• Title/Summary/Keyword: P-M interaction

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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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Effect of Exogenous Sulfur on Hydrogen Peroxide, Ammonia and Proline Synthesis in White Clover (Trifolium repens L.)

  • Baek, Seon-Hye;Muchamad, Muchlas;Lee, Bok-Rye;Kim, Tae-Hwan
    • Journal of The Korean Society of Grassland and Forage Science
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    • v.42 no.3
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    • pp.195-200
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    • 2022
  • Sulfur is an essential element in plants, including amino acids, vitamin synthesis, and acting as an antioxidant. However, the interaction between endogenous sulfur and proline synthesis has not been yet fully documented. White clover (Trifolium repens L.) is known as a species highly sensitive to sulfate supply. Therefore, this study aimed to elucidate the role of sulfur in regulating proline metabolism in relation to ammonia detoxification and hydrogen peroxide (H2O2) accumulation in white clover. The detached leaves of white clover were immersed in solution containing different concentration of sulfate (0, 10, 100, and 1000 mM MgSO4). As MgSO4 concentrations were increased, the concentration of H2O2 increased up to 2.5-fold compared to control, accompanied with H2O2 detection in leaves. Amino acid concentrations significantly increased only at higher levels (100 and 1000 mM MgSO4). No significant difference was observed in protein concentration. Proline and ∆1-pyrroline-5-carboxylate (P5C) concentrations slightly decreased at 10 and 100 mM MgSO4 treatments, whereas it rapidly increased over 1.9-fold at 1000 mM MgSO4 treatment. Ammonia concentrations gradually increased up to 8.6-fold. These results indicate that exogenous sulfur levels are closely related to H2O2 and ammonia synthesis but affect proline biosynthesis only at a higher level.

Effect of Genetic and Non-Genetic Factors Other Than Disease on Kid Survivability in Goat (산양의 생존율에 대한 유전적 및 비유전적 요인)

  • Miah, G.;Husain, S.S.;Hoque, M.A.;Baik, D.H.
    • Journal of Animal Science and Technology
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    • v.44 no.3
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    • pp.271-278
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    • 2002
  • This experiment was conducted to investigate the genetic and non-genetic factors affecting kid survivability in goats from birth to 90 days of age. The purebreds had lower survivability than the crossbreds, with significant (p$<$0.05) difference amongst themselves for the age of 31 to 90 days. The locational effect on survivability was insignificant for all the periods except 16 to 60 days (p$<$0.05) of age. The sex and birth type also had significant (p$<$0.05) effect on survivability for all the periods except 0 to 7 days of age. The survivability was found to be significantly (p$<$0.05) higher for kids born in summer season followed by those born in winter and rainy season. Milk produced by the does were significantly (p$<$0.05) affected on the survivability of kids during the period from 16 to 60 days of age. The survivability of kids were highest and lowest having milk yield of doe found to be 400-600 g/day and 80-200 g/day, respectively. Birth weight had significant (p$<$0.05) effect on survivability for all the stages of growth up to 90 days of age. Survivability was positively correlated with does’ milk yield as well as kids birth weight. Interactions of sex with location or birth type were significant (p$<$0.01 and p$<$0.05, respectively) though interaction between sex and genetic group was insignificant.

Synthesis, Sytructure, and Magnetic Properties of One-Dimensional Thiophoshates, $Al_2NiP_2S_6$ (A=Rb, Cs) (1차원 구조를 갖는 Thiophoshates, $Al_2NiP_2S_6$ (A=Rb, Cs)의 합성, 구조 및 자기적 성질)

