• 제목/요약/키워드: Selective Mechanism

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Effects of Novel Potassium Channel Opener KR-30450 and its Metabolite KR-30818 on the Smooth, Muscle of the Guinea Pig

  • Jung, Yi-Sook;Moon, Chang-Hyun;Yoo, Sung-Eun;Shin, Hwa-Sup
    • Biomolecules & Therapeutics
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    • v.4 no.4
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    • pp.373-377
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    • 1996
  • The effect of potassium channel openers, KR-30450, KR-30818 and lemakalim have been compared against several spasmogens in guinea pig bronchi. In guinea pig bronchi, KR-30450 had a greater relaxant effect than lemakalim and KR-30818 against tone induced by histamine $10^{-5}M$ ($EC_{50}$ $\mu$M: KR-30450, 0.108$\pm$0.077; KR-30818, 0.403$\pm$0.023; lemakalim, 0.968$\pm$0.036) and prostaglandin $F_{2\alpha} 3\times10^{-6} M$ ($EC_{50}$ $\mu$M: KR-30450, 0.018$\pm$0.001; KR-30818, 0.028$\pm$0.003; lemakalim, 0.138$\pm$0.019). Relaxant effect of KR-30450 and KR-30818 were significantly reduced by 20 min pretreatment of tissues with $10^[-6}$ M glibenclamide, a selective blocker of ATP-sensitive potassium channel. Against acetylcholine-induced tone in guinea pig bronchi, however, these compounds had little effect. In summary, KR-30450 and KR-30818 showed greater relaxant effect than lemakalim in guinea pig bronchi (KR-30450>KR-30818>lemakalim). These relaxant actions are suggested to be mediated at least in part by a mechanism which involves the opening of ATP-sensitive potassium channel.

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Inhibitory Effects of Dihydrexidine on Catecholamine Release from the Rat Adrenal Medulla

  • Lee, Jae-Hwang;Lim, Hyo-Jeong;Lim, Dong-Yoon
    • Biomolecules & Therapeutics
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    • v.17 no.1
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    • pp.32-42
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    • 2009
  • The purpose of the present study was to examine the effect of dihydrexidine, a full $D_1$ receptor agonist, on the secretion of catecholamines (CA) from the perfused model of the rat adrenal gland, and to establish its mechanism of action. Dihydrexidine (10-100 ${\mu}M$), perfused into an adrenal vein for 60 min, relatively produced dose- and time-dependent inhibition in the CA secretory responses evoked by ACh (5.32 mM), high $K^+$ (56 mM), DMPP (100 ${\mu}M$) and McN-A-343 (100 ${\mu}M$). Dihydrexidine itself did fail to affect basal CA output. Also, in adrenal glands loaded with dihydrexidine (30 ${\mu}M$), the CA secretory responses evoked by Bay-K-8644 (10 ${\mu}M$), an activator of L-type $Ca^{2+}$ channels, cyclopiazonic acid (10 ${\mu}M$), an inhibitor of cytoplasmic $Ca^{2+}$-ATPase, and veratridine, an activator of voltage-dependent $Na+$ channels (10 ${\mu}M$), were also markedly inhibited, respectively. However, in the simultaneous presence of dihydrexidine (30 ${\mu}M$) and R (+)-SCH23390 (a selective antagonist of $D_1$ receptor, 3 ${\mu}M$), the CA secretory responses evoked by ACh, high K+, DMPP, McN-A-343, Bay-K-8644, cyclopiazonic acid and veratridine were considerably recovered to the extent of the corresponding control secretion compared with the inhibitory responses by dihydrexidinetreatment alone. In conclusion, these experimental results suggest that dihydrexidine significantly inhibits the CA secretion evoked by cholinergic stimulation (both nicotinic and muscarinic receptors) and membrane depolarization from the rat adrenal medulla. It seems that this inhibitory effect of dihydrexidine may be mediated by inhibiting influx of both $Ca^{2+}$ and $Na^+$ into the cytoplasm as well as by suppression of $Ca^{2+}$ release from cytoplasmic calcium store through activation of dopaminergic $D_1$ receptors located on the rat adrenomedullary chromaffin cells.

