• Title/Summary/Keyword: Binding number

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Effect of Electrolytes on the Saturable Binding of Morphine in Rat Brain Tissue (백서(白鼠) 뇌조직(腦組織)에서 Morphine의 Saturable Binding에 미치는 전해질(電解質)의 영향(影響))

  • Ko, Bok-Hyun;Chae, Soo-Wan;Cho, Kyu-Park
    • The Korean Journal of Pharmacology
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    • v.18 no.2
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    • pp.33-44
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    • 1982
  • The binding in vitro of an opiate agonist, $(^3H)-morphine$, was studied using rat brain slices which were incubated in the modified Krebs-Henseleit bicarbonate buffer solution containing various concentrations of electrolytes with or without morphine, naloxone or morphine+naloxone at $4^{\circ}C$ for 24 hours. The binding of $(^3H)-morphine$ may be seperated into two component; one a saturable binding and the other nonsaturable. The saturable binding may be calculated from the differences in binding observed in the absence and presence of high concentration of morphine. The maximal saturable binding and $K_D$ value in the naive preparations were $0.32{\pm}0.02\;pmole/mg$ protein and $0.75{\pm}0.07\;nM$ respectively. The saturable binding of $(^3H)-morphine$ was significantly increased by low temperature-treatment, while $K_D$ value was not changed. Morphine in the incubation media significantly increased the saturable binding of $(^3H)-morphine$ and $K_D$ value. Naloxone also increased the maximal saturable binding of $(^3H)-morphine$ and $K_D$ value of the drug. Decrease of $K^+\;and\;Mg^{++}$, and addition of $Mn^{++}$ in the incubation media significantly increased the saturable binding of $(^3H)-morphine$, but decrease of $Na^+$and increase of $Ca^{++}$ in the incubation media did not influence the binding. The increment of the saturable binding of $(^3H)-morphine$ by nonlabeled morphine in the incubation media was notaffected by decrease of $Na^+,\;K^+\;or\;Mg^{++}$, or addition of $Mn^{++}$ into the incubation media, but was inhibited by increase of $Ca^{++}$ in the incubation media, while the increment of the saturable binding of $(^3H)-morphine$ was net observed by decrease of $Na^+,\;K^+\;or\;Mg^{++}$, or increase of $Ca^{++}$ in the incubation media. The above results indicate that change of opiate binding sites in quality, i.e. affinity, and quantity, i.e. number of binding sites, may occur by low temperature-treatment in the absence and presence of morphine or naloxone and that electrolytes play role of the changes of opiate binding sites.

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Near-Field Detection of Aβ Proteins Using Micro Beads

  • Lee, Seung-Jun;Sung, Hee-Kyung;Choi, Yo-Han
    • Journal of Sensor Science and Technology
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    • v.21 no.5
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    • pp.319-323
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    • 2012
  • In this paper, we present the possibility of quantification analysis for $A{\beta}$ captured by micro beads using Near-filed detection. In order to evaluate detection efficiency, detected signals were compared with different sizes of micro beads and a varied number of micro beads. Also, $A{\beta}$ deposits and $A{\beta}$ binding to micro beads were measured, therefore, we observed the $A{\beta}$ deposit and light scattering around the surface of micro beads induced by attached $A{\beta}$. This method can be used for quantitative analysis for not only the number of $A{\beta}$, but also the binding ratio of $A{\beta}$ to micro beads.

Changes in the Central Dopaminergic Systems in the Streptozotocin-induced Diabetic Rats

  • Lim, D.K.;Lee, K.M.;Ho, I.K.
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.398-404
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    • 1994
  • The behavioral response, depamine metabolism, and characteristics of dopamine subtypes after developing the hyperlycemia were studied in the striata of rats. In animals developed hyperglycemia, the on-set duration of cataleptic behavior responded to SCH 23390 injection was delayed abd shortened, respectively. However, the cataleptic response to spiperone occurred significantly earlier in on-set and prolonged in duration. Dopamine metabolites, dihydroxyphenylacetic acid (DDPAC) and homovanillic acid (HVA), were significantly reduced in teh striata of hyeprglycemic rats. However, level of DA was significantly increased. It is noted that the ratios of DOPAC and HVA to DA were decreased, suggesting decreased tumover of DA. The affinity of striatal D-1 receptors was significantly increased without changes in the number of binding sites, while the maximum binding number of D-2 recptors was significantly increased without affecting its affinity in the diabetic rats. These results indicate that the dopaminergic activity in striatia was altered in hyperglycemic rats. Furthermore, it suggests that the upregulation of dopamine receptors might be due to the decreased dopamine matabolism.

