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NS1643 activates KCNH2. 21 / 21
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"When assessed with 2-s depolarizations, NS1643 enhanced the magnitude of wild-type hERG current in a concentration- and voltage dependent manner with an EC (50) of 10.4 microM at -10 mV."
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"NS1643, which activated hERG current by 55% at 3muM in hERG transfected HEK293 cells, significantly shortened APD and increased coronary flow at 1 and 10muM."
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"In the absence of channel inactivation, NS1643 did not enhance hERG current magnitude."
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"In this study, we showed that both mallotoxin and NS1643 activated hERG current by 87% and 55% at 3muM, respectively."
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"Casis et al. (11) reported that NS1643 activates hERG channels expressed in Xenopus oocytes in a concentration- and voltage dependent manner and strongly affects channel inactivation by shifting the v[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In contrast, NS1643 increased ERG1 current by affecting inactivation properties only."
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"In addition, the different profile of ERG1 and ERG2 channel activation by NS1643 may be useful in structure-function studies of the two channel subtypes.To further characterize the pharmacology of ERG[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The ability of NS1643 to increase ERG1 current was more prominent when recorded at the end of the tail compared to peak current."
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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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"Nevertheless, the two contributions indeed provide compelling arguments for underlying mechanistic principles that possibly govern NS1643-dependent activation of Kv11.1 channels."
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"Nevertheless, NS1643 then continued to produce concentration- and voltage dependent increases in hERG current amplitude."
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"In contrast, hERG1 channel activation by NS1643 and NS3623 preserves the wild-type function making the channels primarily active in the repolarising phase of the action potential."
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"NS1643, a Kcnh2 activator, was applied to activate Kcnh2 for confirming again the role of Kcnh2 in SICD."
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"Activation of Kcnh2 by NS1643 exhibited opposite outcome , indicating a potential role of the molecule in heart protection during sepsis ."
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"Activation of Kcnh2 by NS1643 exhibited opposite outcome, indicating a potential role of the molecule in heart protection during sepsis."
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"NS1643 was initially reported to enhance hERG current magnitude without measurable effects on current kinetics [11] ."
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"Later on, NS1643 was shown to reduce inactivation and slow deactivation of the hERG channel [12,17] ."
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"NS1643 ( Grunnet et al., 2011 ) increases hERG current by shifting the voltage dependence of inactivation to more positive potentials, while also lowering the voltage dependence of activation."
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"The detail molecular mechanism underlying the interaction between ICA-105574 and hERG inhibitors need to be further defined.Similar to ICA-105574, NS1643 activates hERG primarily by altering the volta[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"HERG channels treated with NS1643 behave in a very similar way to WT channels in the absence of NS1643 : following depolarization, NS1643 activated HERG channels inactivate rapidly and recover from inactivation, passing an outward current as the membrane potential recovers."
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"As expected, mallotoxin activated hERG current by 87% at 3muM, and NS1643 activated hERG current by 55% at 3muM."
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