The Ca2 + channel inhibitor EFONIDIPINE (cas 111011-63-3) decreases voltage-dependent K+ channel activity in rabbit coronary arterial smooth muscle cells

Add time:08/25/2019    Source:sciencedirect.com

The effect of EFONIDIPINE (cas 111011-63-3), 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 0.26 μM 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 mV. 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.

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