• Title/Summary/Keyword: single hill

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Relative potency of antihistaminics for $H_1$-and muscarinic receptors (항 히스타민제의 $H_1$ 수용체와 무스카린 수용체에 대한 상대적 역가)

  • 이신웅;박영주;이정수
    • YAKHAK HOEJI
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    • v.37 no.4
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    • pp.397-407
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    • 1993
  • The muscarinic antagonist l-[benzilic-4,4'-$^3H$]quinuclidinyl benzilate([$^3H$]QNB) bound to a single class of muscarinic receptor with high affinity in guinea pig ileal membranes. The $K_{D}$ and B$_{max}$ values for [$^3H$]QNB calculated from analysis of saturation isotherms were 54 pM and 156fmol/mg, respectively. H$_{1}$-blockers inhibited [$^3H$]QNB binding to ileal membranes with $K_{i}$ values ranged from 0.008 $\mu{M}$ to 1.6 $\mu{M}$. The pseudo-Hill coefficients of H$_{1}$-blockers for inhibition of [$^3H$]QNB binding to the ileal membranes were close to unit. The $K_{i}$ values for H$_{1}$-blockers were similar to the $K_{M}$ values calculated by Schild plot of functional data obtained from inhibition of the carbachol-induced contraction in guinea-pig ileum, suggesting that binding of H$_{1}$-blockers vs [$^3H$]QNB in ileal membranes represents an interaction with a receptor of physiological relevance. The $K_{H}$ values of H$_{1}$-blockers for H$_{1}$-receptor estimated from inhibition of the histamine-induced contraction were the range of 0.15 nM to 56.5 nM. The $K_{M}$/K$_{H}$ ratio of H$_{1}$-blockers varied over a wide range of 3 to 2300. Thus, the antihistaminic potencies of H$_{1}$-blockers do not correlate with their antimuscarinic potencies, which suggest that antihistamines have different antimuscarinic potencies in therapeutic blood levels causing similar antiallergic effect. Among 13 traditional antihistaminics examined in this study, drug having the highest and the lowest $K_{M}$/K$_{H}$ ratio is triprolidine and diphenidol, respectively. The present results demonstrate that the antimuscarinic property of antihistamines is not necessary for their antiallergic effect, and data on the affinity of antihistamines for muscarinic and H$_{1}$-receptors can be an important parameter in the selection and evaluation of these drugs.

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Rat Liver $AT_1$ Receptor Binding Analysis for Drug Screening

  • Lee, Sunghou;Lee, Buyean;Hwasup Shin;Jaeyang Kong
    • Biomolecules & Therapeutics
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    • v.3 no.1
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    • pp.21-27
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    • 1995
  • The only compounds with antagonistic activity via AT$_1$receptor, one of two subtypes of angiotensin II (AII) receptor, have been demonstrated to block the vasoconstriction effects of AII and thereby provide therapeutic potential. This initiated the search for compounds with high specific affinity to AT$_1$receptor and their effective screening methods. The radioligand binding assay for the AII receptor is regarded as the primary method for the evaluation of AT$_1$receptor antagonists for their activity. In this paper, we characterized the liver AT$_1$receptor and describe the efficient method of the radioligand binding assay using rat liver as a source of AT$_1$receptor. Equilibrium binding studies with rat adrenal cortex, adrenal medulla, liver and bovine adrenal showed that the specific bindings of [$^3$H] AII were saturable in all tissues and the Scatchard plots of those data were linear, suggesting a single population of binding sites. Hill slopes were very near to the unity in all tissues. Kinetic studies of [$^3$H) AII binding in rat liver homogenates yielded two association rate constants, 4.10$\times$10$^{7}$ M$^{-1}$ min$^{-1}$ and 4.02$\times$10$^{9}$ M$^{-1}$ min$^{-1}$ , with a single dissociation rate constant, 7.07$\times$10$^{-3}$ min-$^{-1}$ , possibly due to the partial dissociation phenomenon. The rank order of inhibition potencies of [$^3$H] AII binding in rat liver was AII>Sarile>Losartan>PD 123177. Rat liver homogenates revealed to have very high density of homogeneous population of the AT$_1$receptor subtype, as the specifically bound [$^3$H] AII was not inhibited by PD 123177, the nonpeptide antagonist of AT$_2$. The results of this study demonstrated that the liver homogenates from rats could be the best receptor preparation for the AT$_1$receptor binding assay and provide an efficient system for the screening of newly synthesized candidate compounds of AT$_1$receptor antagonist.

