Gumina R J, Beier N, Schelling P, Gross G J
Department of Pharmacology and Toxicology, Medical College of Wisconsin, Milwaukee 53226, USA.
J Cardiovasc Pharmacol. 2000 Jun;35(6):949-53. doi: 10.1097/00005344-200006000-00019.
Pharmacologic inhibition of the K(ATP) channel with sulfonylureas or the adenosine receptor with methylxanthines has been shown to attenuate ischemic preconditioning (IPC). Both classes of compounds are widely used clinically, and several reports have demonstrated adverse outcomes in patients taking sulfonylureas. Recently inhibition of the sodium/hydrogen exchanger isozyme-1 (NHE-1) has been shown to be equal to IPC at providing myocardial protection in dogs and may be an alternative to IPC in patients taking sulfonylureas or methylxanthines. However, no experiments have examined the pharmacologic overlap between IPC and NHE-1 inhibitor-mediated cardioprotection in dogs. With an in vivo canine infarct model in which the left anterior descending coronary artery was occluded for 60 min and reperfused for 3 h, neither the K(ATP) channel antagonist glibenclamide nor the adenosine-receptor antagonist PD 115199 attenuated NHE-1 inhibitor-mediated reduction in infarct size expressed as a percentage of the area at risk produced by EMD 85131 (Control, 24.2 +/- 3.6%; EMD 85131, 6.4 +/- 2.3%; PD 115199 + EMD 85131, 6.6 +/- 2.4%; glibenclamide + EMD 85131, 3.5 +/- 1.2%). NHE-1 inhibition and IPC do not overlap pharmacologically, and NHE-1 inhibition may be an alternative for cardioprotection in patients taking sulfonylureas or methylxanthines.
已表明,用磺脲类药物对K(ATP)通道进行药理抑制或用甲基黄嘌呤对腺苷受体进行药理抑制可减弱缺血预处理(IPC)。这两类化合物在临床上都被广泛使用,并且有几份报告表明服用磺脲类药物的患者会出现不良后果。最近,已表明抑制钠/氢交换体同工酶-1(NHE-1)在为犬提供心肌保护方面等同于IPC,并且对于服用磺脲类药物或甲基黄嘌呤的患者而言,NHE-1抑制可能是IPC的替代方法。然而,尚无实验研究犬中IPC与NHE-1抑制剂介导的心脏保护之间的药理重叠情况。在一个体内犬梗死模型中,左前降支冠状动脉闭塞60分钟并再灌注3小时,K(ATP)通道拮抗剂格列本脲和腺苷受体拮抗剂PD 115199均未减弱NHE-1抑制剂介导的梗死面积减小,梗死面积减小以EMD 85131产生的危险区域面积的百分比表示(对照组,24.2±3.6%;EMD 85131,6.4±2.3%;PD 115199 + EMD 85131,6.6±2.4%;格列本脲+ EMD 85131,3.5±1.2%)。NHE-1抑制和IPC在药理上不重叠,并且NHE-1抑制可能是服用磺脲类药物或甲基黄嘌呤患者心脏保护的替代方法。