IndraLab

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Flecainide inhibits KCNH2. 19 / 23
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"Thus, flecainide inhibits hERG currents by 81% at 10mum and lidocaine inhibits hERG by 25% at 100 muM."
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"Supplementary Fig. 1 iCell cardiomyocytes were treated with flecainide, a class Ic antiarrhythmic, which inhibits hERG and sodium channels at similar concentration range."
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"Moreover, Flecainide blocks the rapid component of the delayed rectifier potassium current (IKr) (KCNH2 and KCNQ1), prolonging the action potential duration (APD) in ventricular and atrial muscle fibe[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Flecainide has also been shown to block hERG channels at physiologically relevant concentrations (Paul et al., 2002), and QX-FL and NU-FL have been used to demonstrate that, as is the case in the Na + channel, hERG block requires entry of a cationic blocking molecule from the cell interior (Melgari et al., 2015)."
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"The previous histologic and transcriptome analyses showed hERG is expressed in sour taste cells (Ohmoto et al., 2006; Ren et al., 2017), thus blockade of hERG by flecainide could increase the excitability of sour cells."
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"Flecainide is known to block cardiac Na channels (IC50 = 7.4 μM [45])and hERG channel (IC50 = 4 μM and other K channels (IC50 = 10.7 μM [46])."
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"The inactivation-dependence of flecainide block of hERG was studied further using mutants with impaired inactivation (XREF_FIG)."
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"Flecainide may also inhibit the rapid delayed rectifier K current (I ), which is carried by K 11.1 channels (human Ether-à-go-go-Related Gene, or hERG) and is responsible for the late repolarization restoring the resting membrane potential in cardiomyocytes (Figure 2) [26,30]."
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"Independent support for the idea that flecainide acts to inhibit hERG from the cell interior comes from the observation that the drug 's action is potentiated in cells transfected with the drug uptake transporter OCTN1 XREF_BIBR."
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"However for several drugs , mutation of F656 produces much stronger attenuation of block than does mutation of Y652 ( see Table 1 ) ; block of hERG by flecainide , for example , is relatively insensitive to mutation of Y652 to alanine , whereas block is attenuated by nearly 150-fold in the F656A mutant ( Melgari et al ., 2015a ) ."
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"HERG inhibition by flecainide [XREF_BIBR] at this clinical dose is reported, at higher doses this effect is less marked (XREF_FIG) reflecting the integrated sum of other off-target effects."
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"Results : Ajmaline, amiodarone, ivabradine, flecainide, quinidine, mexiletine and ranolazine inhibited the hERG channel current (I Kr) less strongly in hiPSC-CMs from the SQTS1-patient (SQT1-hiPSC-CMs) comparing with cells from the healthy donor (donor-hiPSC-CMs)."
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"This is probably a consequence of the ability of flecainide to block I Kr / hERG [XREF_BIBR] : decreased repolarization rate of CM membrane leads to prolongation in APD."
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"Flecainide inhibits hERG with reported IC values of ∼3 µM by interacting with F656 in the S6 segment (Melgari et al., 2015)."
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"10muM flecainide blocks 80% and 1muM only 20% of wild-type hERG current in a HEK293 cell model [XREF_BIBR]."
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"T623, S624, G648, and Y652 are also known to affect flecainide inhibition of hERG to a lesser degree (Melgari et al., 2015)."
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"Flecainide strongly inhibited hERG current with additional peak/late Na + current ( Crumb et al., 2016 )."
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"Flecainide also blocks hERG channels and increases the conductance of the potassium rectifier current I K1."
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"For example, both flecainide and procainamide at therapeutic concentrations were reported to reduce I Kr in hERG-expressing cell lines ( Melgari, Zhang, El Harchi, Dempsey, & Hancox, 2015; Paul, Witch[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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