• Title/Summary/Keyword: affinity coefficient

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

  • Lee, Shin-Woong;Kim, Jeung-Gu
    • 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.

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Hydraulic Characteristics of water affinity sea-wall block (환경친화형 친수호안(親水護岸)블록 수리특성)

  • Han, Jea-Myung;Oh, Young-Min
    • Journal of Korean Society of Coastal and Ocean Engineers
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    • v.19 no.2
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    • pp.179-182
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    • 2007
  • In this study hydraulic model experiment was conducted to identify the performance of newly developed water affinity sea-wall block to keep the coastal line from eroding and supply water affinity space by reflection coefficient and safety. In the result, the block is applicable to the field.

Influence of Temperature and Affinity of Disperse Dye on Dyeing of PET(Polyethylene Terephthalate) Microfiber (PET 초극세사 염색에서 분산염료의 친화력과 온도 의존성)

  • Lee, Hun
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.9
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    • pp.532-540
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    • 2019
  • PET microfibers with various diameters (0.5, 0.2, 0.06, and 0.01 dpf) were dyed with a dispersed dye (C.I. Disperse Blue 56) at various temperatures. The dyeing process was conducted under infinite dyebath conditions at constant temperatures. The effects of the dyeing temperature and diameter on the partition coefficient, affinity, and diffusion coefficient of disperse dyes were studied. The curve of isotherms was fitted well to Nernst-type model in a large range of initial dye concentrations. At the same temperature, the partition coefficient and affinity decreased with increasing sample diameter due to the increase in surface area. At all deniers, the partition coefficient and affinity decreased with increasing temperature because the dyeing process is an exothermic reaction. In addition, the decrease in radius of the sample gives rise to a decrease in the heat of dyeing. The fine diameter of the sample resulted in an increased surface area but decreased space between the microfibers. Consequently, decreasing the diameter of the microfibers leads to a decrease in the diffusion coefficient. At the same diameter, the diffusion coefficient increased with increasing temperature because of rapid dye movement and the large free volume of the sample inside. In addition, thermal dependence of the diffusion coefficient increased when the diameter of the sample increased.

A Molecular Dynamics Study of Thermophysical Properties and Stability of Nanoscale Liquid Thread (분자동역학 해석을 이용한 액체 극미세사의 열역학적 물성과 안정성 연구)

  • Kim, Byeong-Geun;Choi, Young-Ki;Kwon, Oh-Myoung;Park, Seung-Ho;Lee, Joon-Sik
    • Proceedings of the KSME Conference
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    • 2003.04a
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    • pp.1366-1371
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    • 2003
  • Molecular dynamics (MD) simulations are conducted to investigate the thermophysical characteristics and the stability of liquid threads for various conditions. A cylindrical thread in the simulation domain is made of Lennard-Jones molecules. The surface tension of liquid threads can be determined from local densities, local normal and transverse components of the pressure force. In order to understand the effects of thread radii on surface tensions, the Tolman equation is modified on the basis of the cylindrical coordinates for prediction of surface tensions. Surface tensions calculated from the MD simulation agree with the prediction from the modified Tolman equation. In addition, surface tensions decrease linearly with increasing system temperature. For a binary system, the surface tension decreased linearly compared to that for a pure system with increasing binary ratio of solute molecules which have relatively large value of the affinity coefficient. For a fixed binary ratio, the surface tension increased slightly with the affinity coefficient and the maximum value appear around where the affinity coefficient is 1.5 and decreased rapidly for upper value of 1.5. In addition, the critical wavelengths of perturbations are proven to be directly proportional to the equimolar dividing radii of the liquid threads.

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Enhanced Partitioning of Proteins in Metal-Affinity Aqueous Two-Phase Systems (금속 친화성 액 이상분계 시스템에서 단백질의 분배 향상)

  • Chung, Bong-Hyun;Park, Young-Hoon
    • Microbiology and Biotechnology Letters
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    • v.21 no.4
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    • pp.336-341
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    • 1993
  • In metal-affinify aqueous two-phase systems, protein partitioning is affected by a variety of parameters such as pH, the number of surface-accessible histidines, and the amount and partition coefficient of metallated polythylene glyco(PEG) ligand. To enhance partitioning of proteins with surface-accessible histidines, we have synthesized and used a (Cu(II)-ininodiacetic acid)$_2$-PEG20,000($Cu(II)_2IDA_2$-PEG20,000) as well as Cu(II)IDA-PEG5,000 as an affinity ligand. The partition coefficient of $Cu(II)_2-IDA_2$-PEG20,000 in a PEG5,000/dextran two-phase system was 30.1, which corresponded to a 3.8-fold increase over that of Cu(II)IDA-PEG5,000. The partitioning experiments were performed on four proteins, horse cytochrome c, S. cerevisiae cytochrome c, horse myoglobin, and sheep myoglobin. Partitioning of proteins which convey surface-accessible histidines was enhanced dramatically by the addition of $Cu(II)_2IDA_2$-PEG20,000 ligand. These results demonstrate that enhanced partitioning of metal-binding proteins in an aqueous two -phase system can by achieved by using an appropriate metallated PEG ligand.

