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KMID : 0811720170210020225
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Korean Journal of Physiology & Pharmacology
2017 Volume.21 No. 2 p.225 ~ p.232
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Nortriptyline, a tricyclic antidepressant, inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells
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Shin Sung-Eun
Li Hongliang
Kim Han-Sol
Kim Hye-Won
Seo Mi-Seon
Ha Kwon-Soo
Han Eun-Taek
Hong Seok-Ho
Firth Amy L.
Choi Il-Whan
Bae Young-Min
Park Won-Sun
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Abstract
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We demonstrated the effect of nortriptyline, a tricyclic antidepressant drug and serotonin reuptake inhibitor, on voltage-dependent K+ (Kv) channels in freshly isolated rabbit coronary arterial smooth muscle cells using a whole-cell patch clamp technique. Nortriptyline inhibited Kv currents in a concentration-dependent manner, with an apparent IC50 value of 2.86±0.52 μM and a Hill coefficient of 0.77±0.1. Although application of nortriptyline did not change the activation curve, nortriptyline shifted the inactivation current toward a more negative potential. Application of train pulses (1 or 2 Hz) did not change the nortriptyline-induced Kv channel inhibition, suggesting that the effects of nortiprtyline were not use-dependent. Preincubation with the Kv1.5 and Kv2.1/2.2 inhibitors, DPO-1 and guangxitoxin did not affect nortriptyline inhibition of Kv channels. From these results, we concluded that nortriptyline inhibited Kv channels in a concentration-dependent and state-independent manner independently of serotonin reuptake.
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KEYWORD
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Coronary artery, Nortriptyline, Voltage-dependent K+ channel
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