The Ca<SUP>2+</SUP> channel inhibitor efonidipine decreases voltage-dependent K<SUP>+</SUP> channel activity in rabbit coronary arterial smooth muscle cells

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초록

The effect of efonidipine, a commercially available antihypertensive drug and Ca2+ channel inhibitor, on voltage-dependent K+ (Kv) channels was studied in freshly isolated rabbit coronary arterial smooth muscle cells using the whole-cell patch clamp technique. The amplitude of Kv current was decreased by application of efonidipine in a dose-dependent manner, with IC50 of 026 mu M and a Hill coefficient of 0.91, which suggests 1:1 binding stoichiometry. Efonidipine did not affect voltage-dependent activation of the Kv channel, but shifted the inactivation curve by -8.87 my. The inhibitory effect of efonidipine was not significantly changed by depletion of extracellular Ca2+ or intracellular ATP, which indicated no involvement of the Ca2+ channel or intracellular protein kinase-dependent cascades. We conclude that efonidipine dose-dependently inhibits Kv current in a phosphorylation- and Ca2+ channel-independent manner. (C) 2013 Elsevier Inc. All rights reserved.

키워드

EfonidipineVoltage-dependent K+ channelsCoronary arteryT-TYPECALCIUM-CHANNELSBLOCKVERAPAMILCURRENTSANTAGONISTSMODULATIONMIBEFRADILACTIVATORRELEASE
제목
The Ca<SUP>2+</SUP> channel inhibitor efonidipine decreases voltage-dependent K<SUP>+</SUP> channel activity in rabbit coronary arterial smooth muscle cells
저자
Park, Mi-HyeongSon, Youn KyoungHong, Da HyeChoi, Il-WhanKim, Dae-JoongLee, HaenaBang, HyoweonNa, Sung HunLi, HongliangJo, Su-HyunPark, Won Sun
DOI
10.1016/j.vph.2013.07.005
발행일
2013-09
유형
Article
저널명
Vascular Pharmacology
59
3-4
페이지
90 ~ 95