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Selectivity of Oxomemazine for the $M_1$ Muscarinic Receptors

  • Lee, Shin-Woong;Woo, Chang-Woo;Kim, Jeung-Gu
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.443-451
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    • 1994
  • The binding characteristics of pirenzepine and oxomemazine to muscarinic receptor were studied to evaluate the selectivity of oxomemazine for the muscarinic receptor subtypes in rat cerebral microsomes. Equililbrium dissociation constant $(K_D){\;}of{\;}(-)[^3H]$quinuclidinyl benzilate$([^3H)QNB)$ determined from saturation isotherms was 64-pM. Analysis of the pirenzepine inghibition curve of [$^3H$]QNB binding to cerebral microsome indicatd the presence of two receptor subtypes with high $(K_1 = 16 nM, M_1 receptor)$two receptor subypes with about 20-fold difference in the affinity for high $(k_1 = 84nM, {\;} O_H receptor){\;} and {\;}low{\;} (K_1{\;} ={\;} 1.65\muM, {\;} O_L receptor$) affinity sites. The percentage populations of $M_1{\;} and M_3$, /TEX> receptors to the total receptors were 61 : 39, and those of $O_H{\;} and{\;} O_L$ receptors 39 : 61, resepectively. Both pirenzepine and oxomemazine increaed the $K_D$ value for $[^3H]QNB$ without affecting the binding site concentrations and Hii coefficient for the $[^3H]QNB$ without affecting the binding site concentractions and Hill coefficient for the [$^{3}$H]QNB binding. Oxomemazine had a 10-fold higher affinity at $M_1$ receptors than at $M_3$ receptors, and pirenzepine a 8-fold higher affinity at $O_H$ receptors were of $O_H$ receptors and 71% of $M_3$ receptors. However, $M_3$for oxomemazine and $O_H$for pirenzepine were composed of a uniform population. These results suggest that oxomemazine could be classified as a selective drug for $M_1$ receptors and also demonstrate that rat cerebral microsomes contain three different subtypes of $M_1{\;} M_3$ and the other site which is different from $M_1, {\;} M_2$, /TEX> receptors.

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Purification of the Candida utilis Extracellular Invertase using Affinity Chromatography

  • Ginalska, G.;Belcarz, A.;Lobarzewski, J.;Leonowicz, A.;Cho, Nam-Seok
    • Journal of the Korean Wood Science and Technology
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    • v.30 no.3
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    • pp.12-17
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    • 2002
  • The extracellular invertase (EC 3.2.1.26) (Candida utilis) preparation was obtained from the liquid medium after desalting and freeze drying. This prepared enzyme was used for the comparative purification on 4 activated matrices by liquid column affinity chromatography method. In this method there were used controlled porous glass (CPG) silanized covalently activated by keratin, silanized silica gel and silica gel covalently covered by keratin. It was found that the invertase purification process was better using both CPG matrices (silanized CPG and keratin activated CPG) than these with two silica gel supports. Also the elution coefficient of the invertase from the two CPG columns was about 93 to 94%. Two silica gel supports found to be superior in terms of purification efficiency. The invertase purification process was confirmed by PAGE electrophoresis.

The Relationship between Affinity of Membrane and Optimum Operation Conditions in the Pervaporation of Aqueous Ethanol (에탄올 수용액의 투과증발에 있어서 막의 친화성과 최적 조업조건의 관계)

  • 전종기;명완재;임선기
    • Membrane Journal
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    • v.1 no.1
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    • pp.34-43
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    • 1991
  • The relationships between affinity of membranes and optimum operation conditions were investigated in the pervaporation of water(1)/ethanol(2) mixture through cellulose acetate(CA) membranes having more affinity to water and silicone rubber(SR) membranes having more affinity to ethanol. CA and SR membranes were prepared and amount of sorption, sorption selectivity, pervaporation separation factor and pervaporation rate in both of membranes were determined and compared. The effects of downstream pressure were analyzed using Thompson diagram and the sorption and pervaporation characteristics with composition of feed and operation temperature were examined in terms of affinity, activity coefficient, plasticizing effect and activation energy of individual species. In the separation of water through CA membranes, high performance of both pervaporation separation factor (water to ethanol, $[\alpha^2_1]_{PV}$) and pervaporation rate was obtained in the conditions of low downstream pressure, middle range of feed concentration and high temperature. In the separation of ethanol through SR membranes, pervaporation separation factor(ethanol to water, $[\alpha^2_1]_{PV}$) increased with downstream pressure and decreased with concentration of ethanol in feed and operation temperature, while pervaporation rate showed opposite trends to those of ($[\alpha^2_1]_{PV}$).

