• Title/Summary/Keyword: saturation bound

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Interaction of Antihistaminics with Muscarinic Receptor (III) - Relationship between binding and functional in vitro data -

  • Lee, Shin-Woong;Park, Young-Joo
    • Archives of Pharmacal Research
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    • v.14 no.2
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    • pp.181-187
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    • 1991
  • The muscarinic antagonist 1-[benzilic 4, 4'-$[^3H]$ QUINUCLIDINYL BENZILATE $([^3H]$ QNB) bound to a single class of muscarinic receptors with high affinity in rabbit ileal membranes. The $K_D\;and\;B_{ max}$ values for $([^3H]$ QNB calculated from analysis of saturation isotherms were 52.5 pM AND 154 fmol/mg, respectively. Chlopheniramine (CHP), histamine $H_1$ blocker, increased $K_D$ vlue for $([^3H]$QNB without affecting the binding site concentrations and Hill coefficient. The $K_i$ value of CHP for inhibition of $([^3H]$QNB binding in ileal membranes was 1.44\mu{M}$ and the pseudo-Hill coefficient for CHP was close to unit. In the functional assay carbachol, muscarinic agonist, increased the contractile force of ileum with $ED_{50}$ value of $0.11\mu{M}$. CHP caused the rightward shift of the dose-response curve to carbachol. The $pA_2$ value of CHP determined from Schild analysis of carbacholinduced contraction was 5.77 and the slope was unity indicating competitive antagonism with carbachol. The dissociation constant $(K_i)$ of CHP obtained in competitive experiments with $([^3H]$ QNB was similar to the $K_A$ value (1.69 \mu{M)}$ of CHP as inhibitor of carbachol induced contraction in rabbit ileum. This result suggest that the binding of $H_i$ blocker. CHP, vs $([^3H]$QNB to muscarinic receptors in ileal membranes represents an interaction with a receptor of physiological relevance.

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Application of Semi-continuous Ambient Aerosol Collection System for Elemental Analysis (대기입자의 원소성분 배출특성연구를 위한 반-연속식 입자채취시스템 적용)

  • Park, Seung-Shik;Ko, Jae-Min;Lee, Dong-Soo
    • Journal of Korean Society for Atmospheric Environment
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    • v.28 no.1
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    • pp.39-51
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    • 2012
  • Aerosol slurry samples were collected in 60-min interval using Korean Semi-continuous Elements in Aerosol Sampler (KSEAS) between May 19 and June 6, 2010 at an urban site of Gwangju. The $PM_{2.5}$ samples were collected with a flow rate of 16.7 L/min and particles are grown by condensation of water vapor in a condenser maintained at ${\sim}5^{\circ}C$ after saturation by direct injection of steam. The resulting droplets are collected in a liquid slurry with a airdroplet separator. Concentrations of 16 elements (Al, Fe, Mn, Ca, K, Cu, Zn, Pb, Cd, Cr, Ti, V, Ni, Co, As, Se) in the collected slurry samples were determined off-line by ICP-MS. KSEAS sample analysis encompassed the sampling periods for which 24-hr average elemental species concentrations were calculated for comparison with those derived from 24-hr integrated filter samples. Relationship between elemental species measured by two methods indicated high correlation coefficients (r), mostly greater than r of 0.80. However, we note that concentrations of Al, K, Ca, Mn, and Fe, which are often associated with crustal elemental particles, in the KSEAS samples, were substantially lower (1.4~11 times) than those found in the typical filter-based samples. This discrepancy is probably due to difficulties in transferring insoluble dust particles to the collection vials in the KSEAS. Temporal profiles of elemental concentrations indicate that some transient events in their concentrations are observed over the sampling periods. For the elemental species studied, atmospheric concentrations during the transient events increased by factors of 4 in Mn~80 in Zn, compared to their background levels. Principle component analyses were applied to the hourly KSEAS data sets to identify sources affecting the concentrations of the metal constituents observed. In this study, we conclude that hourly measurements for particle-bound elemental constituents were extremely useful for revealing the short-term variability in their concentrations and developing insights into their sources.

