IndraLab

Statements

Ezogabine activates KCNQ3. 19 / 20
1 | 15 4
reach
"Retigabine activates KCNQ2 with an IC of 2.5 μM and KCNQ3 with an IC of 600 nM Attali et al. (2023)."
37808870
reach
"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
reach
"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
sparser
"The KCNQ3 activation by retigabine is nearly maximal in tetramers with a single retigabine-sensitive subunit."
30373787
reach
"The KCNQ3 activation by retigabine is nearly maximal in tetramers with a single retigabine-sensitive subunit."
30373787
sparser
"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
reach
"Moreover, KCNQ3 and KCNQ5 channels are potently activated by the anticonvulsant retigabine (Wickenden et al., 2001)."
12890507
reach
"Retigabine activates KCNQ2 with an IC of 2.5 μM and KCNQ3 with an IC of 600 nM (Alexander et al., 2019)."
39625473
reach
"Retigabine activates Kv7.2, Kv7.3, Kv7.4 and Kv7.5 channels [152] , but inhibits Kv7.1 channels [153] ."
36283445
reach
"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
reach
"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
reach
"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
reach
"Recently, Wickenden et al. (2001) have also shown that retigabine can activate the KCNQ5 and KCNQ3 heteromer expressed in CHO cells."
11890900
reach
"Remarkably, however, this single atom alteration in each of the KCNQ3 * subunits entirely abolishes retigabine activation of KCNQ3 * channels (XREF_FIG)."
26333338
reach
"Retigabine potentiation of KCNQ3 * channels was retained with F 3 -Trp substitution at Trp265 (XREF_FIG), a substitution that still potently diminishes the negative electrostatic potential on the face of the side chain (XREF_FIG), indicating that a cation-pi interaction of Trp265 with retigabine or some other entity (perhaps another channel residue) is not required for retigabine effects."
26333338
reach
"The M-type current was activated by 1) 10 muM retigabine, an opener of all KCNQ channels except KCNQ1, 2) 10 muM zinc pyrithione, which augments all KCNQ channels except KCNQ3, and 3) 50 muM N-ethylmaleimide, which activates KCNQ2, KCNQ4, and KCNQ5, but not KCNQ1 or KCNQ3, channels."
22135213
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
reach
"The antiepileptic drug retigabine rescued KCNQ3 currents that were abolished by a mutation disrupting E-M coupling, suggesting that modulating the E-M coupling in KCNQ channels presents a potential strategy for antiepileptic therapy."
35857840
sparser
"Retigabine activates Kv7.2, Kv7.3, Kv7.4 and Kv7.5 channels [152] , but inhibits Kv7.1 channels [153] ."
36283445