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Vertical Profiles of CO2 Concentrations and CO2 Storage in Temperate Forest in Korea (한국 활엽수림의 이산화탄소 농도의 연직구조와 저류항)

  • Thakuri, Bindu Malla;Kang, Minseok;Chun, Jung Hwa;Kim, Joon
    • Proceedings of The Korean Society of Agricultural and Forest Meteorology Conference
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    • 2013.11a
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    • pp.23-24
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    • 2013
  • Micrometeorological fluxes measured over a tall forest in a complex terrain are difficult to interpret. $CO_2$ storage often makes significant contributions to net ecosystem exchange of $CO_2$ (NEE) in early morning and during nighttime due to calm and stable conditions. We measured the above-canopy $CO_2$ flux along with its concentration profiles at eight levels within and above the canopy to evaluate $CO_2$ storage term. Our question is whether or not the $CO_2$ storage term can be estimated accurately from a single level measurement of $CO_2$ concentration in a complex terrain. Our objectives are (1) to document vertical profiles of $CO_2$ concentration and (2) to compare the diurnal and seasonal variations of $CO_2$ storages estimated from single and multi-level $CO_2$ concentration data. Seasonally averaged Diurnal variations of $CO_2$ concentration ranged from 398 to 455 ppm near the forest floor at 0.1 m whereas they ranged from 364 to 395 ppm at 40 m in the atmosphere. The diurnal variation of vertical profiles of $CO_2$ concentration shows very interesting features with season. At all eight levels, diurnal variation of $CO_2$ concentration showed little change in winter. In spring, the diurnal variations of $CO_2$ concentration at 8 levels showed three distinct groups of layers with height: the first layer: 0.1m (near surface), second layer: 1.0 m and 4.0m (below canopy) and the third layer: 7.4m to 40.7 m (near canopy and above). In summer, these three groups of layers were further separated with larger variations whereas such distinction became smaller in fall. The diurnal variation of $CO_2$ concentration in the first three layers near surface always showed higher concentration with larger variability. Typically, $CO_2$ concentration showed peaks in early morning and in the evening. After the evening peak, $CO_2$ concentration gradually increased except for those near the surface (i.e., 0.1, 1.0 and 4.0 m) where the concentrations actually decreased. We suspect that this could be attributed to the drainage flow of $CO_2$ along the hill slope from the headwater to downstream, which is not taken into account for net ecosystem $CO_2$ exchange. In comparison to the results of other studies, the distinct and different vertical structures of $CO_2$ concentrations observed at our site may be due to complex terrain and weak turbulent mixing under calm conditions at the site. The annual mean of diurnal variation of $CO_2$ storage flux from single level ranged from -0.6 to $0.9{\mu}mol\;m^{-2}s^{-1}$ and from multi-level from -1.2 to $1.0{\mu}\;{\mu}mol\;m^{-2}s^{-1}$. When compared against the results from the multi-level concentrations, the storage flux estimated from a single-level concentration was generally adequate except for specific hours near sunrise and sunset. Further details and their implication will be discussed in the presentation.

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Future Development of Genetics and the Broiler (BROILER 육종기술의 전망)

  • 오봉국
    • Korean Journal of Poultry Science
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    • v.8 no.1
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    • pp.1-5
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    • 1981
  • In trying to predict the effect of genetics on the broiler in the year 2000, this is a relatively short period of time as far as broiler genetics in concerned. Modern broiler genetics started around 1945 and tremendous gains when made in past 35 years. Futher improvements on broiler will depend on the evolution and revolution: 1. Evolution: (1) Growth rate has been made 4-5% per year. (2) Feed conversion has improved approximately 1% per year. (3) Abdominal fat is becoming a major complaint in broiler. (4) Because of the changing life-style, broiler meat sales in the future will be more and more in cut-up form. (5) Breeding for stress resistance and selection for docile temperament can be important in order to funker improve fled efficiency. (6) In female parent stock, reproduction characteristics are in many can negatively correlated with the desired broiler traits. (7) Egg production and hatchability in moot commercial parent nod m at a fairly high level. (8) In male parent stock, the heavier and mon super-meat-type male lines are desired to Product better broilers. 2. Revolution: Trying to forecast revolutionary change in broiler genetics is highly speculative, as sudden change are aften unpredictable. (1) Species hybridization, such as a turkey-chicken cross (2) Biochemical tools, such as blood typing. (3) Mutation breeding by radiation or chemical mutagentia. (4) Broiler breeding would be to change the phenotypic appearance by single gene, such as naked, wingless. (5) Changes in production techniques. such as growing in cage or growing in filtered air positive pressure houses.

