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Pharmacological Effects of KR60886, A New β3 Adrenoceptor Agonist

  • Lee, Sang-Suk;Yang, Sung-Don;Ha, Jae-Du;Choi, Joong-Kwon;Cheon, Hyae-Gyeong
    • Biomolecules & Therapeutics
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    • v.12 no.4
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    • pp.215-220
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    • 2004
  • In an attempt to develop new anti-diabetic agents, a series of aryloxypropanolamine derivatives was synthesized to serve as ${\beta}_3$ adrenoceptor agonists. Among these derivatives, 1-{1-methyl-3-[4-(2-methyl-2H-1,2,3,4-tetrazol-5-yl)phenyl]propylamino}-3-phenoxy-2-propanol (KR60886) possessed a high affinity for the ${\beta}_3$ adrenoceptor (Ki = 28 nM) and moderate affinities for ${\beta}_1$ and ${\beta}_2$ adrenoceptors (Ki = 95 nM and 100 nM, respectively). In addition, KR60886 stimulated cAMP production with an EC$_{50}$ of 0.4 ${\mu}M$, confirming its agonistic activity for the ${\beta}_3$ adrenoceptor. In vivo activities of KR60886 were examined by using a fat-fed/streptozotocin (STZ)-treated rat model and the ob/ob mouse model. Oral administration of KR60886 (10 mg/kg) for 3 days (b.i.d.) to fat-fed/STZ-treated rats significantly lowered plasma glucose levels and reduced plasma free fatty acid concentrations. Similarly, KR60886 treatment (10 mg/kg/day for 7 d) resulted in a reduction of plasma glucose concentrations in ob/ob mice. The present study suggests that KR60886 is a potent ${\beta}_3$ receptor agonist with in vivo anti-diabetic properties.

Occurrence and Control System of Aneilema japonica in Dry Seeded Rice (벼 건답직파답(乾畓直播畓)에서 사마귀풀 발생양상(發生樣相)과 방제체계(方劑體系))

  • Moon, B.C.;Park, S.T.;Kim, S.C.;Oh, Y.J.
    • Korean Journal of Weed Science
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    • v.16 no.2
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    • pp.108-113
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    • 1996
  • The experiment was conducted to obtain basic information on occurrence ecology system of Aneilema japonica and to establish its effective control systems in dry seeded rice at National Yeongnam Agricultural Experiment Station in 1995. Total amount of weed in dry seeded rice in the following year('95) as affected by control of barnyardgrass at 70 days after seeding(DAS) in previous year('94) was reduced 47.7% at 30 DAS and 7.8% at 60DAS and also exhibited different weed occurrence as compared with no control plot. Especially in control plot at 60 DAS, occurrence of Echinochloa crus-galli was reduced by 46.9%, But the growth of Aneilema japonica which is one of the problems in weed species was drastically increased by 231 % and Persicaria hydropiper by 11.8%, respectively. Suppressed tillering of rice plant as affected by occurring of A. japonica(300-750 plants/$m^2$) occurred from about 40 DAS and rice grain reduced 74-93% compared with hand weeding due to reduced panicle number. Soil applied Butachlor(EC) at 5 DAS, foliar applied Propanil -Butachlor(EC) at 13 DAS and Lgc 40863+Pendimethalin at 20 DAS were very effective for Aneilema japonica. As considering both weed suppression of Aneilema japonica and yield capacity, middle late foliar application of Lgc 40863+Pendimethalin and systematic application of Butachlor at 5 DAS followed by Propanil/Molinate at 25 DAS were the most effective control systems.

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Characteristics of Manure and Estimation of Nutrient and Pollutant of Holstein Dairy Cattle (홀스타인 젖소 분뇨의 특성과 비료성분 및 오염물질 부하량 추정)

  • Choi, D.Y.;Choi, H.L.;Kwag, J.H.;Kim, J.H.;Choi, H.C.;Kwon, D.J.;Kang, H.S.;Yang, C.B.;Ahn, H.K.
    • Journal of Animal Science and Technology
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    • v.49 no.1
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    • pp.137-146
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    • 2007
  • This study was conducted to determine fertilizer nutrient and pollutant production of Holstein dairy cattle by estimating manure characteristics. The moisture content of feces was 83.9% and 95.1% for urine. The pH of feces and urine were in the ranges of 7.0~7.4 and 7.5~7.8, respectively. The average BOD5, COD, SS, T-N, T-P concentrations of the dairy feces were 18,294, 52,765, 102,889, 2,575, and 457mg/ℓ, respectively. Dairy urine showed lower levels of BOD5(5,455mg/ℓ), COD(8,089mg/ℓ), SS(593mg/ℓ), T-N(3,401mg/l), and T-P(13mg/ℓ) than feces. The total daily produced pollutant amounts of a dairy cow were 924.1g(Milking cow), 538.8g(Dry cow), 284.4g(Heifer) of BOD5, 2,336.5g (Milking cow), 1,651.8g(Dry cow), 734.1g(Heifer) of COD and 4,210.1g(Milking cow), 2,417.1g(Dry cow), 1,629.1g(Heifer) of SS and 194.8g(Milking cow), 96.4g(Dry cow), 58.3g(Heifer) of T-N and 24.0g(Milking cow), 10.2g(Dry cow), 6.1g(Heifer) of T-P. The calculated amount of pollutants produced by a 450kg dairy cow for one year were 181.3kg of BOD5, 492.5kg of COD, 899.9kg of SS, 36.0kg of T-N and 4.1kg of T-P. The total yearly estimated pollutant production from all head(497,261) of dairy cattle in Korea is 90,149 tons of BOD5, 244,890 tons of COD, 447,491 tons of SS, 17,898 tons of T-N and 2,008 tons of T-P. The fertilizer nutrient concentrations of dairy feces was 0.26% N, 0.1% P2O5 and 0.14% K2O. Urine was found to contain 0.34% N, 0.003% of P2O5 and 0.31% K2O. The total daily fertilizer nutrients produced by dairy cattle were 197.4g (Milking cow), 97.4g(Dry cow), and 57.9g(Heifer) of Nitrogen, 54.2g(Milking cow), 22.2g(Dry cow), and 14.2g(Heifer) of P2O5 and 110.8g(Milking cow), 80.4g (Dry cow), and 39.5g(Heifer) of K2O. The total yearly estimated fertilizer nutrient produced by a 450kg dairy animal is 36.2kg of N, 8.8kg of P2O5, 24.6kg of K2O. The estimated yearly fertilizer nutrient production from all dairy cattle in Korea is 18,000 tons of N, 4,397 tons of P2O5, 12,206 tons of K2O. Dairy manure contains useful trace minerals for crops, such as CaO and MgO, which are contained in similar levels to commercial compost being sold in the domestic market. Concentrations of harmful trace minerals, such as As, Cd, Hg, Pb, Cr, Cu, Ni, Zn, met the Korea compost standard regulations, with some of these minerals being in undetected amounts.