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KR-31762, a novel KATP channel opener, exerts cardioprotective effects by opening SarcKATP channels in rat models of ischemia/reperfusion-induced heart injury.
Arch Pharm Res. 2008 Apr; 31(4):482-9.AP

Abstract

The cardioprotective effects of KR-31762, a newly synthesized K+(ATP) opener, were evaluated in rat models of ischemia/reperfusion (I/R) heart injury. In isolated rat hearts subjected to 30-min global ischemia followed by 30-min reperfusion, KR-31762 (3 and 10 microM) significantly increased the left ventricular developed pressure (LVDP) and double product (heart rate x LVDP) after 30-min reperfusion in a concentration-dependent manner, while decreasing the left ventricular end-diastolic pressure (LVEDP). KR-31762 also significantly increased the time to contracture (TTC) during ischemic period (20.0, 22.4 and 26.4 min for control, 3 and 10 microM, respectively), while decreasing the release of lactate dehydrogenase (LDH) from the heart during 30 min reperfusion (30.4, 14.3 and 19.7 U/g heart weight, respectively). All these parameters except LDH release were reversed by glyburide (1 microM), a nonselective blocker of K+(ATP) channel, but not by 5-hydroxydecanoate, a selective blocker of mitoK+(ATP) channel. In anesthetized rats subjected to 45-min occlusion of left anterior descending coronary artery followed by 90-min reperfusion, KR-31762 significantly decreased the infarct size (60.8, 40.5 and 37.8% for control, 0.3 and 1.0 mg/kg, iv, respectively). KR-31762 slightly relaxed the isolated rat aorta precontracted with methoxamine (IC(50): 23.5 microM). These results suggest that KR-31762 exerts potent cardioprotective effects through the opening of sarcolemmal K(ATP) channel in rat hearts with the minimal vasorelaxant effects.

Authors+Show Affiliations

Department of Applied Biochemistry, Division of Life Science, College of Biomedical and Health Science, Konkuk University, 322 Danwol-Dong, Chungju, Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

18449506

Citation

Lee, Sung-Hun, et al. "KR-31762, a Novel KATP Channel Opener, Exerts Cardioprotective Effects By Opening SarcKATP Channels in Rat Models of Ischemia/reperfusion-induced Heart Injury." Archives of Pharmacal Research, vol. 31, no. 4, 2008, pp. 482-9.
Lee SH, Yang MK, Lim JH, et al. KR-31762, a novel KATP channel opener, exerts cardioprotective effects by opening SarcKATP channels in rat models of ischemia/reperfusion-induced heart injury. Arch Pharm Res. 2008;31(4):482-9.
Lee, S. H., Yang, M. K., Lim, J. H., Seo, H. W., Yi, K. Y., Yoo, S. E., Lee, B. H., Won, H. S., Lee, C. S., Choi, W. S., & Shin, H. S. (2008). KR-31762, a novel KATP channel opener, exerts cardioprotective effects by opening SarcKATP channels in rat models of ischemia/reperfusion-induced heart injury. Archives of Pharmacal Research, 31(4), 482-9. https://doi.org/10.1007/s12272-001-1182-9
Lee SH, et al. KR-31762, a Novel KATP Channel Opener, Exerts Cardioprotective Effects By Opening SarcKATP Channels in Rat Models of Ischemia/reperfusion-induced Heart Injury. Arch Pharm Res. 2008;31(4):482-9. PubMed PMID: 18449506.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - KR-31762, a novel KATP channel opener, exerts cardioprotective effects by opening SarcKATP channels in rat models of ischemia/reperfusion-induced heart injury. AU - Lee,Sung-Hun, AU - Yang,Min-Kyu, AU - Lim,Jong-Hyun, AU - Seo,Ho-Won, AU - Yi,Kyu-Yang, AU - Yoo,Sung-Eun, AU - Lee,Byung-Ho, AU - Won,Hyung-Sik, AU - Lee,Chang-Soo, AU - Choi,Wahn-Soo, AU - Shin,Hwa-Sup, Y1 - 2008/05/01/ PY - 2007/11/22/received PY - 2008/5/2/pubmed PY - 2008/6/12/medline PY - 2008/5/2/entrez SP - 482 EP - 9 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 31 IS - 4 N2 - The cardioprotective effects of KR-31762, a newly synthesized K+(ATP) opener, were evaluated in rat models of ischemia/reperfusion (I/R) heart injury. In isolated rat hearts subjected to 30-min global ischemia followed by 30-min reperfusion, KR-31762 (3 and 10 microM) significantly increased the left ventricular developed pressure (LVDP) and double product (heart rate x LVDP) after 30-min reperfusion in a concentration-dependent manner, while decreasing the left ventricular end-diastolic pressure (LVEDP). KR-31762 also significantly increased the time to contracture (TTC) during ischemic period (20.0, 22.4 and 26.4 min for control, 3 and 10 microM, respectively), while decreasing the release of lactate dehydrogenase (LDH) from the heart during 30 min reperfusion (30.4, 14.3 and 19.7 U/g heart weight, respectively). All these parameters except LDH release were reversed by glyburide (1 microM), a nonselective blocker of K+(ATP) channel, but not by 5-hydroxydecanoate, a selective blocker of mitoK+(ATP) channel. In anesthetized rats subjected to 45-min occlusion of left anterior descending coronary artery followed by 90-min reperfusion, KR-31762 significantly decreased the infarct size (60.8, 40.5 and 37.8% for control, 0.3 and 1.0 mg/kg, iv, respectively). KR-31762 slightly relaxed the isolated rat aorta precontracted with methoxamine (IC(50): 23.5 microM). These results suggest that KR-31762 exerts potent cardioprotective effects through the opening of sarcolemmal K(ATP) channel in rat hearts with the minimal vasorelaxant effects. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/18449506/KR_31762_a_novel_KATP_channel_opener_exerts_cardioprotective_effects_by_opening_SarcKATP_channels_in_rat_models_of_ischemia/reperfusion_induced_heart_injury_ L2 - https://dx.doi.org/10.1007/s12272-001-1182-9 DB - PRIME DP - Unbound Medicine ER -