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Ezogabine activates KCNQ2. 32 / 34
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"These results are consistent with voltage clamp studies that demonstrated a leftward shift in the voltage dependence for KCNQ2 activation induced by retigabine [28] ."
12871719
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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]"
27179745
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"Retigabine activates KCNQ2 with an IC of 2.5 μM and KCNQ3 with an IC of 600 nM Attali et al. (2023)."
37808870
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"Retigabine activates the Kv7.2 and Kv7.3 channels via an increase in the maximal opening probability of the channels and a hyperpolarization shift of the voltage dependence of channel activation (17)."
34509475
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"W236 in the S5 is a critical residue for retigabine-induced Kv7.2 activation [ xref ] and ML252-induced Kv7 inhibition [ xref ]."
40175331
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"Retigabine was known to act on KCNQ4 as early as 2012 and confirmed to prolong the opening of KCNQ2 and KCNQ3, but it has also been demonstrated to increase the current from KCNQ4 ."
38956136
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"Altogether, reduction of A-fiber-mediated transmission may also contribute partly to reversal of thermal hypersensitivity by retigabine.Of the five KCNQ channel proteins, retigabine activates neuronal[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
38750803
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"Cryo-electron microscopy was utilized by Li et al. (2021) to determine the structure of human KCNQ2 in its apolipoprotein form; they found that retigabine binds to the pore domain and activates the KCNQ2 channel via allosteric modulation, resulting in adequate control of epileptic symptoms.The voltage-gated sodium channel initiates the transduction of electrical signals to generate and transmit action potentials (Payandeh et al., 2011)."
38989927
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"Ezogabine activates Kv7.2–Kv7.5, but has no effect on Kv7.1 which is primarily found in cardiac myocytes."
22917854
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"Retigabine activates mainly heteromeric Kv7.2 and Kv7.3 channels and as a result causes changes in resting membrane potential towards more negative levels (ie hyperpolarization)."
29101377
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"A previous study reported that PIP2 rundown prevents retigabine activation of KCNQ2 channels ( xref )."
29078287
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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 ."
31701029
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"As expected, the positive controls flupirtine, retigabine, and RL-81 increased the half-maximal voltage-dependent Kv7.2 activation (ΔV ) up to three-fold at 5 μM and thereby provided large shifts in ΔV values."
35671848
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"We further show with the operant behavioral test that oxaliplatin-induced orofacial mechanical allodynia can be alleviated by the KCNQ2 potentiator retigabine."
28741430
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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]"
19439185
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"These results are consistent with voltage clamp studies that demonstrated a leftward shift in the voltage dependence for KCNQ2 activation induced by retigabine [28]."
12871719
sparser
"Retigabine activates the Kv7.2 and Kv7.3 channels via an increase in the maximal opening probability of the channels and a hyperpolarization shift of the voltage dependence of channel activation ( xref )."
34509475
sparser
"Retigabine activates Kv7.2, Kv7.3, Kv7.4 and Kv7.5 channels [152] , but inhibits Kv7.1 channels [153] ."
36283445
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"Retigabine activates KCNQ2 with an IC of 2.5 μM and KCNQ3 with an IC of 600 nM (Alexander et al., 2019)."
39625473
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"Experimental studies have shown retigabine [XREF_BIBR] as well as retigabine derivative HN38 [XREF_BIBR] to significantly increase potassium currents in mutated KCNQ2 channels, suggesting their potential as a targeted therapy for KCNQ2 related epilepsies."
27154366
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"Retigabine activates Kv7.2, Kv7.3, Kv7.4 and Kv7.5 channels [152] , but inhibits Kv7.1 channels [153] ."
36283445
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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]."
33801540
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"In cells expressing WT KCNQ2, G256W and WT KCNQ3, mimicking heterozygosity and predicted to yield a mixed population of channels (Figure 3A), ezogabine significantly increased currents and shifted activation voltage dependence (Figure 3C, D, E)."
38260608
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"In cells expressing WT KCNQ2, G256W and WT KCNQ3, mimicking heterozygosity and predicted to yield a mixed population of channels (Figure 3A), ezogabine significantly increased currents and shifted activation voltage dependence (Figure 3C, D and E)."
39761077
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"W236 in the S5 is a critical residue for retigabine-induced Kv7.2 activation [44] and ML252-induced Kv7 inhibition [45]."
40175331
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"Although retigabine and ztz240 are both activators of KCNQ2 and exhibit antiepileptic activity, they bind at distinct sites in the channel."
37298178
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"A previous study reported that PIP2 rundown prevents retigabine activation of KCNQ2 channels."
29078287
eidos
"Here , we report cryo-electron microscopy ( cryo-EM ) structures of the human KCNQ2 determined in apo state and in complex with two activators , ztz240 or retigabine , which activate KCNQ2 through different mechanisms ."
32884139
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"Retigabine activates Kv7.2, Kv7.3, Kv7.2–Kv7.3, Kv7.4 and Kv7.5 channels, with an effective concentration for half-maximum response (EC 50 ) of 1.4 μM at −30 mV for Kv7.2 [53] ."
18206251
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"KCNQ2-L275 (or L314, its equivalent in KCNQ3), close to the selectivity filter, also influences RTG activation of KCNQ2 and may impinge on or form part of the binding site xref , as illustrated here using in silico docking to a model chimeric structure derived from the Xenopus KCNQ1 cryo-EM structure with KCNQ3 RTG binding residues and close neighbors added (Fig.  xref , upper)."
30242262
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"Since retigabine modulates Kv7.2 thru Kv7.5, Retigabine will also impact tissues such as smooth muscle which could lead to hypotension or defects in lymphatic function (Jepps et al., 2013; Khanamiri et al., 2013) or skeletal muscle where retigabine is reported to modulate proliferation and differentiation (Iannotti et al., 2010)."
36923357
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"In the present study, we used the orofacial operant test to determine effects of subcutaneous administration of KCNQ2 blocker XE991 and KCNQ2 activator retigabine on orofacial cold sensitivity."
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