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Effect of Ginseng Saponin on the $Na^{+}$, $K^{+}$-ATPase of Dog Cardiac Sarcolemma

  • Lee, Shin-Woong;Lee, Jeung-Soo;Kim, Young-Hie;Jin, Kap-Duck
    • Archives of Pharmacal Research
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    • v.9 no.1
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    • pp.29-38
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    • 1986
  • The effects of ginseng saponins on the sarcolemmal $Na^{+}$, $K^{+}$-ATPase were compared to gypsophila saponin, sodium dodecylsulfate (SDS), and Triton X-100 to elucidate whether the effects are due to the membrane distruption, using a highly enriched preparation of cardiac sarcolemma prepared from dog ventricular myocardium. About 26% and 29% of vesicles in the preparation, enriched in ouabain-sensitive $Na^{+}$, $K^{+}$-ATP ase, $\beta$-adrenergic and muscarinic receptors are rightside-out and inside-out orientation, respectively. Ginseng saponins (triol>total> diol) inhibited $Na^{+}$, $K^{+}$-ATP ase activity, $Na^{+}$, $K^{+}$-ATPase activity and [$^{3}$H]ouabain binding of sarcolemmal vesicles. However, gypsophila saponin, SDS (0.4$\mu$g/$\mu$g protein) and Triton X-100 (0.6 $\mu$g/$\mu$g protein) caused about 1.35 and 1.40-fold increase in $Na^{+}$, $K^{+}$-ATPase activity and [$^{3}$H] oubain binding, respectively. Especially, the activating effect of gypsophila saponin on membrane Na+, K+ ATPase was detected at gypsophila saponin to sarcolemmal protein ratios as high as 100. Low dose of ginseng saponin (3$\mu$g/$\mu$g protein) decreased the phosphorylation sites and the concentration of ouabain binding sites (Bmax) without affecting the turnover number and affinity for ouabain binding, while gypsophila saponin, SDS(0.4 ug/ug protein), ahd Triton X-100 (0.6$\mu$g/$\mu$g protein) increased the Bmax. The results suggest that ginseng saponins cause a decrease in the number of active sites by interacting directly with $Na^{+}$, $K^{+}$-ATPase before disruption of membrane barriers of sarcolemmal vesicles.

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Sensory Adaptation in Polar Auxin Transport System to Naphtylphthalamic Acid in Corn Coleoptile Segments (옥수수(Zea mays L.) 자엽초 절편에서 Naphtylphthalamic Acid에 대한 오옥신 이동계의 감지적응)

  • 윤인선
    • Journal of Plant Biology
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    • v.34 no.4
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    • pp.317-323
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    • 1991
  • Partial recovery in auxin transport capacity from inhibition by N-naphthylphthalamic acid (NPA) was observed when corn coleoptile segments were subjected to a prolonged NPA treatment. Kinetic data indicated that the recovery time is a function of the concentration of NPA applied. Desensitization to NPA was also seen in tissue slices where NPA increased net uptake of auxin, indicating that the apparant adaptation in the auxin transport system did not results possibly from auxin accumulated during transport inhibition. Studies on in vitro binding of NPA to membrane vesicles isolated from the coleoptile indicated that preincubation of the tissue with NPA resulted in the reduced binding activity. Scatchard analysis of the data indicated that this was due to decreases in the number of NPA binding sites. The possibility of causal relationship of modified NPA receptors to the sensory adaptation in auxin transport observed in coleoptile segments will be discussed.

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A Hardware Allocation and Binding Algorithm for ASIC Design (ASIC설계를 위한 하드웨어 할당 및 바인딩 알고리듬)

  • Choe, Ji-Yeong;In, Chi-Ho;Kim, Hui-Seok
    • The Transactions of the Korea Information Processing Society
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    • v.7 no.4
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    • pp.1255-1262
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    • 2000
  • This paper proposes a hardware allocation and binding algorithm for ASIC Design. The proposed algorithm works on schedules input graph and simultaneously allocates and binds functional units, interconnections and registers by considering interdependency between operations and storage elements in each control step, in order to share registers and interconnections connected to functional units, as much as possible. Especially, he register allocation is executes the allocation optimal using graph coloring. This paper shows the effectiveness of the algorithm by comparing experiments to determine number of functional unit and register in advance or to separate executing allocation and binding of existing system.

