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RPR260243 activates KCNH2. 5 / 5
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"RPR260243 and ginsenoside Rg3 slow the rate of hERG1 channel deactivation."
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"The first hERG1 activator to be discovered, RPR260243 ((3R,4 R)-4-[3-(6-methoxyquinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluorophenyl)-prop-2-ynyl]-piperidine-3-carboxylic acid) (RPR) induces a pronounced, voltage dependent slowing of hERG1 deactivation."
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"RPR260243 induces two distinct changes in hERG gating: a slowing of deactivation and a positive shift in the voltage-dependence of inactivation [9,15] , while NS1643 and NS3623 enhance hERG current ma[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Some other hERG channel activators such as RPR260243 that can increase the T-wave amplitude, prolong the PR interval and shorten the QT interval in guinea-pig hearts; and PD-118057 that shortens the a[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Here, we show that, at physiological temperature, RPR260243 enhances hERG channel repolarizing currents conducted in the refractory period in response to premature depolarizations."
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