IndraLab

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"Here we show that KCNQ4 channels, stably expressed in HEK293 cells, were activated by retigabine and BMS-204352 in a reversible and concentration-dependent manner in the concentration range 0.1-10 microM."

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"Application of 10 μM retigabine increased the KCNQ4 current amplitude from 0.7 nA to 2.5 nA."

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"In the other experiment shown, retigabine (10 μM) increased the KCNQ4 current at −30 mV from 2.5 nA to 5.7 nA, and at −60 mV from 0.2 nA to 1.3 nA ( Fig. 1(A) , lower panel)."

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"Retigabine increased KCNQ4-mediated whole-cell current by more than 2-fold (Fig. 4a)."

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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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"KCNQ4 channel activation by BMS-204352 and retigabine."

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"Variants p.L47P, p.F182L, p.L281M, p.P291S, p.L285P, p.V672M, and p.S680F were rescued by retigabine (Fig. 4c), indicating that only some DFNA2-associated KCNQ4 variants are rescued by retigabine."

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"We here demonstrate that BMS-204352 as well as retigabine activate KCNQ4 channels expressed in HEK293 cells.The HEK293 cell line stably expressing KCNQ4 channels is described by Søgaard et al. (2000) [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"In this study we found an EC 50 value of 1.4 μM (at −30 mV) for retigabine activation of KCNQ4 channels."

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"The KCNQ4 current was concentration-dependently and reversibly increased by BMS-204352 and retigabine in the concentration range 0.1–10 μM."

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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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"Also, both BMS-204352 and retigabine potentiated the voltage activated KCNQ4 current at all potentials tested."