Estimation of Moisture Diffusivity during Absorption by Boltzmann Transformation Method (Boltzmann법에 의한 목재 흡수시 확산계수 추정)

  • Kang, Wook;Chung, Woo Yang
    • Journal of the Korean Wood Science and Technology
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    • v.37 no.1
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    • pp.1-11
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    • 2009
  • Although the exterior wood such as column may frequently contact with liquid water, little work has been found to measure liquid water absorption in wood. To investigate the moisture diffusivity of wood in the longitudinal direction including bound water and free water movement, liquid water absorption test was conducted at the room temperature. The order of magnitude for absorption coefficient and diffusivity was Japanese elm, horn beam, hemlock, spruce, radiata pine, and painted maple. The Boltzmann transformation method was used to determine the diffusivity from measured moisture content distributions in the absorption test. The shape of the curve representing the dependence of diffusivity with moisture content was similar in test samples. The diffusivity decreased with increasing moisture content until around the fiber saturation point and then increased at the nonhygroscopic region, which ranged from $10^{-10}$ to $10^{-7}m^2/s$.

Relative potency of antihistaminics for $H_1$-and muscarinic receptors (항 히스타민제의 $H_1$ 수용체와 무스카린 수용체에 대한 상대적 역가)

  • 이신웅;박영주;이정수
    • YAKHAK HOEJI
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    • v.37 no.4
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    • pp.397-407
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    • 1993
  • The muscarinic antagonist l-[benzilic-4,4'-$^3H$]quinuclidinyl benzilate([$^3H$]QNB) bound to a single class of muscarinic receptor with high affinity in guinea pig ileal membranes. The $K_{D}$ and B$_{max}$ values for [$^3H$]QNB calculated from analysis of saturation isotherms were 54 pM and 156fmol/mg, respectively. H$_{1}$-blockers inhibited [$^3H$]QNB binding to ileal membranes with $K_{i}$ values ranged from 0.008 $\mu{M}$ to 1.6 $\mu{M}$. The pseudo-Hill coefficients of H$_{1}$-blockers for inhibition of [$^3H$]QNB binding to the ileal membranes were close to unit. The $K_{i}$ values for H$_{1}$-blockers were similar to the $K_{M}$ values calculated by Schild plot of functional data obtained from inhibition of the carbachol-induced contraction in guinea-pig ileum, suggesting that binding of H$_{1}$-blockers vs [$^3H$]QNB in ileal membranes represents an interaction with a receptor of physiological relevance. The $K_{H}$ values of H$_{1}$-blockers for H$_{1}$-receptor estimated from inhibition of the histamine-induced contraction were the range of 0.15 nM to 56.5 nM. The $K_{M}$/K$_{H}$ ratio of H$_{1}$-blockers varied over a wide range of 3 to 2300. Thus, the antihistaminic potencies of H$_{1}$-blockers do not correlate with their antimuscarinic potencies, which suggest that antihistamines have different antimuscarinic potencies in therapeutic blood levels causing similar antiallergic effect. Among 13 traditional antihistaminics examined in this study, drug having the highest and the lowest $K_{M}$/K$_{H}$ ratio is triprolidine and diphenidol, respectively. The present results demonstrate that the antimuscarinic property of antihistamines is not necessary for their antiallergic effect, and data on the affinity of antihistamines for muscarinic and H$_{1}$-receptors can be an important parameter in the selection and evaluation of these drugs.

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Studies on ammonium adsorption by and desorption from various soils (I) -Langmuir adsorption isotherm of ammonium (토양별(土壤別) 암모늄의 흡착(吸着) 및 탈착(脫着)에 관(關)한 연구(硏究) (I) -암모늄의 Langmuir 등온흡착(等溫吸着))

