The Effects of the Selective Serotonin Reuptake Inhibitor Fluvoxamine on Voltage-Dependent K<SUP>+</SUP>Channels in Rabbit Coronary Arterial Smooth Muscle Cells

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초록

We demonstrated the inhibitory effect of fluvoxamine, a selective serotonin reuptake inhibitor (SSRI), on voltage-dependent K+ (Kv) channels in freshly isolated rabbit coronary arterial smooth muscle cells using a whole-cell patch clamp technique. Fluvoxamine reduced the amplitude of Kv currents in a concentration-dependent manner with an IC50 value of 3.71 +/- 1.09 mu m and a Hill coefficient of 0.62 +/- 0.14. Although fluvoxamine did not significantly affect the steady-state activation curve, it shifted the steady-state inactivation curve toward a more negative potential. Pretreatment with another SSRI, paroxetine, did not affect the basal Kv current and did not alter the inhibitory effect of fluvoxamine on Kv channels. We concluded that fluvoxamine inhibits the Kv current in a concentration-dependent manner and in a closed (inactivated) state of the Kv channels independent of serotonin reuptake inhibition.

키워드

fluvoxaminevoltage-dependent K+ channelcoronary arterysmooth muscleselective serotonin reuptake inhibitorGATED K+ CHANNELSCATECHOLAMINE METABOLITESPOTASSIUM CURRENTSSIGMA(1) RECEPTORPLASMA-LEVELSMODULATIONBLOCK
제목
The Effects of the Selective Serotonin Reuptake Inhibitor Fluvoxamine on Voltage-Dependent K<SUP>+</SUP>Channels in Rabbit Coronary Arterial Smooth Muscle Cells
저자
Hong, Da HyeLi, HongliangKim, Han SolKim, Hye WonShin, Sung EunJung, Won-KyoNa, Sung HunChoi, Il-WhanFirth, Amy LeannePark, Won SunKim, Dae-Joong
DOI
10.1248/bpb.b15-00207
발행일
2015-08
유형
Article
저널명
Biological and Pharmaceutical Bulletin
38
8
페이지
1208 ~ 1213