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Dronedarone inhibits KCNH2. 6 / 11
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"RIDLEY JM, MILNES JT, WITCHEL HJ, HANCOX JC : High affinity HERG K+ channel blockade by the antiarrhythmic agent dronedarone : resistance to mutations of the S6 residues Y652 and F656."
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"Dronedarone blocked HERG channels with an IC50 value of 9.2 microM and a maximum tail current reduction of 85.2%."
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"The half-maximal activation voltage was shifted by -6.1 mV, and HERG current block by dronedarone was voltage dependent, but not use dependent."
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"The L532P mutation produced an ~ 5-fold increase in the IC 50 for dronedarone inhibition of I hERG ."
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"However, some exceptions have been found, vesnarinone does not require Y652 ( Kamiya et al., 2001 ) and fluvoxamine and dronedarone, which can block HERG when F656 and Y652 are mutated ( Milnes et al.[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Dronedarone inhibits the I (Kv7.1) and I (Kv11.1) currents.Finally, there are classic drugs that find their therapeutic niche in patients with preserved cardiac function and no structural abnormalities [88]."
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