  • Dong, Yong Kwan;Lee, Kun Soo;Yun, Ho Seop;Hur, Nam Hwi
    • Journal of the Korean Chemical Society
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    • v.45 no.3
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    • pp.242-246
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    • 2001
  • The quaternary thiophosphates, $A_2NiP_2S_6$ (A=Rb, Cs), have been synthesized with halide fluxes and structurally characterized by single-crystal X-ray diffraction technique. These compounds crystallize in the space group $C_{2h}^5-P2_1/n$ of the monoclinic system with two formula units in a cell of dimensions a=5.960(2), b=12.323(4), $c=7.491(3)\AA$, $\beta=97.05(3)^{\circ}$, and $V=546.0(3)\AA^3$ for Rb2NiP2S6 and a=5.957(4), b=12.696(7), $c=7.679(4)\AA$, $b=93.60(5)^{\circ}$, and $V=579.7(5)\AA^3$ for $Cs_2NiP_2S_6.$ These compounds are isostructural. The structure of $Cs_2NiP_2S_6$ is made up of one-dimensional $_\infty^1[NiP_2S_6^{2-}]$ chains along the a axis and these chains are isolated by $Cs^+$ ions. The Ni atom is octahedrally coordinated by six S atoms. These Ni$S_6$ octahedral units are linked by sharing three m-S atoms of the $[P_2S_6^{4-}]$ anions to form the infinite one-dimensional $_\infty^1[NiP_2S_6^{2-}]$ chain. For $Cs_2NiP_2S_6$, the magnetic susceptibility reveals an antiferromagnetic exchange interaction below 8K,which corresponds to the Neel temperature ($T_N$). Above $T_N$, this compound obeys Curie-Weiss law. The magnetic moment, C, and ${\theta}forCs_2NiP_2S_6$ are 2.77 B.M., 0.9593 K, and -19.02 K, respectively. The effective magnetic moment obtained from the magnetic data is agreed with the spin-only value of $Ni^{2+}d^8$(2.83 B.M.) system.

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Physical Activity- and Alcohol-dependent Association Between Air Pollution Exposure and Elevated Liver Enzyme Levels: An Elderly Panel Study

  • Kim, Kyoung-Nam;Lee, Hyemi;Kim, Jin Hee;Jung, Kweon;Lim, Youn-Hee;Hong, Yun-Chul
    • Journal of Preventive Medicine and Public Health
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    • v.48 no.3
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    • pp.151-169
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    • 2015
  • Objectives: The deleterious effects of air pollution on various health outcomes have been demonstrated. However, few studies have examined the effects of air pollution on liver enzyme levels. Methods: Blood samples were drawn up to three times between 2008 and 2010 from 545 elderly individuals who regularly visited a community welfare center in Seoul, Korea. Data regarding ambient air pollutants (particulate matter ${\leq}2.5{\mu}m$ [$PM_{2.5}$], nitrogen dioxide [$NO_2$], ozone [$O_3$], carbon monoxide, and sulfur dioxide) from monitoring stations were used to estimate air pollution exposure. The effects of the air pollutants on the concentrations of three liver enzymes (aspartate aminotransferase [AST], alanine aminotransferase [ALT], and ${\gamma}$-glutamyltranspeptidase [${\gamma}$-GTP)]) were evaluated using generalized additive and linear mixed models. Results: Interquartile range increases in the concentrations of the pollutants showed significant associations of $PM_{2.5}$ with AST (3.0% increase, p=0.0052), ALT (3.2% increase, p=0.0313), and ${\gamma}$-GTP (5.0% increase, p=0.0051) levels; $NO_2$ with AST (3.5% increase, p=0.0060) and ALT (3.8% increase, p=0.0179) levels; and $O_3$ with ${\gamma}$-GTP (5.3% increase, p=0.0324) levels. Significant modification of these effects by exercise and alcohol consumption was found (p for interaction <0.05). The effects of air pollutants were greater in non-exercisers and heavy drinkers. Conclusions: Short-term exposure to air pollutants such as $PM_{2.5}$, $NO_2$, and $O_3$ is associated with increased liver enzyme levels in the elderly. These adverse effects can be reduced by exercising regularly and abstinence from alcohol.