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Spectroscopic investigations on the interaction of bovine serum albumin with amoxicillin and cloxacillin

  • BHALCHANDRA P. KAMAT,
    • Journal of Photoscience
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    • v.12 no.1
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    • pp.11-15
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    • 2005
  • The mechanism of interaction of two drugs viz., amoxicillin and cloxacillin with bovine serum albumin has been investigated using fluorescence absorption and circular dichroism spectroscopy. The quenching mechanism of fluorescence of bovine serum albumin by amoxicillin and cloxacillin was discussed. The binding sites number n and apparent binding constant Kwere measured by fluorescence quenching method. The thermodynamic parameters obtained from data at different temperatures were calculated. The distance r between donor (bovine serum albumin) and acceptor (amoxicillin and cloxacillin) was obtained according to Forster theory of non-radiative energy transfer. The effect of common ions on binding constant was also investigated. The results of synchronous fluorescence spectra, UV-vis absorption spectra and circular dichroism of BSA in presence of amoxicillin and cloxacillin show that the conformation of bovine serum albumin changed

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Growth and Electronic Properties of Ag Overlayers on Stepped Pt(211) Surface

  • 김유권;김정원;김세훈
    • Bulletin of the Korean Chemical Society
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    • v.17 no.12
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    • pp.1154-1157
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    • 1996
  • The growth and electronic properties of ultrathin silver films deposited onto Pt(211) surface were studied using Auger electron spectroscopy (AES), low-energy electron diffraction (LEED), and x-ray photoelectron spectroscopy. The AES and LEED results indicate that the silver grows by a layer by layer growth followed by three dimensional islands growth. The XPS results show that the Ag 3d core-level binding energy of Ag overlayers on Pt(211) shifts toward lower binding energy relative to the bulk value at lower Ag coverage. This negative binding energy shift of the Ag 3d core level is explained by the reduced coordination number of the overlayer atoms and the resulting initial state band narrowing effect suggested by Wertheim and Citrin [Phys. Rev. Lett. 1978, 41, 1425].

Drug-biomacromolecule interaction IV

  • Kim, Chong-Kook;Yang, Ji-Sun;Lim, Yun-Su
    • Archives of Pharmacal Research
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    • v.6 no.1
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    • pp.55-62
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    • 1983
  • Binding of six cephalosporins (cefotaxime, cefuroxime, cefazoline, cephalothin, cephaloridine, cephacetrile) to bovine serum albumin was studied. Fluorescence probe technique and difference spectrophotometry were employed to evaluate the nature and degree of association of cephalosporin albumin complex. 1-Anilinonaphthalene-8-sulfonate (ANS) was used as the fluorescence probe. 2-(4'-hydroxybenzeneazo) benzoic acid(HBAB) was employed as the UV spectrophotometric probe. Compentitive bindings between cephalosporins and probes were observed. The number of binding sites of bovine serum albumin for each cephalcsporin is 2. Among six cephaloporins, cefotaxime has the highest binding constant followed by cafazoline, cefuroxime, cephalothin, cephaloridine and cephacetrile.

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DESIGN AND SYNTHESIS OF A3 ADENOSINE RECEPTOR LlGANDS, 2′-FLUORO ANALOGUES OF CI- IB-MECA

  • Park, Jae-Gyu;Kim, Hea-Ok;Moon, Hyung-Ryong;Jeong, Lak-Shin
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.365.1-365.1
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    • 2002
  • Since adenosine A3 receptor has been cloned from rat brain. a number of compounds have been synthesized and evaluated for the binding affinity to this receptor. Among these. 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-methylcarboxamide (2-CI-IB-MECA) has been found to be one of the most selective agonists (Ki = 1.0 nM) for rat adenosine A3 receptor. On the basis of the high binding affinity of 2-CI-IB-MECA to adenosine A3 receptor. it was interesting to find out whether 2'-hydroxyl group of 2-CI-IB-MECA is essential for the binding affnity to the receptor. (omitted)

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