• Title/Summary/Keyword: CB-1A

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SR144528 as Inverse Agonist of CB2 Cannabinoid Receptor

  • M.H. Rhee;Kim, S.K.
    • Proceedings of the Korean Society of Embryo Transfer Conference
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    • 2002.11a
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    • pp.96-96
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    • 2002
  • We examined the role of SR 144528 (N-[-(1S-endo-1,3,,3-trimethyl-bicycle[2, 2, 1 ] heptan-2-y1]-5-(-4-chloro-3-mothyl-phenyl)-(4-methylbenzyl)-pyrazole-3- carboxamide) in the modulation of certain AC isoforms in transiently transfected COS-7 cells. We found that CB2 in COS cells has a constitutive activity, and thus leading to inhibition of AC-V activity even in the absence of agonist. In addition, this constitutive modulation of AC is reversed by SR144528. It is now well established that several G protein-coupled receptors can signal without agonist stimulation(constitutive receptors). Inverse agonists have been shown to inhibit the activity of such constitutive G protein-coupled receptor signaling. Agonist activation of the G$\_$i/o/-coupled peripheral cannabinoid receptor CB2 normally inhibits adenylyl cyclase type V and stimulates adenylyl cyclase type II. Using transfected COS cells, we show here that application of SR144528, an inverse agonist of CB2, leads to a reverse action (stimulation of adenylyl cyclase V and inhibition of adenylyl cyclase II). This inverse agonism of SR144528 is dependent on the temperature, as well as on the concentration of the cDNA of CB2 transfected. Pertussis toxin blocked the regulation of adenylyl cyclase activity by SR 144528.

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Fluorescence Enhancement of 7-Diethylamino-4-methylcoumarin by Noncovalent Dipolar Interactions with Cucurbiturils

  • Park, Mee Ock;Moon, Myung Gu;Kang, T.J.
    • Bulletin of the Korean Chemical Society
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    • v.34 no.5
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    • pp.1378-1382
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    • 2013
  • We have investigated the complex forming behavior of cucurbit[6]urils(CB6) and cucurbit[7]urils(CB7) with 7-diethylamino-4-methylcoumarin(C460) in water. The electronic absorption maximum of C460 shows bathochromic shift with the addition of CB7 and fluorescence intensity is greatly increased, while CB6 has no noticeable effects on the spectroscopic properties of C460. It is noted that CB7 interacts more strongly with C460 than CB6 does. Fluorescence lifetime also significantly increased for the CB7 complex, which is attributed to reduced polarity surrounding C460 and/or C460 being in a restricted environment. The stoichiometry for the complex formation determined from the fluorescence titration measurement indicates that 2:1 complex in which two CB7 molecules bind to C460 is formed. Thus, two step equilibrium processes are suggested for the complex formation and the binding constants are estimated. The semi-empirical electronic structures calculations indicate that C460 is not included in the CB7 cavity but interacts noncovalently with the portal carbonyls of CB7.

A Study on the Stabilization Effects of 1-Chlorobutadiene-Butadiene Copolymer by Triazine Thiol Derivative (Triazine Thiol 유도체(誘導體)에 의한 1-Chlorobutadiene-Butadiene Copolymer의 안정화효과(安定化效果)에 관한 연구(硏究))

  • Yoo, Chong-Sun;Yamashita, S.;Paik, Nam-Chul
    • Elastomers and Composites
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    • v.22 no.2
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    • pp.109-120
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    • 1987
  • In this study, as one of the developing ways of the functional elastomer, improvement of the functionality of CB-BR was attemped through stabilization. At first the stabilization effect of CB-BR and the concentration dependancy in CB-BR were determined. Then, triazine thiol derivative(BPTT) was synthesized by reacting p-aminodiphenylamine with cyanuric chloride. Further the functional mechanism and the effects of the antioxidants were investigated using BPTT together with other various antioxidants in liquid and solid states. The results obtained are as follows: 1) The aging of CB-BR depended on the concentration and temperature. Thus, at a low temperature of $50^{\circ}C$, the aging proceeded with gel formation; at high temperature above $100^{\circ}C$ and in above 4wt% concentration, the aging occured by the formation of gel. And in concentrations below that, the aging proceeds with a decomposition caused by oxygen attacked to elastomer molecules. 2) The effect of antioxidation of CB-BR in the liquid state was at it's best when the MBIZ and BPTT were used at $110^{\circ}C$, 4hrs after the oxidation. 3) The effect of antioxidation of CB-BR in the solid state was the best choice the simultaneous use of NDBC and BPTT at $50^{\circ}C$, 30days after the oxidation.