A Study on the Effect of Drape by the Construction Method of th eCircular Skirt (Circular Skirt의 구성방법에 따른 Drape효과에 관한 연구)

  • 홍정민
    • Journal of the Korean Society of Costume
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    • v.33
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    • pp.217-228
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    • 1997
  • The purpose of this study was to investigate influence of the construction method of the circular skirt on drapability and shape of static silhouette and length variation. In made 24 types of skirts giving the variations (six kinds of peach skin-like finished fabrics two types of cutting method two types of machine stitch method of hem), The results were as follows: 1. Analysis of drapability In the cutting method thre was similarity between warp direction and true bias direc-tion. In the machine stitch method of hem there was similarity between blind stitch and blind stitch machine. According to the fabrics analysis of drapability was excellent in the order N/P 80/20(fabric 1)>P 100(fabric 5)>P 100(fabric 6)>P 100 (fabric 2)>P 100 (fabric 4)>N/C 50/50(fabric 3). 2. Analysis of the characteristics values of static silhouette shape In the cutting method shape of static sil-houette became wide in the warp direction. In the machine stitch method of hem shape of static silhouette became wide in the blind stitch. According to the fabrics shape of static silhouette became most wide in the N/C 50/50(fabric 3) and shape of static sil-houette become most narrow in the P 100(fabric 2,5) 3. Analysis of the length variation In the cutting method the true bias direc-tion was longer than the warp direction. In the machine stitch method of hem there was simi-machine stitch method of hem there was simi-larity between blind stitch and blind stitch ma-chine. In fabrics the P 100(fabric 6) showed the longest the N/C 50/50(fabric 3) showed most slight. Interaction between the cutting and messure-ment part of skirt lengh. In the warp diretion parts that showed longest length variation were C. G, K, O in the true bias diretion parts that showed most slight length variation were A, E, M, I.

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Effects of Dietary Various Energy and Protein Levels on Productivity, Blood Composition and Meat Quality in Cross-Bred Chicks (유색 육용계의 사료내 다양한 에너지 및 단백질 수준이 생산 능력, 혈액 성상, 계육 품질에 미치는 영향)

  • Jeong, Y.D.;Youn, M.J.;Ryu, M.S.;Ryu, K.S.
    • Korean Journal of Poultry Science
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    • v.36 no.1
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    • pp.57-67
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    • 2009
  • These studies were conducted to investigate the various dietary CP and ME feeding effect on productivity, blood composition and meat quality in cross bred chicks. Seven hundred twenty one day old cross bred chicks (Hanhyup Samho) were alloted to the floor pen for early starting (0~2 weeks), starting (3~5 weeks), growing (6~8 weeks), finishing period (9~10 weeks). Dietary ME and CP were 3,000, 3,100 kcal/kg, and 22% for early starting period, 19, 20, 21% for starting period, 18, 19, 20% for growing period, 17, 18, 19% for finishing period. Weight gain and feed consumption were weekly measured and feed conversion ratios were calculated. Blood and breast meat were collected at the end of experiment. Birds fed ME 3,100 kcal/kg diets improved significantly compared with others for the first two weeks (P<0.05). Feed conversion was statistically improved in CP (22)21% treatment relative to that of CP (22)20% from three to five weeks of age. No difference were found from 6 to 8 weeks of age. Weight gain and feed conversion also improved in ME 3,100 kcal/kg treatments, but feed intake decreased significantly in CP ($22{\times}21{\times}20$)19% treatment for the rest of experimental period (P<0.05). There was interaction between ME and CP for the first five weeks (P<0.05). Blood total protein showed higher in ME 3,100 kcal/kcal treatment than ME 3,000 kcal/kg (P<0.05). There were no differences in albumin, total cholesterol and glucose, but CP ($22{\times}20{\times}19$)18 treatment showed higher glucose than other treatments (P<0.05). Cooking loss, tenderness and water holding capacity were not different. However, pH was dependent on dietary ME, CP and existing the interaction between ME and CP treatments (P<0.05). As the results of this experiment, ME and CP were confirmed the 3,000 kcal/kg, 22% for the first two weeks 3,100 kcal/kg, 21% from three to five weeks of age, 3,100 kcal/kg, 18% for the growing period, 3,100 kcal/kg, 17% for the rest of period. However, further research would be required to confirm more optimum dietary nutrition for cross bred chicks.

