title: Wide spectrum of inhibitory effects of sertraline on cardiac ion channels.
abstract: 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 IC(50) values of 0.7, 10.5, and 15.2 µM, respectively. In addition to K(+) channels, sertraline also inhibited I(Na) and I(Ca), and the IC(50) values are 6.1 and 2.6 µM, 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.
authors.affiliation: Next-Generation Pharmaceutical Research Center, Korea Institute of Toxicology, Korea Research Institute of Chemical Technology, Daejeon 305-600, Korea. ; Department of Physiology and Department of Biomedical Sciences, Seoul National University College of Medicine, Seoul 110-799, Korea.
authors.forename: Hyang-Ae
authors.initials: HA
authors.lastname: Lee
authors.forename: Ki-Suk
authors.initials: KS
authors.lastname: Kim
authors.forename: Sung-Ae
authors.initials: SA
authors.lastname: Hyun
authors.forename: Sung-Gurl
authors.initials: SG
authors.lastname: Park
authors.forename: Sung Joon
authors.initials: SJ
authors.lastname: Kim
keywords: Antidepressant; Cardiac; Ion channel; Selective serotonin reuptake inhibitor; Sertraline