IndraLab

Statements

Propafenone inhibits KCNH2. 11 / 11
1 4 | 6
reach
"The data show that extending the size of a trapped HERG blocker like propafenone by adding a bulky side chain may impede channel closure and thereby facilitate drug dissociation at rest."
21175572
reach
"Propafenone and 5-hydroxypropafenone (2 microM) inhibited HERG current by 78.7 +/-2.3% (n = 7) and 71.1 +/-4.1% (n = 7, P> 0.05) when measured at the end of 5-s depolarizing pulses to -10 mV."
12618228
ctd
No evidence text available
24052561
reach
"In the early 2000s, racemic propafenone was demonstrated to block overexpressed hERG1 channels in cellular models and native I Kr current from isolated rabbit ventricular myocytes at IC 50 values comparable with those of quinidine 0.4-0.8 muM in mammals) and within therapeutic plasma concentrations."
21833176
reach
"The low-potency, voltage dependent HERG blocker propafenone -- molecular determinants and drug trapping."
15308760
reach
"In this study, the trapping mechanisms of a trapped hERG blocker propafenone and a bulky derivative (MW : 647.24 g mol -1) were studied by making use of electrophysiological measurements in combination with molecular dynamics simulations."
28337337
ctd
No evidence text available
21175572
reach
"In conclusion, propafenone has been found to block HERG potassium channels."
11330342
ctd
No evidence text available
18724381
tas
No evidence text available
15324906
ctd
No evidence text available
14678746