IndraLab

Statements

Flecainide inhibits KCNH2. 14 / 15
2 | 1 11
reach
"10muM flecainide blocks 80% and 1muM only 20% of wild-type hERG current in a HEK293 cell model [XREF_BIBR]."
29760739
reach
"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]"
29551391
reach
"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)."
34025432
ctd
No evidence text available
15272206
ctd
No evidence text available
24052561
reach
"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."
29760739
reach
"HERG channels were blocked by D,L-sotalol, quinidine and flecainide (IC (50) : 69, 0.33 and 0.74 micromol/L, respectively)."
17604185
reach
"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)."
27237957
reach
"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."
28379974
eidos
"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 ) ."
32038248
reach
"Thus, flecainide inhibits hERG currents by 81% at 10mum and lidocaine inhibits hERG by 25% at 100 muM."
18493243
reach
"The inactivation-dependence of flecainide block of hERG was studied further using mutants with impaired inactivation (XREF_FIG)."
26159617
reach
"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."
26159617
reach
"Flecainide also blocks hERG channels and increases the conductance of the potassium rectifier current I K1."
33519442