• Title/Summary/Keyword: P-M interaction

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Interaction of Antihistaminics with Muscarinic Receptor(I) -Action on the cardiac muscarinic receptor- (항(抗) Histamine제(劑)와 Muscarinic Receptor와의 상호작용(相互作用)(I) -심장(心臟) muscarinic receptor에 대한 작용(作用)-)

  • Lee, Shin-Woong;Park, Yeung-Joo;Lee, Jeung-Soo;Ha, Kwang-Won;Jin, Kap-Duck
    • YAKHAK HOEJI
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    • v.32 no.2
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    • pp.101-111
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    • 1988
  • $[^3H]$ Quinuclidinyl benzilate(QNB) binding assays were performed in the dog ventricular sarcolemma fraction enriched approx. 32-fold in sarcolemma compared to the starting homogenate to elucidate the effect of antihistaminics on cardiac muscarinic receptor. Chlorpheniramine(CHP) inhibited specific binding of $[^3H]$QNB and delayed the equilibrium binding. The rate constants at $37^{\circ}C$ for formation and dissociation of the QNB receptor complex were $0.38{\times}10^9\;M^{-1}$ and $1.6{\times}10^{-2}\;min^{-1}$, respectively. The mean value for the dissociation constant from the pairs of the rate constants was 43. 2 pM and this value was similar to the value(44.8pM) determined from Scatchard analysis. CHP decreased association rate constant, indicating increase in $K_D$ value. Decrease in affinity without affecting the binding site concentration$(B_{max})$ for $[^3H]$QNB binding by CHP was also demonstrated by Scatchard analysis. $K_i$ values for $H_i$-blockers that inhibited specific $[^3H]$QNB binding were $0.02{\sim}4.8{\mu}M$. Cimetidine with $K_i$ value of $230{\mu}M$, however, was ineffective in displacing $[^3H]$QNB binding at concentration of $50{\mu}M$. The Hill coefficient for $H_1$-blockers were about one. The results indicate that $H_1$-antihistaminics inhibit $[^3H]$ QNB binding by interaction with myocardiac muscarinic cholinergic receptor and anticholinergic side effects of these drugs are mainly due to this receptor blocking mechanism.

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The interaction of zipeprol with $\beta$-cyclodextrin

  • Kim, Chong-Kook;Choi, Han-Gon
    • Archives of Pharmacal Research
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    • v.10 no.2
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    • pp.69-74
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    • 1987
  • The characteristics of zipeprol-$\beta$-cyclodextrin system were studied by circular dichroism, competitive UV method and dialysis method. In this experiment, binding constants by competitive UV method, circular dichroism and dialysis method were 155 M$^{-1}$ 187 M$\^{-1}$/($\pm$ 5%) and 315 $^{-1}$, repectively. It shows that zipeprol forms 1:1 compelx with $\beta$-cyclodextrin by circular dichroism and 1:2 by dialysis method. pH profile shows that binding force seems to be a hydrophobic interaction. It is suggested that benzene ring be accomodated in the cavity of $\beta$-cyclodextrin.

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Emulsion Liquid Membrane Transport of Heavy Metal Sons by Macrocyclic Carriers (거대고리 운반체에 의한 중금속이온의 에멀죤 액체막 수송)