Design of the Fixed-Bed Catalytic Reactor for the Maleic Anhydride Production (무수마레인산 생산을 위한 고정층 촉매 반응기 설계)

  • Yoon, Young Sam;Koo, Eun Hwa;Park, Pan Wook
    • Applied Chemistry for Engineering
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    • v.10 no.3
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    • pp.467-476
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    • 1999
  • This paper analyzed the behavior of fixed-bed catalytic reactor (FBCR) which synthesizing maleic anhydride(MA) from the selective oxidation of n-butane. The behavior of FBCR describing convection-diffusion-reaction mechanism is examined by using two-dimensional pseudohomogeneous plug-flow transient model, with the kinetics of Langmuir-Hinshelwood type. Prediction model is composed by optimum parameter estimation from temperature profile, yield and conversion of single FBCR on operating condition variations of Sharma's pilot-plant experiment. A double FBCR with same yield and conversion for single FBCR generated a $8.96^{\circ}C$ lower hot spot temperature than a single FBCR. We could predict parametric sensitivity according to the variation of possible operating condition (temperature, concentration, volumetric flow of feed reactant and coolant flow rate) of single and double FBCR. Double FBCR showed the behavior of more operating range than single FBCR. Double FBCR with nonuniform activities could assure safety operation condition for the possible variation of operating condition. Also, double FBCR had slightly higher than the single FBCR in conversion and yield.

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Influence of 5′-(N′-Ethylcarboxanlido) Adenosine on Catecholarnine Secretion Evoked by Cholinergic Stimulation and Membrane Depolarization in the Rat Adrenal Gland

  • Lim, Dong-Yoon;Oh, Hyeong-Geun;Woo, Seong-Chang
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.338-348
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    • 2000
  • The present study was attempted to determine the effect of 5'-(N'-ethylcarboxamido) adenosine (NECA), which is an potent $A_2$-adenosine receptor agonist, on catecholamine (CA) secretion evoked by cholinergic stimulation, membrane depolarization and calcium mobilization from the isolated perfused rat adrenal gland. NECA (20 nM) perfused into the adrenal vein for 60 min produced a time-related inhibition in CA secretion evoked by ACh (5.32x10$^{-3}$ M), high $K^{+}$(5.6x10$^{-2}$ M), DMPP (10$^{-4}$ M for 2 min), McN-A-343 (10$^{-4}$ M for 2 min), cyclopiazonic acid (10$^{-5}$ M for 4 min) and Bay-K-8644 (10$^{-5}$ M for 4 min). Also, in the presence of $\beta$,${\gamma}$-methylene adenosine-5'-triphosphate (MATP), which is also known to be a selective $P_{2x}$-purinergic receptor agonist, showed a similar inhibition elf CA release evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid. However, in adrenal glands preloaded with 20$\mu$M NECA for 20 min under the presence of 20$\mu$M 3-isobutyl-1-methyl-xanthine (IBMX), an adenosine receptors antagonist, CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were much recovered in comparison to the case of NECA-treatment only. Taken together, these results indicate that NECA causes the marked inhibition of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization. This inhibitory effect may be mediated by inhibiting influx of extracellular calcium and release in intracellular calcium in the rat adrenomedullary chromaffin cells through the adenosine receptor stimulation. Therefore, it is suggested that the inhibitory mechanism of adenosine receptor stimulation may play a modulatory role in regulating CA secretion.n.n.

