Wide Spectrum of Inhibitory Effects of Sertraline on Cardiac Ion Channels

Wide Spectrum of Inhibitory Effects of Sertraline on Cardiac Ion Channels

Sertraline is a commonly used antidepressant of the selective serotonin reuptake inhibitors (SSRIs) class. In these experiments, we have used the whole cell patch clamp technique to examine the effects of sertraline on the major cardiac ion channels expressed in HEK293 cells and the native voltage-gated Ca^2＋ channels in rat ventricular myocytes. According to the results, sertraline is a potent blocker of cardiac K^＋ channels, such as hERG, I_Ks and I_K1. The rank order of inhibitory potency was hERG ＞I_K1＞I_Ks with IC₅₀ values of 0.7, 10.5, and 15.2 ՌM, respectively. In addition to K^＋ channels, sertraline also inhibited I_Na and I_Ca, and the IC₅₀ values are 6.1 and 2.6 ՌM, respectively. Modification of these ion channels by sertraline could induce changes of the cardiac action potential duration and QT interval, and might result in cardiac arrhythmia.