Department of Pharmacy Practice, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 46202, USA.
J Cardiovasc Pharmacol. 2009 Sep;54(3):253-62. doi: 10.1097/FJC.0b013e3181b2b706.
The contribution of the slow component of the delayed rectifier current (IKs) to ventricular repolarization is increased during rapid heart rates and prolonged repolarization. The objective was to characterize physiologically relevant paroxysmal beta-adrenergic receptor-mediated alterations on ventricular repolarization under these conditions. Paced guinea pig hearts were perfused with (1) control, (2) sparfloxacin (IKr inhibitor), or (3) sparfloxacin and HMR 1556 (IKs inhibitor). The mean +/- standard error of the mean epicardial action potential duration at 90% repolarization (APD90) increased from baseline with IKr inhibition (12.9% +/- 4.7%) and dual IKr/IKs inhibition (25.1% +/- 5.3). Paroxysmal isoproterenol (0.01 and 1.0 nM) significantly decreased APD90 in the presence of IKr inhibition but was attenuated with the addition of IKs inhibition. Spontaneous episodes of polymorphic ventricular tachycardia were observed with isoproterenol during dual IKr and IKs inhibition. The endocardial expression of KCNQ1 increased greater than 2-fold after exposure to IKr and dual IKr/IKs inhibition relative to control but was not altered in epicardial tissue. The beta-adrenergic receptor-mediated decrease in APD90 during IKr inhibition is reversed in the presence of IKs inhibition at rapid heart rates. IKs may serve as an important compensatory mechanism to protect against adrenergically induced arrhythmias when the repolarization reserve is depleted.
在快速心率和延长复极期间,延迟整流钾电流(IKs)的缓慢成分对心室复极的贡献增加。目的是在这些条件下描述生理相关的阵发性β-肾上腺素能受体介导的心室复极改变。用(1)对照、(2)司帕沙星(IKr 抑制剂)或(3)司帕沙星和 HMR 1556(IKs 抑制剂)灌流豚鼠心脏。心外膜动作电位复极 90%时的平均 +/- 标准误差(APD90)与 IKr 抑制(12.9% +/- 4.7%)和双重 IKr/IKs 抑制(25.1% +/- 5.3%)时从基线增加。阵发性异丙肾上腺素(0.01 和 1.0 nM)在 IKr 抑制存在时显著缩短 APD90,但加入 IKs 抑制后减弱。在双重 IKr 和 IKs 抑制期间,异丙肾上腺素观察到自发多形性室性心动过速。与对照相比,暴露于 IKr 和双重 IKr/IKs 抑制后,心内膜 KCNQ1 的表达增加了 2 倍以上,但在心外膜组织中没有改变。在快速心率时,当复极储备耗尽时,IKs 抑制存在时,IKr 抑制导致的 APD90 降低的 β-肾上腺素能受体介导的作用被逆转。当复极储备耗尽时,IKs 可能作为一种重要的代偿机制,防止肾上腺素能诱导的心律失常。