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The Ca2+ channel inhibitor efonidipine decreases voltage-dependent K+ channel activity in rabbit coronary arterial smooth muscle cells
- Authors
- 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
- Issue Date
- Sep-2013
- Publisher
- ELSEVIER SCIENCE INC
- Keywords
- Efonidipine; Voltage-dependent K+ channels; Coronary artery
- Citation
- VASCULAR PHARMACOLOGY, v.59, no.3-4, pp 90 - 95
- Pages
- 6
- Journal Title
- VASCULAR PHARMACOLOGY
- Volume
- 59
- Number
- 3-4
- Start Page
- 90
- End Page
- 95
- ISSN
- 1537-1891
1879-3649
- Abstract
- 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.
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