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Anti-nociceptive Effect of Curcuma longa Extract on Acetic Acid induced Pain Model (강황 에탄올 추출물 및 그 분획물의 초산 유발에 의한 통증억제 효과)

  • Yoon, Won Ho;Lee, Keyong Ho
    • Korean Journal of Pharmacognosy
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    • v.46 no.3
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    • pp.229-233
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    • 2015
  • The anti-nociceptive effect of an ethanol extract and its various solvent fractions from Curcuma longa Linne ethanol extract was studied using the writhing test in mice. Different fractions by various solvent extraction from Curcuma longa Linne ethanol extract were administered orally 1 hr or time-course (0.5, 1, 2 and 5 hr) before intraperitoneal injection of acetic acid. After treatment with 30% ethanol extract and n-butanol fraction, CB-1, at a dose of 250 mg/kg, the significant writhing responses were 87.5 ± 13.4 (inhibition rate 31%, p<0.01) and 75.1 ± 11.1 (inhibition rate 41%, p<0.01) lower than the control group. At the dose of CB-1 50 mg/kg and 250 mg/kg, CB-1 showed a similar activity comparing to diclofenac of 10 mg/kg. A time-course experiment was performed, which involved oral administration of CB-1 (250 mg/kg) at 0, 0.5, 1, 2, and 5 hr before acetic acid intraperitoneal injection. The most effective time of CB-1 was 30 min before treatment and persisting until 2 hr. This study showed that Curcuma longa Linne has anti-nociceptive properties comparable with those of diclofenac, which suggests promise for the treatment of intractable visceral pain in humans. Major components of the active fraction are identified as curcumin, cyclocurcumin and demethoxycurcumin.

Chitin from Cuttlebone Activates Inflammatory Cells to Enhance the Cell Migration

  • Lim, Sung Cil;Lee, Ki-Man;Kang, Tae Jin
    • Biomolecules & Therapeutics
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    • v.23 no.4
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    • pp.333-338
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    • 2015
  • Our previous report showed that the extract from cuttlebone (CB) had wound healing effect in burned lesion of rat and the extract was identified as chitin by HPLS analysis. We herein investigated the morphology in CB extract using scanning electron microscope (SEM). Chitin was used as a control. There is no difference in morphology between CB extract and chitin. We also assessed the role of CB extract on the production of inflammatory mediators using murine macrophages and the migration of inflammatory cells. The extract induced the production of nitric oxide (NO) in macrophages. While the extract of CB itself stimulated macrophages to increase the expression of pro-inflammatory cytokines such as tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-$1{\beta}$, and IL-6, CB extract suppressed the production of those cytokines by LPS. CB extract also induced the production of mouse IL-8 which is related to the cell migration, and treatment with CB enhanced fibroblast migration and invasion. Therefore, our results suggest that CB activates inflammatory cells to enhance the cell migration.

Design of LLCL Filter for Single Phase Inverters with Confined Band Variable Switching Frequency (CB-VSF) PWM

  • Attia, Hussain A.;Freddy, Tan Kheng Suan;Che, Hang Seng;El Khateb, Ahmad H.
    • Journal of Power Electronics
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    • v.19 no.1
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    • pp.44-57
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    • 2019
  • Recently, the use of LLCL filters for grid inverters has been suggested to give better harmonic attenuation than the commonly used L and LCL filters, particularly around the switching frequency. Nevertheless, this filter is mainly designed for constant switching frequency pulse width modulation (CSF PWM) methods. In variable switching frequency PWM (VSF PWM), the harmonic components are distributed across a wide frequency band which complicates the use of a high order filter, including LCL and LLCL filters. Recently, a confined band variable switching frequency (CB-VSF) PWM method has been proposed and demonstrated to be superior to the conventional constant switching frequency (CSF) PWM in terms of switching losses. However, the applicability of LLCL filters for this type of CB-VSF PWM has not been discussed. In this paper, the authors study the suitability of an LLCL filter for CB-VSF PWM and propose design guidelines for the filter parameters. Using simulation and experimental results, it is demonstrated that the effectiveness of an LLCL filter with CB-VSF PWM depends on the parameters of the filters as well as the designed variable frequency band of the PWM. Simulation results confirm the performance of the suggested LLCL design, which is further validated using a lab scale prototype.

A Study on Curing Reaction of 1-Chlorobutadiene-Butadiene Copolymer by Moisture (1-Chlorobutadiene-Butadiene Copolymer의 수가교반응(水架橋反應)에 관한 연구(硏究)(II))

  • Yoo, Chong-Sun;Paik, Nam-Chul
    • Elastomers and Composites
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    • v.22 no.4
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    • pp.305-313
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    • 1987
  • In this study, as one of the developing ways of the functional elastomer, improvement of the functionality of 1-Chlorobutadiene-Butadiene Copolymer(CB-BR) was attempt through curing reaction by moisture. The curing reaction of CB-BR was determined an use of $\gamma$-Aminopropyltriethoxysilane(APS) and $\gamma$-Aminopropylmethyldiethoxysilane(ADS) as a crosslinking agent with filler at so the uncrosslinked elastomer was exposured in the air and curing reaction by moisture in the air was studied. The results obtained are as follows. 1. APS was more efficient than ADS as a crosslinking agent for CB-BR 2. Optimum amount of APS for moisture cured elastomer was r=1.5(at the ratio of $[APS]/[Cl^*]$) also in case(r=1.5), elastomer formed after soaking $T_{72}$ had similar physical properties with elastomer crosslinked by sulfur and it was very good. 3. Uncrosslinked elastomer(CB-BR+APS+Silica) was easily crosslinked by exposure to the air, and the physical properties was also satisfactory.