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The Dyeing Properties of Poly(trimethylene terephthalate) by Disperse Dyes with Different Energy Level (Energy Level이 다른 분산염료를 이용한 Poly(trimethylene terephthalate)섬유의 염색성)

  • 백지연;김정렬;이난형;윤태희;김삼수
    • Textile Coloration and Finishing
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    • v.15 no.5
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    • pp.316-320
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    • 2003
  • In order to investigate the dyeing property of poly trimethylene terephthalate(PTT) fabric, the dyeing of PTT fabric was carried at under condition of different dyeing temperature by using several disperse dyes with different energy level. Particularly, this study discussed the PTT dyeing thermodynamically. Used disperse dyes were selected based on the their chemical structure and energy level. The obtained results were as followings; The dye adsorption of S type disperse dye such as C. I. Disperse Blue 79 increased with increasing dyeing temperature. In a exhaustion rate of PTT fabric with disperse dyes, C. I. Disperse Blue 56 showed higher values than that of C. I. Disperse Orange 29 and Blue 79. For the interpretation of thermodynamic dyeing behavior, the partition coefficient ( K ) and some several thermodynamic parameters such as standard affinity$(-\mu^\circ)$ and heat of dyeing$(\Delta{H}^\circ)$ calculated from the adsorption isotherm. From above results, as the energy level of disperse dye is small, the partition coefficient and standard affinity increased. But the heat of dyeing of PTT fabric with disperse dye showed high negative value in order of E type(C. I. Disperse Blue 56), SE type(C. I. Disperse Orange 29) and S type(C. I. Disperse 79).

Partial Characterization of Physicochemical and Kinetic Properties of $Ca^{++}-ATPase$ System in Luteal Membranes (황체막에서의 $Ca^{++}-ATPase$의 특성)

  • Choi, Gyu-Bog;Koo, Bon-Sook;Kim, In-Kyo
    • The Korean Journal of Physiology
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    • v.20 no.2
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    • pp.257-270
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    • 1986
  • It has been reported that the luteal function may be regulated by the intracellular calcium in luteal cells (Higuchi et al, 1976; Dorflinger et at, 1984; Gore and Behrman, 1984) which is adjusted partially by $Ca^{++}-ATPase$ activities in luteal cell membranes (Verma and Pennistion, 1981). However, the physicochemical and kinetic properties of $Ca^{++}-ATPase$ in luteal membranes were not fully characterized. This study was, therefore, undertaken to partially characterize the physicochemical and kinetic properties of $Ca^{++}-ATPase$ system in luteal membranes and microsomal fractions, known as an one of the major $Ca^{++}$ storge sites (Moore and Pastan, 1978), from the highly luteinized ovary Highly luteinized ovaries were obtained from PMSG-hCG injected immautre female rats. Light membrane and heavy membrane fractions and microsomal fractions were prepared by the differential and discontinuous sucrose density gradient centrifugation method desribed by Bramley and Ryan (1980). Light membrane and heavy membrane fractions and microsomal fractions from highly luteinized ovaries are composed of the two different kinds of $Ca^{++}-ATPase$ system. One is the high affinity $Ca^{++}-ATPase$ which is activated in low $Ca^{++}$ concentration (Km, 10-30 nM), the other is low affinity $Ca^{++}-ATPase$ activated in higher $Ca^{++}$ concentration $(K_{1/2},\;40\;{\mu}M)$. At certain $Ca^{++}$ concentrations, activities of high and low affinity $Ca^{++}-ATPase$ are the highest in light membrane fractions and are the lowest in microsomal fractions. It appeares that high affinity $Ca^{++}-ATPase$ system have 2 binding sites for ATP (Hill's coefficient; around 2 in all membrane fractions measured) and the positive cooperativity of ATP bindings obviously existed in each membrane fractions. The optimum pH for high affinity $Ca^{++}-ATPase$ activation is around S in all membrane fractions measured. The lipid phase transition temperature measured by Arrhenius plots of high affinity $Ca^{++}-ATPase$ activity is around $25^{\circ}C$. The activation energies of high affinity $Ca^{++}-ATPase$ below the transition temperature are similar in each membrane fractions, but at the above transition temperature, it is the hightest in heavy membrane fractions and the lowest in microsomal fractions. According to the above results, it is suggested that intracellular $Ca^{++}$ level, which may regulate the luteal function, may be adjusted primarily by the high affinity $Ca^{++}-ATPase$ system activated in intracellular $Ca^{++}$ concentration range $(below\;0.1\;{\mu}M)$.

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