Abstract
We examined the effects of the selective serotonin reuptake inhibitor (SSRI) sertraline on voltage-dependent K+ (Kv) channels in freshly isolated rabbit coronary arterial smooth muscle cells using the voltage-clamp technique. Sertraline decreased the Kv channel current in a dose-dependent manner, with an IC50 value of 0.18 μM and a slope value (Hill coefficient) of 0.61. Although the application of 1 μM sertraline did not affect the steady-state activation curves, sertraline caused a significant, negative shift in the inactivation curves. Pretreatment with another SSRI, paroxetine, had no significant effect on Kv currents and did not alter the inhibitory effects of sertraline on Kv currents. From these results, we concluded that sertraline dose-dependently inhibited Kv currents independently of serotonin reuptake inhibition by shifting inactivation curves to a more negative potential.
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Acknowledgements
This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (Ministry of Education: 2014-R1A1A4A01003840) (Ministry of Science, ICT and Future Planning: 2012-M3A9C7050184). This study was also supported by 2015 Research Grant from Kangwon National University (No. 520150339).
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Corresponding editor: Neeraj Jain
[Kim HS, Li H, Kim HW, Shin SE, Choi I-W, Firth AL, Bang H, Bae YM and Park WS 2016 Selective serotonin reuptake inhibitor sertraline inhibits voltage-dependent K+ channels in rabbit coronary arterial smooth muscle cells. J. Biosci.]
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Kim, H.S., Li, H., Kim, H.W. et al. Selective serotonin reuptake inhibitor sertraline inhibits voltage-dependent K+ channels in rabbit coronary arterial smooth muscle cells. J Biosci 41, 659–666 (2016). https://doi.org/10.1007/s12038-016-9645-6
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DOI: https://doi.org/10.1007/s12038-016-9645-6