Abstract
The action of alprenolol, a non-selective beta blocker as well as 5-HT receptor antagonist, on the cloned cardiac human ether-a-go-go-related gene (HERG) channels was investigated using the whole-cell patch-clamp technique. Alprenolol reduced HERG whole-cell currents in a reversible concentration-dependent manner, with an IC50 value and a Hill coefficient of 12.3 ± 0.8 ∈1/4M and 0.98 ± 0.06, respectively. Alprenolol affected the channels in the activated and inactivated states but not in the closed states. The alprenolol-induced blockade of HERG was found to be use-dependent, exhibiting a more rapid onset and a greater steady-state block at the higher frequencies of activation. These results suggest that alprenolol prolongs the QT interval by direct inhibition of activated HERG channels.Keywords: alprenolol, HERG channel
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