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  • Title: The class III anti-arrhythmic agent, amiodarone, inhibits voltage-dependent K(+) channels in rabbit coronary arterial smooth muscle cells.
    Author: Li H, Kim HS, Kim HW, Shin SE, Jung WK, Ha KS, Han ET, Hong SH, Firth AL, Bae YM, Choi IW, Park WS.
    Journal: Naunyn Schmiedebergs Arch Pharmacol; 2016 Jul; 389(7):713-21. PubMed ID: 27030392.
    Abstract:
    We examined the inhibitory effect of amiodarone, a class III anti-arrhythmic agent, on voltage-dependent K(+) (Kv) currents in freshly isolated rabbit coronary arterial smooth muscle cells, using a whole-cell patch clamp technique. Amiodarone inhibited Kv currents in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) value of 3.9 ± 1.44 μM and a Hill coefficient of 0.45 ± 0.14. Amiodarone did not have a significant effect on the steady-state activation of Kv channels, but shifted the inactivation current toward a more negative potential. Application of consecutive pulses progressively augmented the amiodarone-induced Kv channel inhibition. Another class III anti-arrhythmic agent, dofetilide, did not inhibit the Kv current or change the inhibitory effect of amiodarone on Kv channels. Therefore, these results strongly suggest that amiodarone inhibits Kv currents in a concentration- and state-dependent manner.
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