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The Effect of Single and Compound Fertilizerson Paddy Rice (수도에 대(對)한 단비(單肥)와 복비(複肥)의 효과)

  • Oh, Wang-Keun
    • Korean Journal of Soil Science and Fertilizer
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    • v.11 no.2
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    • pp.81-87
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    • 1979
  • In order to observe the lasting effect of NK-compound mineral fertilizer and organic compound fertilizer including Myweon organic liquid fertilizer, a pot experiment was conducted with rice (Oriza Sativa) variety: Nong Back. These fertilizers were applied as basal and the same amount of urea form of nitrogen was top dressed about a month after transplanting, July seventh, 1977. Results obtained are as follows; 1. The lasting effect of various fertilizers were laid in following decreasing order; Myweon liquid < Organic compound fertilizer (Myweon coop. made) > NK-compound fertilizer (Chosun coop. made) Single fertilizer. It was considered that organic matter served as microbial feed and lead a temporary fixation of available plant nutrients in the soil, and the reduced surface area of the compound fertilizers slowed down the availability of the fertilizers. 2. The fertilizer showing greater lasting effect produced more panicles per hill and less grains per panicle than the fertilizers showing less lasting effect, and brought low maturity, which resulted in low paddy yield the paddy producing efficiency of nitrogen absorbed by straw was also low in the former fertilizers. Such advanced effect of the former fertilizer was considered to be related with the variety of early maturity and unseasonable topdressing of fertilizer which made at the maximum tillering stage. 3. For the production of Japonica type paddy with heavy fertilization which may required to depress the early growth a little and promote the late growth, it might be necessary to develop slow releasing fertilizers such as single fertilizer formulated to a large grains or compound fertilizer containing organic matter. 4. If the nitrogen content of paddy, Nong Back, far excess 0.64 or 0.65% and reaches 0.68% or above, the yield of the variety seemed to be decreased remarkbly through the low maturity rate and thousand grain weight.

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Genetic Variability Based on Tandem Repeat Numbers in a Genomic Locus of 'Candidatus Liberibacter asiaticus' Prevalent in North East India

  • Singh, Yanglem Herojit;Sharma, Susheel Kumar;Sinha, Bireswar;Baranwal, Virendra Kumar;Singh, N. Bidyananda;Chanu, Ngathem Taibangnganbi;Roy, Subhra S.;Ansari, Meraj A.;Ningombam, Arati;Devi, Ph. Sobita;Das, Ashis Kumar;Singh, Salvinder;Singh, K. Mamocha;Prakash, Narendra
    • The Plant Pathology Journal
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    • v.35 no.6
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    • pp.644-653
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    • 2019
  • The genetic variability of 'Candidatus Liberibacter asiaticus' (CLas) population associated with huanglongbing (HLB) disease of citrus in North Eastern (NE) region of India, a geographically locked region, and home for the diversity of many citrus species was analyzed on the basis of tandem repeat numbers (TRN) in variable CLIBASIA_01645 genomic loci. Fifty-five CLas strains sampled from different groves of NE Hill (NEH) region of India were in single amplicon group, but there was remarkable genetic variability in TRNs. The TRN in HLB-associated CLas strains varied from 0-21 and two novel repeat motifs were also identified. Among the NE population of CLas, TRN5 and TRN9 were most frequent (total frequency of 36.36%) followed by TRN4 (14.55%) and TRN6, TNR7 with a frequency of 12.73% each. Class II type CLas genotypes (5 < TRN ≤ 10) had highest prevalence (frequency of 60.00%) in the samples characterized in present study. Class I (TRN ≤ 5) genotypes were second highest prevalent (29.09%) in the NEH region. Further analysis of genetic diversity parameters using Nei's measure (H value) indicated wide genetic diversity in the CLas strains of NE India (H value of 0.58-0.86). Manipur CLas strains had highest genetic variability (0.86) as compared to Eastern, Southern and Central India. The R10 values (TRN ≤ 10/TRN > 10) of NE CLas population was 10.43 (73/7), higher from other regions of India. Present study conclusively reported the occurrence of high genetic variability in TRN of CLas population in North East Indian citrus groves which have evolved to adapt to the specific ecological niche.

