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Statements

Propafenone inhibits KCNH2. 9 / 17
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"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
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"The Class Ic drug propafenone has also been reported to produce a rapid open-state dependent block of hERG [53,54] that is not strongly contingent upon inactivation [16,32] , and with only the F656 re[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
21989164
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"WITCHEL HJ, DEMPSEY CE, SESSIONS RB et al. : The low potency, voltage dependent HERG blocker propafenone - molecular determinants and drug trapping."
17298291
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"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
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"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
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"Chloroquine, ajamaline and propafenone block HERG channels with similar IC 50 as maprotiline, and they have been found to essentially interact with Y652 and F656 ( Sanchez-Chapula et al., 2002; Kiesec[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16423345
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"In conclusion, propafenone has been found to block HERG potassium channels."
11330342
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"The low-potency, voltage dependent HERG blocker propafenone -- molecular determinants and drug trapping."
15308760
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"The effects of hERG blockers such as propafenone [23] and bepridil [10] were also reported to be selectively mediated by Phe656."
22020101