신규 합성 KATP 통로 개방제인 SKP-450과 대사체 SKP-818의 흰쥐 적출 심장 및 대동맥에 대한 작용

• 영문명: Cardiovascular Effects of Novel Potassium Channel Opener SKP-450 and SKP-818 in Isolated Rat Heart and Aorta
• 발행기관: 대한약학회
• 저자명: 정이숙(Yi Sook Jung) 문창현(Chang Hyun Moon) 유성은(Sung Eun Yoo) 신화섭(Hwa Sup Shin)
• 간행물 정보: 『약학회지』제41권 제2호 (1997년), 241~246쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1997.04.30

영문 초록

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 inotropic 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 10-6M 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 (EC50, mcM : SKP-30450, 0.107 +/- 0.009; SKP-30818, 0.476 +/- 0.022; lemakalim, 0.565 +/- 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.

키워드

Potassium channel opener SKP-450 SKP-818 lemakalim negative inotropic effect vasorelaxant effect.