• Title/Summary/Keyword: Kr

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KR-25018: A Novel, Orally Active Analgesic with Non-Narcotic Properties

  • Lee, Buyean;Kim, Jae-Hong;Park, No-Sang;Kong, Jae-Yang
    • Archives of Pharmacal Research
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    • v.17 no.5
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    • pp.304-308
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    • 1994
  • Among the new series of phenylacetamides, one of capsaicin derivatives, KR-25018 was found to have a very potent analgesic activity. Thus, the phamacological properties of KR-25018 were compared with those of morphine, capsaicin, and nonsteroidal antiinflammatory drugs (NSAIDs). The analgesic activities were evaluated in several animal models, using different stimuli, such as phenylbenzoquinone(PBQ)-induced weithing test, tail-filck test in mice and adjuvant arthritic flexion test in rat. The relationship of phamacological properties of KR-25018 to that of centrally acting opioids was assessed by the blocking test using naloxone. The analgesic potency of the KR-25018 $(MPED_{50}=0.89{\;}p.o.{\;}in{\;}PBQ-induced{\;}weithing{\;}test, {\;}MPED_{50}$=0.61$ s.c. in tail-flick test in mice0, with different action mechanism from morphine and NSAIDs, was comparable to that of morphine.

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$Co_{2}$ Fixation by Chlorella KR-1 Using Flue Gas and its Utilization as a Feedstuff for Chicks

  • Lee, Jin-Suk;Kim, Deog-Keun;Lee, Joon-Pyo;Park, Soon-Chul;Koh, Jong-Ho;Ohh, Sang-Jip
    • Journal of Microbiology and Biotechnology
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    • v.11 no.5
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    • pp.772-775
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    • 2001
  • A highly $CO_2$ tolerant microalga, Chlorella KR-1, has been isolated and used to fix $CO_2$ from actual flue gas. Growth of Chlorella KR-1 with the supply of flue gas from a liquified natural gas boiler was comparable to that obtained with 10% $CO_2$. Chlorella KR-1 produced from $CO_2$ fixation using the flue has about 50% crude protein with balanced amino acid profiles. Toxicity was not detected when the microalga was used as a feedstuff for chicks. These results indicate that the KR-1 cells could be a favorable protein source for poultry.

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The Electrophysiological Effects of Benzopyran Potassium Channel Openers on Coronary Artery Occlusion/Reperfusion-induced Arrhythmias in the Rat (흰쥐에서의 관상동맥 결찰/재관류로 유도된 부정맥에 대한 benzopyran계 $K^+$ channel opener의 전기생리학적인 효과)

  • Lee, Jae Heung;Shin, Hwa Sup;Kwon, Kwang Il
    • Korean Journal of Clinical Pharmacy
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    • v.6 no.2
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    • pp.32-40
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    • 1996
  • The electrophysiological effects of benzopyran potassium channel openers (PCOs: lemakalim, KR-30450 and KR-30818) on the ischemia/reperfusion-induced arrythmias were investigated. In anesthetized rats, subjected to 45 min occlusion of the left anterior descending coronary artery (LAD) followed by 90 min reperfusion, ventricular arrythmias were identified according to the Lambeth Conventions by lead II ECG. Rats were intravenously given vehicle ($1\%$ DMSO), lemakalim, KR-30450, and KR-30818 alone or in combination with a selective $K_{ATP}$ blocker glibenclamide, 30 min prior to coronary occlusion. Compared to vehicle, lemakalim ($30{\mu}g/kg$ i.v.), the active enantiomer of cromakalim, had a tendancy to increase the duration of ventricular tachycardia (Vl) and ventricular fibrillation (VF), the number of premature ventricular complexes (PVC) and the incidence of VF, especially in the early post-occlusion peroid ($0\~15$ min), while increasing ST-segment elevation. Both KR-30450 ($30{\mu}g/kg$, i.v.) and KR-30818 (30, $100{\mu}g/kg$, i.v.) showed similar proarrhythmic effects to lemakalim (PVC, duration of VT, and incidence of VF) with a tendancy to decrease the duration of VF and ST-segment elevation. Unlike other PCOs, however, glibenclamide (0.3, 1.0 mg/kg) had opposite effects on the induction of arrhythmias (PVC, the duration of VF); it had a tendancy to increase the duration of VT with a slight elevation of ST-segment. It seems likely that glibenclamide (0.3 mg/kg, i.v.), reduced the effects of lemakalim or KR-30450 ($30{\mu}g/kg$, i.v.) on arrhythmias (PVC, VT, VF and ST-segment). These results indicate that, in the coronary occluded rat model of ischemia, lemikuiln and KR-30450 exert a proarrhythmic activity, the effect being considered related to the opening of KATP channel.

