XE-991 dihydrochloride, KCNQ channel blocker; blocks M current

• FuncS

PubMed

Functional Studies - XE-991 dihydrochloride, KCNQ channel blocker; blocks M current (AB120089)

To assess the effects of blockade of muscarine-dependent K+ current, I_M, under voltage clamp conditions, and to determine if carbachol, CCh, acts through the blockade of an additional conductance other than I_M, voltage ramps were performed in ACSF containing TTX (0.5 μM), ZD7288 (50 μM), prior to and during sequential addition of XE-991 (10 μM) and CCh (50 μM) (n=9). Application of XE-991 in the presence of TTX and ZD7288 resulted in a significant increase in current required to hold neurons at -60 mV (-18.1±6.6 pA; N–K : p<0.05).

Bath application of XE-991 (10 μM; white bar) resulted in an inward current in cells held at -60 mV indicating that the cells express I_M, and the subsequent perfusion with CCh (50 μM) resulted in an additional inward current, suggesting that CCh blocks a second K+ conductance (* : p<0.05).

Image from Glasgow SD et al., PLoS One. 2013;8(3):e58901. Fig 7(A).; doi: 10.1371/journal.pone.0058901. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

• FuncS

PubMed

Functional Studies - XE-991 dihydrochloride, KCNQ channel blocker; blocks M current (AB120089)

Left - Theta burst stimulation (TBP) does not induce long-term potentiation (LTP) under control conditions. Coincident TBP of subthreshold excitatory post-synaptic potentials (EPSPs) and somatic action potentials induced no change in EPSC amplitude in the test (black circles) or control (white circles) pathways. The arrow indicates the timing of the TBP protocol. Example voltage traces show the initial burst of 5 coincident EPSPs and action potentials and a single test burst of 5 subthreshold EPSPs. Example current traces from a single experiment illustrating the mean EPSC response during the baseline (1) and at 30–35 minutes (2) in the test and control pathways.Right - TBP does induce LTP in the presence of the Kv7 channel inhibitor XE-991 (ab120089). In the presence of XE-991 (10 µM), coincident TBP of subthreshold EPSPs and somatic action potentials induced pathway-specific LTP.

Image from Petrovic MM et al., PLoS One. 2012;7(2):e30402. Fig 1(B,C).; doi: 10.1371/journal.pone.0030402. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

• Chemical Structure

Lab

Chemical Structure - XE-991 dihydrochloride, KCNQ channel blocker; blocks M current (AB120089)

2D chemical structure image of ab120089, XE-991 dihydrochloride, KCNQ channel blocker; blocks M current