  • 정오진
    • Journal of Environmental Science International
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    • v.4 no.2
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    • pp.223-232
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    • 1995
  • New two macrocyclic compounds using as carriers of liquid emulsion menbrame, have been synthesized. These reuslts provide evidance for the usefulness of the theory in designing the systems. The efficiency of selective transport for heavy metal ions have been discussed from the membrane systems that make use of $SCN^-$,<>,$I^-$,CN- and $Cl^-$ ion as co-anions in source phase and make use of $S_2O_3^{2-}$ and $P_2O_7^{4-}$ ion as receiving phase, respectively. The transport rate of M(II) was highest when a maximum amount of the M(II) in the source phase was present as$Cd(SCN)_2$$(P[SCN^-]= 0.40M)$, $Hg(SCN)_2([SCN^-]=0.40M)$ and Pd(CN)$([CN^-]= 0.40M)$. The Cd(II) and Pb(II) over each competitive cations were well transprted with 0.3M-S2032- and 0.3M-P2O74-, respectively in the receiving phase. Results of this study indicate that two criteria must be met in order to have effective macrocycle-mediated transport in these emulsion system. First one must effective extraction of the $M^{n+}$ into the toluene systems. The effectiveness of this extraction is the greatest if locK for $M^{n+}$macrocycle interaction is large and if the macrocycle is very insoluble in the aqueous phase. Second, the ratio of the locK values (or Mn+-receiving phase ($S_2O_3^{2-}$- or $P_2O_7^{4-}$) to $M^{n+}$-macrocycle (($L_1$이나 $L_2$) interaction must be large enough to ensure quantitative stripping of Mn+(($Cd^{2+}$,$Pb^{2+}$)at the toluene receiving Phase interface. $L_1$(3.5-benzo-10,13,18,21-tetraoxa-1,7,diazabicyclo(8,5,5) eicosan) forms a stable ($Cd^{2+}$ and >,$Pb^{2+}$ complexes and $L_1$ is very insoluble in water and its $Cd^{2+}$ and >,$Pb^{2+}$ complex is considerably less stable than $Cd^{2+}$-(S2O3)22- and $Pd^{2+}-P_2O_7^{4-}$ complexes. On the other hand, the stability of the $Hg^{2+}$)+-$L_1$( complex exceed that of the $Hg^{2+}$- (S2O3)22- and Hg2+-P2O74-, and the distribution coefficient of $L_2$(5,8,15,18,23,26-hexaoxa-1,12- diazabicyclo-(10,8,8) octacosane) is much smaller than that of $L_1$. Therefore, the partitioning of Lr is favored by the aqueous receiving Phase, and little heavy metal ions transport is seen despite the large logK for $Hg^{2+}$+-$L_1$ and $Mn^+$($Cd^{2+}$+, $Pb^{2+}$+ and $Hg^{2+}$)-$L_2$ interactions. Key Words : macrocycles, transport, heavy metal, co-anion, source phase, receiveing, complex separation, interaction, destribution coefficient.

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Self-Assembled and Alternative Porphyrin-Phthalocyanine Array

  • Kwag, Gwang-Hoon;Park, Eun-Joo;Kim, Sung-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.25 no.2
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    • pp.298-300
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    • 2004
  • An alternative molecular porphyrin-phthalocyanine aggregate was prepared and characterized with UV-visible and X-ray absorption spectroscopies. UV-visible experiments evidence 1-dimensional porphyrin-phthalo-cyanine array formed by mixing $SnTPPCl_2 ({\lambda}_{max}=429,\;{\varepsilon}=2.4{\times10^ 5 /M{\cdot}cm)\;and\;NiPc(OBu)_8({\lambda}_{max}=744 nm,\;{\varepsilon}= 2.0{\times}10^ 5 /M{\cdot}cm)$ in solution. In the UV-visible spectrum of the porphyrin-phthalocyanine array, $(SnPNiPc)_n$, a new Q-band appeared at 844 nm with decrease of the Q-band peak of $NiPc(OBu)_8$ at 744 nm. The red-shift of Q-band evidences an alternative porphyrin-phthalocyanine array formed in solution through metal-halide interaction rather than ${\pi}-{\pi}$ facial interaction, in which nickel of $NiPc(OBu)_8$ coordinates with chloride of $SnTPPCl_2$ through self assembly. Ni K-edge XANES (X-ray absorption near edge structure) spectra also support the axial ligation of nickel to chloride. The square planar structure of $NiPc(OBu)_8$ turns to an octahedral structure in (SnPNiPcSnP) by axial ligation. A higher energy-shift (0.2 eV) of the preedge peak of (SnPNiPcSnP) indicaties partial oxidation of nickel by charge transfer from NiPc$(OBu)_8$ to SnTPPCl$_2$.