Influence of Arg72 of pharaonis Phoborhodopsin on M-intermediate Decay and Proton Pumping Activity

  • Ikeura, Yukako;Shimono, Kazumi;Iwamoto, Masayuki;Sudo, Yuki;Kamo, Naoki
    • Journal of Photoscience
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    • v.9 no.2
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    • pp.311-313
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    • 2002
  • X-ray structures of pharaonis phoborhodopsin (ppR) show the different direction of the side chain of Arg72 from that of the corresponding residue (Arg82) of bacteriorhodopsin, BR. For BR, this residue is considered to play an important role in the proton pumping. In order to investigate the role of Arg72 in ppR, we constructed Arg72 mutants of R72A, R72K and R72Q, and measured the photocycle and proton pumping activities. The pH-titration curves on the absorption maximum of the mutants were shifted to alkaline in comparison of that of the wild-type. This may imply the increase of pKa of D75, suggesting the presence of the (probably electric) interaction between D75 and Arg72. Rate constants of the M-decay were 3-7 times faster than that of the wild-type, and the time for the completion of the photocycling was also reduced. Using Sn0$_2$ electrode, the rate of transmembrane proton transport was measured upon illumination. The photo-induced proton pumping activities were estimated after the corrections that are the percentages of the associated form of D75 (which has no pumping activity) and the photocycling rates. R72A and R72Q showed the reduced activity while R72K did not reduce the activity.

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Mechanisms of Selective Antimicrobial Activity of Gaegurin 4

  • Kim, Hee-Jeong;Lee, Byeong-Jae;Lee, Mun-Han;Hong, Seong-Geun;Ryu, Pan-Dong
    • The Korean Journal of Physiology and Pharmacology
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    • v.13 no.1
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    • pp.39-47
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    • 2009
  • Gaegurin 4(GGN 4), an antimicrobial peptide isolated from a Korean frog, is five times more potent against Gram-positive than Gram-negative bacteria, but has little hemolytic activity. To understand the mechanism of such cell selectivity, we examined GGN4-induced $K^+$ efflux from target cells, and membrane conductances in planar lipid bilayers. The $K^+$ efflux from Gram-positive M. luteus(2.5 ${\mu}g/ml$) was faster and larger than that from Gram-negative E. coli(75 ${\mu}g/ml$), while that from RBC was negligible even at higher concentration(100 ${\mu}g/ml$). GGN4 induced larger conductances in the planar bilayers which were formed with lipids extracted from Gram-positive B. subtilis than in those from E. coli(p<0.01), however, the effects of GGN4 were not selective in the bilayers formed with lipids from E. coli and red blood cells. Addition of an acidic phospholipid, phosphatidylserine to planar bilayers increased the GGN4-induced membrane conductance(p<0.05), but addition of phosphatidylcholine or cholesterol reduced it(p<0.05). Transmission electron microscopy revealed that GGN4 induced pore-like damages in M. luteus and dis-layering damages on the outer wall of E. coli. Taken together, the present results indicate that the selectivity of GGN4 toward Gram-positive over Gram-negative bacteria is due to negative surface charges, and interaction of GGN4 with outer walls. The selectivity toward bacteria over RBC is due to the presence of phosphatidylcholine and cholesterol, and the trans-bilayer lipid asymmetry in RBC. The results suggest that design of selective antimicrobial peptides should be based on the composition and topology of membrane lipids in the target cells.

The correlation between Spin Polarized Tunneling and Magnetic Moment in Co-Mn and Co-Fe Alloy Films (Co1-xFex와 Co1-xMnx 강자성 전이 합금 박막의 자기 모멘트와 터널 접합에 의한 스핀 편극치의 상관관계 연구)

  • Choi, Deung-Jang;Jang, Eun-Young;Lee, Nyun-Jong;Kim, Tae-Hee
    • Journal of the Korean Magnetics Society
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    • v.17 no.5
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    • pp.194-197
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    • 2007
  • Understanding the spin polarization (P) has been an ongoing research challenge. The $Co_{1-x}Mn_x$ (x=0.27, 1) and $Co_{1-x}Fe_x$ (x=0, 0.5, 1) films were prepared using UHV-MBE system. For these films, the magnetic properties and spin polarization were investigated using SQUID and Meservey-Tedrow technique, respectively. Although measured P is uncorrelated to the bulk magnetic moment (M) in Co-Fe and Ni-Fe alloy films, it correlates with M in some alloys such as Co-Mn and Ni-Cu. The results can be understood by the tunneling currents made up of the hybridized sp-d electrons near the Fermi-energy level. Our work shows the feasibility to tailor new materials with large P values.