  • Shim, Sang-Chil;Kim, Kwang-Rai;Kim, Moo-Sung;Park, Hoon
    • Korean Journal of Soil Science and Fertilizer
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    • v.10 no.1
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    • pp.1-6
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    • 1977
  • Fifteen soils including volcanic ash, acid sulfate and degraded saline soils were investigated for Languir adsorption isotherm of ammonium using $NH_4H_2PO_4$. The results are as follows. Languir adsorption maxima of ammonium (LAMA) ranged from 2.4me/100g soil to 12.3 and the average was 5.3. Initial concentration of 30 to 60 or 40 to 80 ppm(as N) appears to be suitable for LAMA measurement. There were two LAMA in some soils. Difference between adsorption constants (bonding energy) was mostly greater than that between LAMA. LAMA ranged from 9.4% to 72% of cation exchange capacity and average was 47%. It did not show any clear tendency with CEC, pH, organic matter content, base saturation percent, P, K, Ca, Mg, Na and Si. Except volcanic ash soils which were grouped into two groups according to ammonium adsorption LAMA was significantly (r=0.951 at 1%) correlated with adsorption at 200ppm. This single concentration seems suitable for LAMA measurement. Probable mechanism of ammonium adsorption was discussed, in which the associated anions were combined with iron and aluminum and then ammonium was bound to phosphorus. Applicability of Langmuir adsorption isotherm model to the soils under field condition was also discussed.

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A Study on Analysis Technique for Chloride Penetration in Cracked Concrete under Combined Deterioration (복합열화에 노출된 균열부 콘크리트 내의 염화물 침투 해석 기법에 대한 연구)

  • Kwon, Seung-Jun;Song, Ha-Won;Byun, Keun-Joo
    • Journal of the Korea Concrete Institute
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    • v.19 no.3
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    • pp.359-366
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    • 2007
  • Recently, analysis researches on durability are focused on chloride attack and carbonation due to increased social and engineering significance. Generally, chloride penetration and carbonation occur simultaneously except for in submerged condition and chloride behavior in carbonated concrete is evaluated to be different from that in normal concrete. Furthermore, if unavoidable crack occurs in concrete, it influences not only single attack but also coupled deterioration more severely. This is a study on analysis technique with system dynamics for chloride penetration in concrete structures exposed to coupled chloride attack and carbonation through chloride diffusion, permeation, and carbonation reaction. For the purpose, a modeling for chloride behavior considering diffusion and permeation is performed through previous models for early-aged concrete such as MCHHM (multi component hydration heat model) and MPSFM (micro pore structure formation). Then model for combined deterioration is developed considering changed characteristics such as pore distribution, saturation and dissociation of bound chloride content under carbonation. The developed model is verified through comparison with previous experimental data. Additionally, simulation for combined deterioration in cracked concrete is carried out through utilizing previously developed models for chloride penetration and carbonation in cracked concrete. From the simulated results, CCTZ (chloride-carbonation transition zone) for evaluating combined deterioration is proposed. It is numerically verified that concrete with slag has better resistance to combined deterioration than concrete with OPC in sound and cracked concrete.

Pharmacological Characterization of (10bS)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline Oxalate (YSL-3S) as a New ${\alpha}_2$-Adrenoceptor Antagonist

  • Chung, Sung-Hyun;Yook, Ju-Won;Min, Byung-Jun;Lee, Jae-Yeol;Lee, Yong-Sup;Jin, Chang-Bae
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.353-359
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    • 2000
  • ${\alpha}_2$-Adrenoceptor antagonists, which can enhance synaptic norepinephrine levels by blocking feedback inhibition processes, are potentially useful in the treatment of disease states such. as depression, memory impairment, impotence and sexual dysfunction. (10bS)-1,2,3,5,6,10b-Hexahydropyrrolo[2,1-a]isoquinoline oxalate (YSL-3S) was evaluated in several in vitro biological tests to establish its pharmacological profile of activities as an ${\alpha}_2$-adrenoceptor antagonist. Saturation binding assay revealed that$^{3}[H]$rauwolscine bound to the $\alpha$$_2$-adrenoceptors with a Kd value of 6.3$\pm$0.5 nM and a Bmax value of 25l$\pm$39 fmol/mg protein in rat cortical synaptic membranes. Competitive binding assay showed that YSL-3S inhibited the binding of$^3[H]$rauwolscine (1 nM) in a concentration-dependent manner with a Ki value of 98.2$\pm$12.1 nM while it did not inhibit the binding of [$^3$H]cytisine (1.25 nM) to neuronal nicotinic cholinergic receptors. The Ki values of yohimbine, clonidine and norepinephrine for $^3[H]$rauwolscine binding were 15.8$\pm$1.0, 40.1$\pm$5.9 and 40.0$\pm$11.5 nM, respectively. In addition, the binding affinity of YSL-3S for ${\alpha}_2$-adrenoceptors was higher than that of its antipode and the racemic mixture. The functional activity of YSL-3S at the presynaptic ${\alpha}_2$-adrenoceptors was assessed using the prostatic portion of the rat vas deferens. Clonidine inhibited field-stimulated contractions of the vas deference in a dose-dependent manner. The presence of YSL-3S or yohimbine caused a parallel, rightward the dose-response curve of clonidine in a dose-dependent manner, indicating an antagonistic action at the presynaptic ${\alpha}_2$-adrenoceptors. The $pA_2$values of yohimbine and YSL-3S were 7.66$\pm$0.13 and 6.64$\pm$0.18, respectively. The results indicate that YSL-3S acts as a competitive antagonist at presynaptic ${\alpha}_2$ -adrenoceptors with a potency approximately ten times lower than yohimbine, but is devoid of binding affinity for neuronal nicotinic cholinergic receptors.