Load carrying capacity of deteriorated reinforced concrete columns

  • Tapan, Mucip;Aboutaha, Riyad S.
    • Computers and Concrete
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    • v.6 no.6
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    • pp.473-490
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    • 2009
  • This paper presents a new methodology to evaluate the load carrying capacity of deteriorated non-slender concrete bridge pier columns by construction of the full P-M interaction diagrams. The proposed method incorporates the actual material properties of deteriorated columns, and accounts for amount of corrosion and exposed corroded bar length, concrete loss, loss of concrete confinement and strength due to stirrup deterioration, bond failure, and type of stresses in the corroded reinforcement. The developed structural model and the damaged material models are integrated in a spreadsheet for evaluating the load carrying capacity for different deterioration stages and/or corrosion amounts. Available experimental and analytical data for the effects of corrosion on short columns subject to axial loads combined with moments (eccentricity induced) are used to verify the accuracy of proposed model. It was observed that, for the limited available experimental data, the proposed model is conservative and is capable of predicting the load carrying capacity of deteriorated reinforced concrete columns with reasonable accuracy. The proposed analytical method will improve the understanding of effects of deterioration on structural members, and allow engineers to qualitatively assess load carrying capacity of deteriorated reinforced concrete bridge pier columns.

Effect of cold water immersion after rowing ergometer on blood fatigue substance, reactive oxygen species and anti-oxidation enzyme in rowing athletes (조정 선수의 로잉 에르고미터 수행 후 저온침수 처치가 혈중 피로 물질, 활성산소 및 항산화 효소에 미치는 영향)

  • Hyun-Wook Hong;Su-han Koh;Tae-kyu Kim;Min-Kyo Kim;Do-yeon Kim
    • Journal of the Korean Applied Science and Technology
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    • v.40 no.4
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    • pp.761-772
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    • 2023
  • The purpose of this study is to help a recovery of fatigue through the effect of cold immersion treatment after rowing ergometer on blood fatigue substance, MDA and SOD in rowing athletes. For this, 10 subjects participated in this study and we divided them into cold water immersion group (CWI, n=10), non-cold immersion group (NCI, n=10). The exercise program was performed to 2000 m rowing ergometer for maintaining high intensity. The data was collected with regard to the interaction effect of the group and time among the CWI and NCI, ANOVA was used. As the post-hoc test, Bonferroni test was used. The significance was set at .05 and the following conclusions were deduced. For lactic acid, there were the main effect of time (p<.001) and significant difference in the both group (p<.001). Also, LDH were significant difference in the each group (p<.05). For MDA, there were the interaction between group and time (p<.05) and the main effect of group (p<.05) and time (p<.001). SOD were indicated main effect of group and time (p<.05), there was significant difference between each group in the after 30 min recovery (p<.05). Collectively, The results of this study suggest that positive effect on blood fatigue substances, reactive oxygen species and anti-oxidation enzyme through cold water immersion intervention. Therefore, we strongly recommend that performing the cold immersion intervention would be beneficial after high intervention exercise.

Removal of Red Tide Organisms -1. flocculation of Red Tide Organisms by Using IOSP- (적조생물의 구제 -1. IOSP에 의한 적조생물의 응집제거-)

  • KIM Sung-Jae;CHO Kyu-Dae
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.33 no.5
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    • pp.448-454
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    • 2000
  • This study was to examine the physicochemical characteristics of coagulation reaction between ignited oyster shell powder (IOSP) and red tide organisms (RTO), and its feasibility, in developing a technology for the removal of RTO bloom in coastal sea,IOSP was made from oyster shell and its physicochemical characteristics were examined for particle size distribution, surface characteristic by scanning electron microscope, zeta potential, and alkalinity and pH variations in sea water. Two kinds of RTO that were used in this study, Cylindrotheca closterium and Skeletonema costatum, were sampled in Masan bay and were cultured in laboratory. Coagulation experiments were conducted using various c(Incentrations of IOSP, RTO, and a jar tester. The supernatant and RTO culture solution were analyzed for pH, alkalinity, RTO cell number, IOSP showed positive zeta potentials of $11.1{\~}50.1\;mV\;at\;pH\;6.2{\~}12.7$, A positive zeta potential of IOSP slowly decreased with decreasing pNa 4,0 to 2,0. When pNa reached zero, the zeta potential approached zero, When a pMg value was decreased, the positive zeta potential of IOSP increased until pMg 3.0 and decreased below pMg 3.0. IOSP showed 4.8 mV of positive zeta potential while RTO showed -9.2 mV of negative zeta potential in sea water. A positive-negative EDL (electrical double-layer) interaction occurred between $Mg(OH)_2$ adsorption layer of IOSP and RTO in sea water so that EDL attractive force always worked between them. Hence, their coagulation reaction occurred at primary minimum on which an extreme attractive force acted because of charge neutralization by $Mg(OH)_2$ adsorption layer of IOSP. As a result, the coagulation reaction was rapidly processed and was irreversible according to DLVO (Deriaguin-Landau-Verwey-Overbeek) theory. Removal rates of RTO were exponentially increased with increasing both IOSP concentration and G-value. The removal rates were steeply increased until 50 mg/l of IOSP and reached $100{\%}\;at\;400\;mg/l$ of IOSP. Removal rates of RTO were $70.5,\;70.5,\;81.7,\;85.3{\%}$ for G-values of $1,\;6,\;29,\;139\;sec^(-1)$at IOSP 100 mg/l, respectively. This indicated that mixing (i.e., collision among particles) was very important for a coagulation reaction.