Interaction of Antihistaminics with Muscarinic Receptor(II) -Action on the cerebral muscarinic $M_1$ Receptor- (항 Histamine제와 Muscarinic Receptor와의 상호작용(II) -대뇌 Muscarinic $M_1$ Receptor에 대한 작용-)

  • Lee, Shin-Woong;Park, Young-Joo;Park, In-Sook;Lee, Jeung-Soo
    • YAKHAK HOEJI
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    • v.34 no.4
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    • pp.224-237
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    • 1990
  • A single uniform population of specific, saturable, high affinity binding site of $[^3H]QNB$ guinuclidinyl benzilate(QNB) was identified in the rat cerebral microsomes. The Kd value(37.2 pM) for $[^3H]QNB$ calculated from the kinetically derived rate constants was in agreement with the Kd value(48.9 pM) determined by analysis of saturation isotherms at various receptor concentrations. Dimenhydrinate(DMH), histamine $H_1-blocker$, increased Kd value for $[^3H]QNB$ QNB without affecting the binding site concentrations and this effect resulted from the ability of DMH to slow $[^3H]QNB-receptor$ association. Pirenzepine inhibition curve of $[^3H]QNB$ binding was shallow(nH = 0.52) indicating the presence of two receptor subtypes with high ($M_1-site$) and low($M_2-site$) affinity for pirenzepine. Analysis of these inhibition curves yielded that 68% of the total receptor populations were of the $M_1-subtype$ and the remaining 32% of the $M_2-subtype$. Ki values for the $M_1-$ and $M_2-subtypes$ were 2.42 nM and 629.3 nM, respectively. Ki values for $H_1-blockers$ that inhibited $[^3H]QNB$ binding varied with a wide range ($0.02-2.5\;{\mu}M$). The Pseudo-Hill coefficients for inhibition of $[^3H]QNB$ binding by most of $H_1-blockers$ examined except for oxomemazine inhibition of $[^3H]QNB$ binding were close to one. The inhibition curve for oxomemazine in competition with $[^3H]QNB$ was shallow(nH = 0.74) indicating the presence of two receptor populations with different affinities for this drug. The proportion of high and low affinity was 33:67. The Ki values for oxomemazine were $0.045{\pm}0.016\;{\mu}M$ for high affinity and $1.145{\pm}0.232\;{\mu}M$ for low affinity sites. These data indicate that muscarinic receptor blocking potency of $H_1-blockers$ varies widely between different drugs and that most of $H_1-blockers$ examined are nonselective antagonist for the muscarinic receptor subtypes, whereas oxomemazine might be capable of distinguishing between subclasses of muscarinic receptor.

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Optimal Design for Marker-assisted Gene Pyramiding in Cross Population

  • Xu, L.Y.;Zhao, F.P.;Sheng, X.H.;Ren, H.X.;Zhang, L.;Wei, C.H.;Du, L.X.
    • Asian-Australasian Journal of Animal Sciences
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    • v.25 no.6
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    • pp.772-784
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    • 2012
  • Marker-assisted gene pyramiding aims to produce individuals with superior economic traits according to the optimal breeding scheme which involves selecting a series of favorite target alleles after cross of base populations and pyramiding them into a single genotype. Inspired by the science of evolutionary computation, we used the metaphor of hill-climbing to model the dynamic behavior of gene pyramiding. In consideration of the traditional cross program of animals along with the features of animal segregating populations, four types of cross programs and two types of selection strategies for gene pyramiding are performed from a practical perspective. Two population cross for pyramiding two genes (denoted II), three population cascading cross for pyramiding three genes(denoted III), four population symmetry (denoted IIII-S) and cascading cross for pyramiding four genes (denoted IIII-C), and various schemes (denoted cross program-A-E) are designed for each cross program given different levels of initial favorite allele frequencies, base population sizes and trait heritabilities. The process of gene pyramiding breeding for various schemes are simulated and compared based on the population hamming distance, average superior genotype frequencies and average phenotypic values. By simulation, the results show that the larger base population size and the higher the initial favorite allele frequency the higher the efficiency of gene pyramiding. Parents cross order is shown to be the most important factor in a cascading cross, but has no significant influence on the symmetric cross. The results also show that genotypic selection strategy is superior to phenotypic selection in accelerating gene pyramiding. Moreover, the method and corresponding software was used to compare different cross schemes and selection strategies.

