearby Dipole Source with Applications to EMC

  • Kim, Ki-Chai;Lim, Sung Min;Kim, Jong-Woo
    • Journal of Electrical Engineering and Technology
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    • 제12권1호
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    • pp.329-334
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    • 2017
  • This paper discusses the near field characteristics of a dipole source located near conducting metallic walls from an electromagnetic compatibility (EMC) point of view. An integral equation for a dipole source near a metallic wall is derived and solved by applying Galerkin's method of moments (MoM). The results show that in the regions outside the dipole source, total electric near fields decrease gradually in magnitude with an increasing field point from the dipole source. But in the regions inside the dipole source, total electric near fields decrease rapidly with a dipole position of $h{\leq}0.3{\lambda}$. For a dipole position of $h{\geq}0.7{\lambda}$, the peaks and nulls of the total near electric field occur periodically in the regions inside the dipole source, and the fluctuation period is almost $0.5{\lambda}$. The worst position for a receptor location is along the z-axis, and a range of a half-magnitude of the maximum near electric field in the principal H-plane is about two times broader than that of the principal E-plane. Experimental measurements are also presented to validate the theory.

수용모델을 이용한 청주시 미세입자($PM_{2.5}$)의 기여도 추정 (Source Identification of Fine Particle($PM_{2.5}$) in Chongju Using a Chemical Mass Balance Model)

  • 강병욱;이학성;김희강
    • 한국대기환경학회지
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    • 제16권5호
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    • pp.477-485
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    • 2000
  • The data set was collected on fifty-eight different days with a 24-h sampling period from October 27, 1995 through August 25, 1996. From the chemical mass balance (CMB) analysis of $PM_{2.5}$ in the Chongju area, the contributions from soil, gasoline, diesel, light and heavy oil combustion were 2.6%, 15.4%, 9.0%, 28.8% and 1.5%, respectively. Residual $NO_{3}^{-}$), residual $SO_{4}^{2-}$ and residual OC, possibly formed in the atmosphere. represented additional 8.0, 10.2, and 1.6% of the $PM_{2.5}$, respectively. Other unidentified sources constituted the remaining 22.9%. From the CMB analysis, the $PM_{2.5}$ source contribution for fall, winter, spring and summer were 92, 76.8, 77.5 and 59.2%, respectively.

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도시 대기오염물중 다환방향족 탄화수소의 배출원 규명을 위한 화학물질 수지모델의 적용 (Application of chemical Mass Balance Model for the Source Apportionment of Polynuclear Aromatic Hydrocarbons in Urban Atmosphere)

  • 구자공;서영화
    • 한국대기환경학회지
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    • 제8권4호
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    • pp.229-239
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    • 1992
  • A receptor model application was performed by using a chemical mass balance (CMB) model to identify and apportion the specific source of airborne organic pollutants, particularly polynuclear aromatic hydrocarbons (PAHs). Source profiles of PAHs produced from the combustion of fossil fuels for CMB modeling were prepared by measuring them in emission gases. The emission sources which were examineed for the development of PAH source profiles are a coal-fired furnace using Yontan, a bunker-C iol heating boiler, and gasoline-and diesel engine automobiles. The ambient concentrations of PAHs were determined at four sites in Daejon city in 1991 with a seasonal variation. Wintertime air samples contained more extractable organic matter than summertime samples. The results of CMB modeling were various depending on the sampling sites and seasons, but the emission from bunker-C oil heating boliers was the predominant factor to affect local air quality throughout the year.

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黃砂의 量的推定을 위한 基礎硏究 (Basic Research on the Quantitative Estimation of Yellow Sand)

  • 김동술
    • 한국대기환경학회지
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    • 제6권1호
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    • pp.11-21
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    • 1990
  • To quantitatively estimate the effect of yellow sand(loess) fromt he Northern China, various soil sources having similar chemical compositions to yellow sands should be separated and identified. After that, mass contribution for yellow sand can be calculated. The study showed that it was impossible to solve this problem by the traditional bulk analyses. However, particle-by-particle analysis by a CCSEM (computer controlled scanning electron microscope) gave enormous potentials to solve it. To perform this study, seven soil source data analyzed by CCSEM were obtained from Texas, U.S.A. Initially, each soil date was classified into two groups, coarse and fine particle groups since the particle number distribution showed a minimum occurring at 5.2$\mu$m of aerodynamic diameter. Particles in each group were then classified into one of the 283 homogeneous particle classes by the universal classification rule which had been built by an expert system in the early study. Further, mass fractions and their uncertainties for each class in each source were calculated by the Jackknife method, and then source profile matrix for the 7 soil sources was created. To use the profile matrix in the study of source contribution, it is necessary to test the degree of collinearity among sources. The profiles were tested by the singular value decomposition method. As a result, each soil source characterized by artificially created variables was totally independent each other and is ready to use in source contribution studies as a receptor model.

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