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In Vitro Metabolism of a New Neuroprotective Agent, KR-31543 in the Human Liver Microsomes : Identification of Human Cytochrome P450

  • Ji, Hye-Young;Lee, Seung-Seok;Yoo, Sung-Eun;Kim, Hosoon;Lee, Dong-Ha;Lim, Hong;Lee, Hye-Suk
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.239-245
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    • 2004
  • KR-31543, (2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2 -methyl-2H-tetrazol-5-ylmethyl) amino]-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran, is a new neuroprotective agent for preventing ischemia-reperfusion damage. This study was performed to identify the metabolic pathway of KR-31543 in human liver microsomes and to characterize cytochrome P450 (CYP) enzymes that are involved in the metabolism of KR-31543. Human liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of two metabolites, M1 and M2. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LC/MS/MS analysis with a synthesized authentic standard, and M2 was suggested to be hydroxy-KR-31543. Correlation analysis between the known CYP enzyme activities and the rates of the formation of M 1 and M2 in the 12 human liver microsomes have showed significant correlations with testosterone 6$\beta$-hydroxylase activity (a marker of CYP3A4). Ketoconazole, a selective inhibitor of CYP3A4, and anti-CYP3A4 monoclonal antibodies potently inhibited both N-hydrolysis and hydroxylation of KR-31543 in human liver microsomes. These results provide evidence that CYP3A4 is the major isozyme responsible for the metabolism of KR-31543 to M1 and M2.

Determination of Complete Genome Sequence of Korean Isolate of Potato virus X

  • Choi, Sun-Hee;Ryu, Ki-Hyun
    • The Plant Pathology Journal
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    • v.24 no.3
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    • pp.361-364
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    • 2008
  • The complete nucleotide sequences of a Korean isolate of Potato virus X(PVX-Kr) has been determined. Full-length cDNA of PVX-Kr has been directly amplified by long template reverse transcription and polymerase chain reaction(RT-PCR) using virus specific 5'-end primer and 3'-end primer, and then constructed in a plasmid vector. Consecutive subclones of a full-length cDNA clone were constructed to identify whole genome sequence of the virus. Total nucleotide sequences of genome of PVX-Kr were 6,435 excluding one adenine at poly A tail, and genome organization was identical with that of typical PVX species. Comparison of whole genome sequence of PVX-Kr with those of European and South American isolates showed 95.4-96.8% and 77.4-77.9%, in nucleotide similarity, respectively. Sequenced PVX-Kr in this study and twelve isolates already reported could be divided into two subgroups in phylogeny based on their complete nucleotide sequences. Phylogenetic tree analysis demonstrated that PVX-Kr was clustered with European and Asian isolates(Taiwan, os, bs, Kr, S, X3, UK3, ROTH1, Tula) in the same subgroup and South American isolates(CP, CP2, CP4, HB) were clustered in the other subgroup.

Effects of a New Neuroprotective Agent KR-31378 on Liver Cytochrome P450s in Male Sprague Dawley Rats

  • Jeong, Tae-Cheon;Kim, Ji-Young;Ji, Hye-Young;Lee, Dong-Ha;Kim, Sun-Ok;Lim, Hong;Yoo, Sung-Eun;Lee, Hye-Suk
    • Archives of Pharmacal Research
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    • v.26 no.10
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    • pp.800-804
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    • 2003
  • The effects of KR-31378, a neuroprotective agent for ischemia-reperfusion damage, on liver microsomal cytochrome P450s (CYPs) were investigated in male Sprague Dawley rats. When rats were treated orally with KR-31378 for 7 consecutive days, CYP3A-selective erythromycin N-demethylase (ERDM) activity was significantly induced in a dose-dependent manner. In Western immunoblotting, CYP 3A proteins were clearly induced by treatment with KR-31378. Within 24 h after treatment with 80 mg/kg of KR-31378, ERDM activity was induced in liver microsomes in accompanied by induction of the level of CYP 3A proteins. The present results suggest that KR-31378 might modulate the expression of CYP 3A enzymes in humans.

The Analysis of Electron Transport Coefficients in Kr and Xe Atom Gas (Kr과 Xe 원자기체의 전자수송계수의 해석)

  • Jeon, Byung-Hoon
    • Journal of the Korean Institute of Illuminating and Electrical Installation Engineers
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    • v.22 no.8
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    • pp.104-108
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    • 2008
  • Accurate sets of electron collision cross sections and the electron transport coefficients for atoms and molecules are necessary for quantitative understanding of plasma phenomena Kr and Xe atom are used in many industrial applications, such as in PDP and fluorescent induction lamps(FILs). Therefore, we analysed and calculated the electron transport coefficients, the electron drift velocity W, the longitudinal and transverse diffusion coefficient $ND_L$ and $ND_T$, and the ionization coefficient $\alpha$/N in pure Kr and Xe gases over the wide E/N range from 0.001 to 500[Td] at 1[Torr] by two-tenn approximation of the Boltzmann equation.

