IndraLab

Statements

Ezogabine activates KCNQ2. 16 / 16
1 1 1 | 1 8 4
sparser
"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
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
"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
dgi
No evidence text available
reach
"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
reach
"A previous study reported that PIP2 rundown prevents retigabine activation of KCNQ2 channels."
29078287
reach
"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
ctd
No evidence text available
15634793
sparser
"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
sparser
"A previous study reported that PIP2 rundown prevents retigabine activation of KCNQ2 channels ( xref )."
29078287
signor
No evidence text available
Other
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
"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."
29133175
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
reach
"KCNQ2, KCNQ2/Q3, and KCNQ3/Q4 channels were activated to a similar degree as KCNQ4 channels by 10 microM of BMS-204352 and retigabine, respectively."
11378159
reach
"We further show with the operant behavioral test that oxaliplatin-induced orofacial mechanical allodynia can be alleviated by the KCNQ2 potentiator retigabine."
28741430