IndraLab

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"LFZ also appears more potent than the previously studied antianginal agent perhexiline (IC 50 of 7.8 μM in CHO-K1 cells [14] ), and than mibefradil and bepridil (IC 50 values of 0.55 and 1.43 μM in CO[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Since verapamil inhibits hERG and L-type calcium channels at overlapping concentrations ( Harris et al., 2013 ), the inhibitory effect on hERG may therefore have been masked by the inhibitory effect o[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"The lack of prolongation with verapamil suggests that strong calcium block may attenuate the effects of hERG potassium channel block.Loratadine is a second-generation, peripheral H 1 -receptor antagon[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Several preclinical studies suggest an important role for sodium, potassium (Ca activated, outward rectifying, and hERG) and chloride ion-channels as well as Na-K-Cl cotransporter on GBM cell migration and parenchymal invasion, possibly through effects on cellular volume and shape."

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"An external Ca 2+ also accelerates the rate of HERG tails ( Johnson et al., 1999 )."

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"Electrophysiological studies have identified a number of different ion channels in type-1 cells from various species including voltage-gated Na-channels, voltage-gated Ca 2+ -channels (see above), del[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"We recently found that extracellular Ca 2+ can modulate the voltage dependence of HERG channel activation independently of inactivation (Johnson et al., 1999)."

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"These changes reflect altered hERG1 gating because no rapid currents were induced in uninjected oocytes treated with these concentrations of Ca 2+ or Cd 2+ (XREF_FIG)."

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"Further research has revealed that simultaneous block of other ion channels, especially the late sodium and the L-type calcium channel, can attenuate the proarrhythmic effects of pure hERG and IKr block despite the presence of QT prolongation."

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"Although we can not definitively rule out the possibility that Ca 2+ causes an allosteric change in HERG channels that mimics a specific association near the activation voltage sensor, our data are consistent with a simple Ca 2+ -induced change in membrane potential sensed specifically by the activation process."

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"Targets (2007) 11 (3) 329 The hERG potassium channel as a therapeutic targetExceptions include the calcium channel antagonist verapamil, which blocks hERG at clinically relevant concentrations [129], as does the antihistamine clemastine [130] and the selective serotonin receptor inhibitor citalopram [131]; yet none of these are associated with a substantial clinical risk of QT prolongation, TdP or even AP duration lengthening [132]."

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"Elevated extracellular K + (20 mM) decreases the shift in the HERG channel isochronal current-voltage curve caused by Ca 2+."