Pharmacological Characterization of KR-31125, a Novel Nonpeptide AT1 Receptor Antagonist (안지오텐신 수용체 길항제 KR-31125의 특성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.6
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    • pp.831-837
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    • 2010
  • KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) is a potent inhibitor of angiotensin II type 1 ($AT_1$) receptors in human recombinant $AT_1$ receptors and rabbit aorta. These in vitro studies revealed that KR-31125 inhibited specific [$^{125}I$] [$Sar^1$, $Ile^8$]-angiotensin II binding to human recombinant $AT_1$ receptors in a concentration dependent manner with an $IC_{50}$ value of $19.72{\pm}2.65$ nM. However, no interaction with $AT_2$ receptors was detected as displayed by the competition binding of [$^{125}I$] CGP 42112A to human recombinant $AT_2$ receptor. The binding action was also confirmed as a competitive mode that was identical to the previously studied compound, losartan. In addition, KR-31125 caused a nonparallel shift to the right in the concentration response curves to angiotensin II with a 30-80% decrease in the maximum contractile responses ($pK_B$: 7.63). Compared to the previous studies with losartan that showed a parallel right shift in the maximum contractile responses to AII ($pA_2$: 7.59), KR-31125 presented a different mode of action with a similar potency to losartan. These results demonstrate that KR-31125 is a highly potent and $AT_1$ selective angiotensin II receptor antagonist that can be applied to the fields of new diagnostic and research tools with upcoming in vivo study results.

In Vitro Metabolism of a New Cardioprotective Agent, KR-33028 in the Human Liver Microsomes and Cryopreserved Human Hepatocytes

  • Kim Hyojin;Yoon Yune-Jung;Kim Hyunmi;Cha Eun-Young;Lee Hye Suk;Kim Jeong-Han;Yi Kyu Yang;Lee Sunkyung;Cheon Hyae Gyeong;Yoo Sung-Eun;Lee Sang-Seop;Shin Jae-Gook;Liu Kwang-Hyeon
    • Archives of Pharmacal Research
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    • v.28 no.11
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    • pp.1287-1292
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    • 2005
  • KR-33028 (N-[4-cyano-benzo[b]thiophene-2-carbonyl]guanidine) is a new cardioprotective agent for preventing ischemia-reperfusion injury. This study was performed to identify the metabolic pathway of KR-33028 in human liver microsomes and to compare its metabolism with that of cryopreserved human hepatocytes. Human liver microsomal incubation of KR-33028 in the presence of NADPH and UDPGA resulted in the formation of four metabolites, M1, M2, M3, and M4. M1 and M2 were identified as 5-hydroxy-KR-33028 and 7-hydroxy-KR-33028, respectively, on the basis of LC/MS/MS analysis with the synthesized authentic standard. M3 and M4 were suggested to be dihydroxy-KR-33028 and hydroxy-KR-33028-glucuronide, respectively. Metabolism of KR-33028 in cryopreserved human hepatocytes resulted in the formation of M1, M2, and M4. These data show a good correlation between major metabolites formed in human liver microsomes and cryopreserved human hepatocytes. In addition, KR­33028 was found to inhibit moderately the metabolism of CYP1A2 substrates. Based on the results obtained metabolic pathway of KR-33028 is proposed.

AC Breakdown Characteristics of $Ar/N_2 and Kr/N_2$Gas Mixtures ($Ar/N_2 및 Kr/N_2$혼합가스의 교류절연파괴 특성)

  • Lee, Sang-Woo;Kim, In-Sik;Lee, Dong-In;Lee, Kwang-Sik;Kim, Lee-Kook
    • The Transactions of the Korean Institute of Electrical Engineers C
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    • v.50 no.12
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    • pp.599-606
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    • 2001
  • In this paper, the ac breakdown characteristics of pure Ar, Kr and $N_2$ gas with gas pressure range of 58.8-137.3[kPa] under uniform and non-uniform fields were investigated, and the measured values were compared with those In Ar/$N_2$ and Kr/$N_2$ gas mixtures with pressure varying. Summarizing the experimental results, the breakdown voltages of Pure $N_2$gas, under uniform and non-uniform fields, were increased about 4.8 and 1.1 times than those of pure Ar gas, and about 4.4 and 1.2 times than those of pure Kr gas, and the ac breakdown voltage increased with the pressure increasing. The breakdown voltages of Ar/$N_2$ gas mixtures were decreased with decreasing the mixture ratio of Pure $N_2$ gas. In case of Ar(85%)/$N_2$ (15%) and Ar(70%)/$N_2$ (30%) gas mixtures comparing to the pure Ar gas, the breakdown voltages under uniform field were increased about 1.8 and 2.2 times, and under non-uniform field were increased about 1.1 and 1.3 times at the pressure of 101.3[kPa]. Also, in case of Kr(85%)/$N_2$ (15%) and Kr(70%)/$N_2$ (30%) gas mixtures comparing to the pure Kr gas, the breakdown voltages under uniform field were increased about 1.7 and 2.0 times, and under non-uniform field were increased about 1.0 and 1.2 times. Corona inception voltage of Kr(70%)/$N_2$(30%) gas mixtures under non-uniform fields were increased about 1.28 times than those of Ar(70%)/$N_2$ (30%) gas mixtures. In case of practical incandescent lamps, luminous and lifetime of Kr(70%)/$N_2$ (30%) gas mixtures were increased about 1.15 and 1.21 times than those of Ar(70%)/$N_2$ (30%) gas mixtures.

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