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Cloning and Characterization of a Gene Coding for a Dextransucrase from Leuconostoc mesenteroides B-742CB (Leuconostoc mesenteroides B-742CB로부터 Dextransucrase를 Coding하는 유전자 분리 및 특성 연구)

  • 박미란;이소영;류화자;김호상;강희경;유선균;조성용;조동련;김도만
    • KSBB Journal
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    • v.16 no.2
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    • pp.188-199
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    • 2001
  • A gene encoding the dextransucrase(dsCB) that synthesizes mostly $\alpha-(1\rightarrow6)$ linked dextran with low amount(10%) of $\alpha-(1\rightarrow3)$ branching was cloned and sequenced from Leuconostoc mesenteroides B-742CB. The 6.1 kbp DNA fragment carrying dsCB showed one open reading frame(ORF) composed of 4,536bp. The deduced amino acid sequence shows that it begins from the start codon(ATG) at position 698 of the cloned DNA fragment and extends to the termination condon(TAA) at position 5,223. The enzyme is consisted of 1,508 amino acids and has an calculated molecular mass of 168.6kDa. This calculated Mw was in good agreement with an activity band of 170kDa on non-denaturing SDS-PAGE. A recombinant E. coli DH5 $alpha$ harboring pDSCB produced extracellular dextransucrase in 2% sucrose medium, and synthesized both soluble and insoluble dextran. To compare the properties of enzyme with B-742CB dextransucrase, the acceptor reaction, hydrolysis of dextran and methylation were performed. The expressed enzyme showed the same properties as B-742CB dextransucrease, but its ability to synthesize $\alpha-(1\rightarrow3)$ branching was lower than that of B-742CB dextransucrase. In order to identify the critical amino acid residues known as conserved regions related to catalytic activity, Asp-492 was replaced with Asn. D492N resulted in a 1.6 fold decrease in specific activity.

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A Study On the Integration Reasoning of Rule-Base and Case-Base Using Rough Set (라프집합을 이용한 규칙베이스와 사례베이스의 통합 추론에 관한 연구)

  • Jin, Sang-Hwa;Chung, Hwan-Mook
    • The Transactions of the Korea Information Processing Society
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    • v.5 no.1
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    • pp.103-110
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    • 1998
  • In case of traditional Rule-Based Reasoning(RBR) and Case-Based Reasoning(CBR), although knowledge is reasoned either by one of them or by the integration of RBR and CBR, there is a problem that much time should be consumed by numerous rules and cases. In order to improve this time-consuming problem, in this paper, a new type of reasoning technique, which is a kind of integration of reduced RB and CB, is to be introduced. Such a new type of reasoning uses Rough Set, by which we can represent multi-meaning and/or random knowledge easily. In Rough Set, solution is to be obtained by its own complementary rules, using the process of RB and CB into equivalence class by the classification and approximation of Rough Set. and then using reduced RB and CB through the integrated reasoning.

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Experimental study on the strength behavior of cement-stabilized sand with recovered carbon black

  • Chhun, Kean Thai;Choo, Hyunwook;Kaothon, Panyabot;Yune, Chan-Young
    • Geomechanics and Engineering
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    • v.23 no.1
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    • pp.31-38
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    • 2020
  • Soil-cement stabilization is a type of ground improvement method which has been used to improve the engineering properties of soil. The unconfined compression test is the commonly used method to evaluate the quality of the stabilized soil due to its simplicity, reliability, rapidity and cost-effectiveness. The main objective of this study was to evaluate the effect of recovered carbon black (rCB) on the strength characteristic of cement-stabilized sand. Various rCB contents and water to cement ratios (w/c) were examined. The unconfined compression test on stabilized sand with different curing times was also conducted for a reconstituted specimen. From the test result, it was found that the compressive strength of cement-stabilized sand increased with the increase of the rCB content up to 3% and the curing time and with the decrease of the w/c ratio, showing that the optimum rCB concentration of the tested stabilized sand was around 3%. In addition, a prediction equation was suggested in this study for cement-stabilized sand with rCB as a function of the w/c ratio and rCB concentration at 14 and 28 days of curing.