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Fluid-structure interaction analysis of sloshing in an annular - sectored water pool subject to surge motion

  • Eswaran, M.;Goyal, P.;Reddy, G.R.;Singh, R.K.;Vaze, K.K.
    • Ocean Systems Engineering
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    • v.3 no.3
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    • pp.181-201
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    • 2013
  • The main objective of this work is to investigate the sloshing behavior in a baffled and unbaffled three dimensional annular-sectored water pool (i.e., tank) which is located at dome region of the primary containment. Initially two case studies were performed for validation. In these case studies, the theoretical and experimental results were compared with numerical results and good agreement was found. After the validation of present numerical procedure, an annular-sectored water pool has been taken for numerical investigation. One sector is taken for analysis from the eight sectored water pool. The free surface is captured by Volume of Fluid (VOF) technique and the fluid portion is solved by finite volume method while the structure portions are solved by finite element approach. Baffled and un-baffled cases were compared to show the reduction in wave height under excitation. The complex mechanical interaction between the fluid and pool wall deformation is simulated using a partitioned strong fluid-structure coupling.

A New Approach for Thermodynamic Study on the Binding of Human Serum Albumin with Cerium Chloride

  • Rezaei Behbehani, G.;Divsalar, A.;Saboury, A.A.;Faridbod, F.;Ganjali, M.R.
    • Bulletin of the Korean Chemical Society
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    • v.30 no.6
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    • pp.1262-1266
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    • 2009
  • Thermodynamics of the interaction between Cerium (III) chloride, $Ce^{3+}$, with Human Serum Albumin, HSA, was investigated at pH 7.0 and $27\;{^{\circ}C}$ in phosphate buffer by isothermal titration calorimetry. Our recently solvation model was used to reproduce the enthalpies of HSA interaction by $Ce^{3+}$. The solvation parameters recovered from our new model, attributed to the structural change of HSA and its biological activity. The interaction of HSA with $Ce^{3+}$ showed a set of two binding sites with negative cooperativity. $Ce^{3+}$ interacts with multiple sites on HSA affecting its biochemical and biophysical properties.

Spectroscopic Studies on the Mechanism of Interaction of Vitamin $B_{12}$ with Bovine Serum Albumin

  • Kamat, B.P.;Seetharamappa, J.
    • Journal of Photoscience
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    • v.11 no.1
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    • pp.29-33
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    • 2004
  • The mechanism of interaction of cyanocobalamin (CB) with bovine serum albumin (BSA) has been investigated by spectrofluorometric and circular dichroism methods. Association constant for the CB-BSA system showed that the interaction is non-covalent in nature. Binding studies in the presence of an hydrophobic probe, 8-anilino-l-naphthalene sulphonic acid, sodium salt (ANS) showed that there is hydrophobic interaction between CB and ANS and they do not share common sites in BSA. Stern-Volmer analysis of fluorescence quenching data showed that the fraction of fluorophore (protein) accessible to the quencher (CB) was close to unity indicating thereby that both tryptophan residues of BSA are involved in drug-protein interaction. The rate constant for quenching, greater than $10^{10}$ $M^{-1}$ $s^{-1}$, indicated that the drug binding site is in close proximity to tryptophan residue of BSA. Thermodynamic parameters obtained from data at different temperatures showed that the binding of CB to BSA involves hydrophobic bonds predominantly. Significant increase in concentration of free drug was observed for CB in presence of paracetamol. Circular dichroism studies revealed the change in helicity of BSA due to binding of CB to BSA.

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