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Characteristics of Cu(II) Extraction by β-ketohexanal (β-ketohexanal에 의한 Cu(II)의 추출 특성)

  • Shin, Jeong-Ho;Lee, Sang-Hoon;Jeong, Kap-Seop;Park, Kyung-Kee;Jun, Sang-Woo
    • Applied Chemistry for Engineering
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    • v.7 no.6
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    • pp.1053-1060
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    • 1996
  • $\beta$-ketohexanal as a chelating extractant was synthesized from the reaction of ethyl formate and methyl propyl ketone in the presence of sodium amide, and the equilibrium characteristics in the extraction of copper by $\beta$-ketohexanal-chloroform were investigated. The equilibrium constants such as the dissociation constant and the partition coefficients of $\beta$-ketohexanal, the stability constant and the partition coefficient of copper chelating complex, and the overall equilibrium constant in the extraction of copper were determined by spectrophotometric measurements, and the mechanism of extraction was proposed. The percent of extracted copper by $\beta$-ketohexanal-chloroform was near 100%, and the selective extraction of copper from Cu-Zn-Cd mixture was possible. Copper was found to be extracted as $CuR_2$ and the equilibrium reaction was expressed as $Cu^{2+}+2{\overline{HR}}{\rightleftarrows}{\overline{CuR{_2}}}+2H^+$.

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ANTICANCER EFFECT OF TAMOXIFEN IN ORAL CANCER CELL (구강암세포주에서의 Tamoxifen의 항암효과)

  • Jung, Jae-Hwa;Yun, Pil-Young;Myoung, Hoon;Shin, Jae-Il;Lee, Jong-Ho;Kim, Myung-Jin
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.29 no.6
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    • pp.365-373
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    • 2003
  • Tamoxifen is an selective estrogen receptor antagonist widely used in the management of patients with breast cancer for more than 30 years. It was thought to act primarily through occupying the estrogen receptor sites in ER positive breast cancer cells and directly on cancer cell proper. These inhibitory effects, which have been shown to be independent of the ER, highlight new mechanism of therapeutic action of tamoxifen. The purposes of this study were to identify ER in oral carcinoma cell lines and to evaluate ER independent cytotoxic effect of tamoxifen. KB(SCC), HSC-3(SCC) and A253(ACC) cell line were used and capacity of cell proliferation, apoptosis, in vitro invasion and gelatin zymography were tested. ER expression of each cell line were detected by RT-PCR and immunocytochemistry. Dose dependent inhibition of cell proliferation and inhibition of gelatinolytic activity were observed in all oral carcinoma cell lines and significant difference of apoptotic index were observed in A253 and KB. Tamoxifen inhibited in vitro invasion in all experimental groups. ER expression was detected in KB and A253. These data suggest that tamoxifen may play a role in management of oral carcinoma by independent cytotoxic effect and more advanced research must processed confirming ER-dependent cytotoxicity.

3D Architectures of LaVO4:Eu3+ Microcrystals via an EG-assisted Hydrothermal Method: Phase Selective Synthesis, Growth Mechanism and Luminescent Properties

  • Ding, Yi;Zhang, Bo;Ren, Qifang;Zhang, Qicai;Zha, Weiwei;Li, Xin;Chen, Shaohua;Oh, Won-Chun
    • Journal of the Korean Ceramic Society
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    • v.54 no.2
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    • pp.96-101
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    • 2017
  • In this article, pure $m-LaVO_4:Eu^{3+}$ and $t-LaVO_4:Eu^{3+}$ nanocrystals were prepared by an EG-assisted hydrothermal method with regular shapes. A series of controlled experiments showed that the pH value of a mixed solution, the volume ratio of $EG/H_2O$ and the dosage of the doped $Eu^{3+}$ all had an important effect on the sizes and shapes of the final products. Furthermore, the constitutional unit of the products changed from 0D to 2D with an increase in the EG dosage. The PL results showed that $t-LaVO_4$ doped with $Eu^{3+}$ ions had better luminescence properties than $m-LaVO_4$ due to its special structure. All of these results not only expand our understanding of the luminescence properties of lanthanide orthovanadates, but they also elucidate the principles of the crystal growth.

