IndraLab

Statements

Cocaine inhibits KCNH2. 5 / 5
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"These results indicate that cocaine suppresses HERG, but not KvLQT1+ minK, channels by preferentially blocking activated channels, that it unblocks upon repolarization, and does so with unique ultrarapid kinetics."
11306689
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"At clinically relevant doses, cocaine inhibits the HERG channel, but not the KvLQT1+ mink K + channel (Ferreira et al., 2001; Zhang et al., 2001)."
12576134
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"In contrast, cocaine reversibly blocked HERG current with half-maximal block of peak tail current of 7.2 microM."
11306689
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"Although Peles et al. [10] did not find a significant correlation between methadone dose and QTc duration in their overall sample, a significant correlation was found among patients who tested positive for cocaine (r = 0.4, P = 0.003), which is known to block the HERG potassium channel that contributes to cardiac repolarization [19-22]."
20508789
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"Blockade of HERG by cocaine, cocaethylene, and methylecgonidine increased significantly over the voltage range where HERG activates, but became constant at voltages where HERG activation was maximal, indicating that all three drugs block open channels, but by a mechanism that is not highly sensitive to voltage per se."
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