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The Ca<SUP>2+</SUP> channel inhibitor efonidipine decreases voltage-dependent K<SUP>+</SUP> channel activity in rabbit coronary arterial smooth muscle cells
- Park, Mi-Hyeong;
- Son, Youn Kyoung;
- Hong, Da Hye;
- Choi, Il-Whan;
- Kim, Dae-Joong;
- ... Na, Sung Hun;
- ... Jo, Su-Hyun;
- ... Park, Won Sun;
- 외 3명
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12초록
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
- 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-Hyeong; Son, Youn Kyoung; Hong, Da Hye; Choi, Il-Whan; Kim, Dae-Joong; Lee, Haena; Bang, Hyoweon; Na, Sung Hun; Li, Hongliang; Jo, Su-Hyun; Park, Won Sun
- 발행일
- 2013-09
- 유형
- Article
- 권
- 59
- 호
- 3-4
- 페이지
- 90 ~ 95