Protective Effect of Korean Red Ginseng against 6-Hydroxydopamine-induced Nitrosative Cell Death via Fortifying Cellular Defense System (6-Hydroxydopamine으로 유도된 질소적 세포 사멸에 대한 고려홍삼 추출물의 보호효과)

  • Lee, Chan;Jang, Jung-Hee;Park, Gyu Hwan
    • YAKHAK HOEJI
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    • v.60 no.2
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    • pp.92-99
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    • 2016
  • Parkinson's disease (PD) is one of the representative neurodegenerative movement disorders with the selective loss of dopaminergic neurons in the substantia nigra. 6-Hydroxydopamine (6-OHDA) is widely used as an experimental model system to mimic PD and has been reported to cause neuronal cell death via oxidative and/or nitrosative stress. Therefore, daily intake of dietary or medicinal plants which fortifies cellular antioxidant capacity can exert neuroprotective effects in PD. In the present study, we have investigated the protective effect of Korean red ginseng (KRG) against 6-OHDA-induced nitrosative death in C6 glioma cells. Treatment of C6 cells with 6-OHDA decreased cell viability and increased expression of inducible nitric oxide synthase, production of nitric oxide as well as peroxynitrite, and formation of nitrotyrosine. 6-OHDA led to apoptotic cell death as determined by decreased Bcl-2/Bax, phosphorylation of JNK, activation of caspase-3, and cleavage of PARP. Conversely, pretreatment of C6 cells with KRG attenuated 6-ODHA-induced cytotoxicity, apoptosis, and nitrosative damages. To further elucidate the molecular mechanism of KRG protection against 6-OHDA-induced nitrosative cell death, we have focused on the cellular self-defense molecules against exogenous noxious stimuli. KRG treatment up-regulated heme oxygenase-1 (HO-1), a key antioxidant enzyme essential for cellular defense against oxidative and/or nitrosative stress via activation of Nrf2. Taken together, these findings suggest KRG may have preventive and/or therapeutic potentials for the management of PD.

Separation and Recovery of Rare Earths by Ion Exchange Chromatography (이온교환 크로마토그래피에 의한 희토류 원소의 분리와 회수)

  • Cha, Ki Won;Park, Kwang Won;Hong, Sung Wook
    • Journal of the Korean Chemical Society
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    • v.41 no.11
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    • pp.612-638
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    • 1997
  • The methods of separation and recovery of rare earth elements in monazite sand have been studied by the ion exchange chromatography. Both of cation and anion exchange resin were used as ion exchange resins and the solutions of EDTA, DTPA, IMDA and Ln-EDTA were used as eluents. The H+, Zn2+, Fe3+, Al3+, Cu2+, and NH4+ forms of cation exchange resin were used as retaining ions. Ln-EDTA solution was loaded on the EDTA form of anion exchange resin and separated. The Ln-EDTA solution was also used as an eluent for a selective separation of one element from the rare earth mixture solution. The size effects of resin column, the elution mechanism for the various elution types and the separation of a large amount of rare earths were studied.

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Selective Mechanism of Cyhalofop-butyl ester between Rice and Echinochloa crus-galli - 2. Anatomical influence of Cyhalofop-butyl ester on rice and Echinochla crus-galli (제초제(除草劑) Cyhalofop-butyl ester의 벼와 피간(間) 선택성기작(選擇性機作) - 2. 제초제(除草劑) cyhalofop-butyl ester의 벼와 피간(間)에 미친 해부학적(解剖學的) 영향(影響))

  • Park, J.E.;Ryu, G.H.;Lee, I.Y.;Lee, H.K.;Shin, H.S.;Lee, J.O.;Kim, K.U.
    • Korean Journal of Weed Science
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    • v.14 no.3
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    • pp.223-227
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    • 1994
  • Basis for differential response of rice and E. crus-galli to cyhalofop-butyl ester (R-butyl 2-(4-(4-cyano-2-fluoro-phenoxy)phenoxy)propionate) was anatomically compared. Cell division in the growing point of E. crus-galli was severely inhibited by the herbicide, leading to malformation and irregular arrangement of cells. The inhibitory symptom of rice by cyhalofop-butyl ester appeared to be very similiar to that of E. crus-galli although its injury was negligible in rice when applied at the rate of 180ppm.

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