• Title/Summary/Keyword: Iemakalim

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Cardiovascular Effects of Novel Potassium Channel Opener SKP-450 and SKP-818 in Isolated Rat Heart and Aorta (신규 합성 $K_{ATP}$ 통로 개방제인 SKP-450과 대사체 SKP-818의 흰쥐 적출 심장 및 대동맥에 대한 작용)

  • Jung, Yi-Sook;Moon, Chang-Hyun;Yoo, Sung-Eun;Shin, Hwa-Sup
    • YAKHAK HOEJI
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    • v.41 no.2
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    • pp.241-246
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    • 1997
  • The effect of potassium channel openers, SKP-450, SKP-818 and lemakalim have been compared in rat heart and aorta. In rat isolated heart, SKP-450 had a greater negative inotrop ic effect than lemakalim and KR-30818 against left ventricular developed pressure (LVDP) and double product of heart rate and LVDP (DP). In addition, SKP-450 had a greater effect than lemakalim and KR-30818 in increasing coronary flow, indicating a more potent vasodilating effect in coronary artery. Negative inotropic effect and coronary vasodilating effect of SKP-450 and SEP-818 were significantly reduced by 10 min-perfusion with $10^{-6}M$ glyburide, a selective blocker of ATP-sensitive potassium channel. In rat aorta, SKP-30450 and SKP-30818 as well as lemakalim induced powerful concentration-dependent relaxations against norepinephrinc-induced tone ($EC_{50},\;{\mu}M$ : SKP-30450, $0.107{\pm}0.009$; SKP-30818, $0.476{\pm}0.022$ ; lemakalim, $0.565{\pm}0.039$ ). These relaxant effects were significantly reduced by pretreatment with glyburide. In sununary, SKP-30450 and SKP-30818 showed greater negative inotropic and vasorelaxant effect than lemakalim in rat aorta with order of potency of SKP-30450 > SKP-30818 > lemakalim. These 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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