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Ezogabine activates KCNQ4. 15 / 17
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"Retigabine has been the most characterized activator of KCNQ channels and has been shown to potentiate KCNQ2, KCNQ3, KCNQ4, and KCNQ5, without activating KCNQ1, thereby avoiding potential cardiac effects [XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR]."
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"Retigabine increased KCNQ4-mediated whole-cell current by more than 2-fold (Fig. 4a)."
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"It was initially found that 200 μM retigabine was sufficient to produce a maximal current activation of Kv7.4, in the sense that higher concentrations of retigabine did not result in further augmentat[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"In the other experiment shown, retigabine (10 μM) increased the KCNQ4 current at −30 mV from 2.5 nA to 5.7 nA, and at −60 mV from 0.2 nA to 1.3 nA ( Fig. 1(A) , lower panel)."
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"SCHRODER RL, JESPERSEN T, CHRISTOPHERSEN P et al. : KCNQ4 channel activation by BMS-204352 and retigabine."
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"KCNQ4 channel activation by BMS-204352 and retigabine."
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"Application of 10 μM retigabine increased the KCNQ4 current amplitude from 0.7 nA to 2.5 nA."
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"The KCNQ4 current was concentration-dependently and reversibly increased by BMS-204352 and retigabine in the concentration range 0.1–10 μM."
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"Retigabine activates Kv7.2, Kv7.3, Kv7.4 and Kv7.5 channels [152] , but inhibits Kv7.1 channels [153] ."
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"Ezogabine also activates neuronal Kv7.4 and Kv7.5, but at clinically relevant concentrations has no effect on cardiac Kv7.1 channels [87]."
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"In this study we found an EC 50 value of 1.4 μM (at −30 mV) for retigabine activation of KCNQ4 channels."
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"Also, both BMS-204352 and retigabine potentiated the voltage activated KCNQ4 current at all potentials tested."
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"The preference for KCNQ4 activation was in contrast to GABA and gabapentin, which we previously found to each activate only KCNQ3 and KCNQ5, and to retigabine which favors KCNQ3 and activates KCNQ2, KCNQ4 and KCNQ5 to a lesser extent, and does not activate KCNQ1 ."
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"Retigabine activates Kv7.2, Kv7.3, Kv7.4 and Kv7.5 channels [152] , but inhibits Kv7.1 channels [153] ."
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"We here demonstrate that BMS-204352 as well as retigabine activate KCNQ4 channels expressed in HEK293 cells.The HEK293 cell line stably expressing KCNQ4 channels is described by Søgaard et al. (2000) [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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