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Highly sensitive and selective detection of cyanide in aqueous solutions using a surface acoustic wave chemical sensor (표면음향파 화학센서를 이용한 수용액 중 시안화이온의 선택적인 고감도 검출)

  • Lee, Soo Suk
    • The Journal of the Acoustical Society of Korea
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    • v.35 no.6
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    • pp.473-479
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    • 2016
  • We report a highly selective and sensitive 200 MHz Surface Acoustic Wave (SAW) sensor that can detect cyanide ion in aqueous solution using surface immobilized thioester molecules in combination with gold nanoparticles (AuNPs). To construct the sensor device, a monolayer of thioester compound was immobilized on the SAW sensor surface. At the sensor surface, hydrolysis of thioester group by nucleophilic addition of cyanide occurred and the resulting free thiol unit bound to AuNP to form thiol-AuNP conjugate. For the signal enhancement, gold staining signal amplification process was introduced subsequently with gold (III) chloride trihydrate and reducing agent, hydroxylamine hydrochloride. The SAW sensor showed a detection ability of $17.7{\mu}M$ for cyanide in aqueous solution and demonstrated a saturation behavior between the frequency shift and the concentration of cyanide ion. On the other hand, our SAW sensor had no activities for other anions such as fluoride ion, acetate ion and sulfate ion, moreover, no significant interference observed by other anions. Finally, all the experiments were carried out in-house developed sensor and fluidics modules to obtain highly reproducible results.

A Study on Change in Cement Mortar Characteristics under Carbonation Based on Tests for Hydration and Porosity (수화물 및 공극률 관측 실험을 통한 시멘트모르타르의 탄산화 특성 변화에 대한 연구)

  • Kwon, Seung-Jun;Song, Ha-Won;Park, Sang-Soon
    • Journal of the Korea Concrete Institute
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    • v.19 no.5
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    • pp.613-621
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    • 2007
  • Due to the increasing significance of durability, much researches on carbonation, one of the major deterioration phenomena are carried out. However, conventional researches based on fully hardened concrete are focused on prediction of carbonation depth and they sometimes cause errors. In contrast with steel members, behaviors in early-aged concrete such as porosity and hydrates (calcium hydroxide) are very important and may be changed under carbonation process. Because transportation of deteriorating factors is mainly dependent on porosity and saturation, it is desirable to consider these changes in behaviors in early-aged concrete under carbonation for reasonable analysis of durability in long term exposure or combined deterioration. As for porosity, unless the decrease in $CO_2$ diffusion due to change in porosity is considered, the results from the prediction is overestimated. The carbonation depth and characteristics of pore water are mainly determined by amount of calcium hydroxide, and bound chloride content in carbonated concrete is also affected. So Analysis based on test for hydration and porosity is recently carried out for evaluation of carbonation characteristics. In this study, changes in porosity and hydrate $(Ca(OH)_2)$ under carbonation process are performed through the tests. Mercury Intrusion Porosimetry (MIP) for changed porosity, Thermogravimetric Analysis (TGA) for amount of $(Ca(OH)_2)$ are carried out respectively and analysis technique for porosity and hydrates under carbonation is developed utilizing modeling for behavior in early-aged concrete such as multi component hydration heat model (MCHHM) and micro pore structure formation model (MPSFM). The results from developed technique is in reasonable agreement with experimental data, respectively and they are evaluated to be used for analysis of chloride behavior in carbonated concrete.