IndraLab

Statements

Ezogabine activates KCNQ5. 15 / 15
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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 activates Kv7.2–Kv7.5, but has no effect on Kv7.1 which is primarily found in cardiac myocytes."
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"Recently, Wickenden et al. (2001) have also shown that retigabine can activate the KCNQ5 and KCNQ3 heteromer expressed in CHO cells."
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"In the present study, retigabine enhanced the KCNQ5 current at -30 and -60 mV, by 3 and 7 fold, respectively."
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"Retigabine activated the KCNQ5 channel by increasing the current in a concentration dependent way."
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"The ability of retigabine, which activates Kv7.2–Kv7.5 (but not Kv7.1) to enhance portal vein K + currents, hyperpolarize myocyte resting membrane potential, and decrease portal vein spontaneous contr[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Interestingly, flupirtine and retigabine activate Kv7.2–Kv7.5 channels, but not Kv7.1 channels, apparently because the Kv7.1 channel lacks a transmembrane tryptophan residue required for the actions o[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Moreover, KCNQ3 and KCNQ5 channels are potently activated by the anticonvulsant retigabine (Wickenden et al., 2001)."
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"Exposures to DMSO vehicle control as well as retigabine, ICA-110381 and ML277 at 3 µM final concentrations were assessed and clearly show that both the Kv7.2 thru Kv7.5 activator retigabine as well as the Kv7.2/Kv7.3 activator ICA-110381 profoundly inhibited spontaneous activity while the Kv7.1 activator ML277 showed little or no inhibition of spontaneous spiking (Figure 2B)."
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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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"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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"In addition, the possible effects of form deprivation on potassium ionic currents and the pharmacological sensitivity of KCNQ5 activator Retigabine and inhibitor XE991 to the M-current in RPE cells were investigated using the patch-clamp technique."
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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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"KCNQ5 can be activated and inhibited by the specific KCNQ5 channel activator Retigabine and inhibitor XE991, which were selected to continue the in vitro cell experiment."
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