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-g...

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Published in:The Korean journal of physiology & pharmacology 2012, 16(5), , pp.327-332
Main Authors: Lee, Hyang-Ae, Kim, Ki-Suk, Hyun, Sung-Ae, Park, Sung-Gurl, Kim, Sung Joon
Format: Article
Language:English
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약리학
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Summary: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.
ISSN:1226-4512
2093-3827
DOI:10.4196/kjpp.2012.16.5.327