Attenuation Structure of the Mt. Fuji Region, Japan (일본 후지산의 감쇠구조)

  • Chung, Tae-Woong;Lees, Jonathan M.;Yoshimoto, Kazuo;Fujita, Eisuke;Ukawa, Motoo
    • 한국지구물리탐사학회:학술대회논문집
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    • 2008.10a
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    • pp.97-100
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    • 2008
  • Mount Fuji is the focus of intense study because of its potential hazard signaled by seismic, geologic and historical activity. Based on extensive seismic data recorded in the vicinity of Mt. Fuji, coda quality factor ($Q_c^{-1}$) using a single scattering model hypothesis, and intrinsic and scattering quality factor $(Q_i^{-1}$ and $Q_s^{-1})$ using the Multiple Lapse Time Window Analysis (MLTW) method was measured. To focus the study on the magmatic structure below Mt. Fuji, to the data were separated into two groups: a near-Fuji region of rays traversing an area with radius 5 km around the summit (R < 5 km), and a far-Fuji region of rays beyond a radius of 20 km around the summit (R > 20 km). The results of the study have a small error range due to the large data sample, showing that all $Q^{-1}$ values in near-Fuji area are greater than those of far-Fuji area, and $Q_i^{-1}$ for both the near and far-Fuji area is higher than $Q_s^{-1}$ at high frequencies. The $Q_i^{-1}$ values of the near-Fuji area are lower than those of the other volcanic areas considered, while values of $Q_s^{-1}$ are not. The low $Q_i^{-1}$ for the volcanic region of near-Fuji suggests that the magmatic activity, or percent of partial melt, at Mt. Fuji is not as active as hot spot volcanoes such as Kilauea, Hawaii.

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Memory Enhancing and Neuroprotective Effects of Selected Ginsenosides

  • Sao Hai Ying;Zhang Jing;Yeo Soo Jeong;Myung Chang Seon;Kim Hyang Mi;Kim Jong Moon;Park Jeong Hill;Cho Jung Sook;Kang Jong Seong
    • Archives of Pharmacal Research
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    • v.28 no.3
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    • pp.335-342
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    • 2005
  • The effects of ginsenosides Rg$_3$(R) , Rg$_3$(S) and Rg$_5$/Rk$_1$ (a mixture of Rg$_5$ and Rk$_1$ 1:1, w/w), which are components isolated from processed Panax ginseng C.A. Meyer (Araliaceae), on memory dysfunction were examined in mice using a passive avoidance test. The ginsenosides Rg3(R), Rg3(S) or Rg$_5$/Rk$_1$, when orally administered for 4 days, significantly ameliorated the memory impairment induced by the single oral administration of ethanol. The memory impairment induced by the intraperitoneal injection of scopolamine was also significantly recovered by ginsenosides Rg3(S) and Rg$_5$/Rk$_1$. Among the three ginsenosides tested in this study, Rg$_5$/Rk$_1$ enhanced the memory function of mice most effectively in both the ethanol­and scopolamine-induced amnesia models. Moreover, the latency period of the Rg$_5$/Rk$_1$­treated mice was 1.2 times longer than that of the control (no amnesia) group in both models, implying that Rg$_5$/Rk$_1$ may also exert beneficial effects in the normal brain. We also evaluated the effects of these ginsenosides on the excitotoxic and oxidative stress-induced neuronal cell damage in primary cultured rat cortical cells. The excitotoxicity induced by glutamate or N­methyl-D-aspartate (NMDA) was dramatically inhibited by the three ginsenosides. Rg$_3$(S) and Rg$_5$/Rk$_1$ exhibited a more potent inhibition of excitotoxicity than did Rg$_3$(R). In contrast, these ginsenosides were all ineffective against the H$_2$O$_2$- or xanthine/xanthine oxidase-induced oxidative neuronal damage. Taken together, these results indicate that ginsenosides Rg$_3$(S) and Rg$_5$/Rk$_1$ significantly reversed the memory dysfunction induced by ethanol or scopolamine, and their neuroprotective actions against excitotoxicity may be attributed to their memory enhancing effects.