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- Rundfeldt, C. (1997) Eur. J. Pharmacol. 336, 243.
- Wickenden, A.D. et al. (2000) Mol. Pharmacol. 58, 591.
- Tatulian, L. et al. (2000) J. Neurosci. 21, 5535.
- Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.
- Brodie, M.J. et al. (2010) Neurology 75, 1817.
- Alomone Labs Retigabine enhances KCNQ2/3 (KV7.2/7.3) currents in Xenopus oocytes.A. Superimposed traces (responses to 600 ms voltage steps from -50 mV to 0 mV, holding potential -100 mV, applied every 10 sec) of KCNQ2/3 channel current responses, before (left) and during (right) application of 10 µM Retigabine (#R-100). B. Time course of current amplitude at -50 mV (holding potential -100 mV, applied every 10 sec) before, during application of 0.1 and 1 µM Retigabine (indicated by bars) and upon wash, demonstrating the current amplitude enhancement. C. I-V relations in an experiment such as in A (left before, and right, during Retigabine application). D. Voltage dependence of current increase/decrease by Retigabine.
- Kullmann, D.M. (2002) J. Mol. Brain 125, 1117.
- Robbins, J. (2001) Pharmacol. Ther. 90, 1.
- Wang, H.S. et al. (1998) Science 282, 1890.
- Rundfeldt, C. (1997) Eur. J. Pharmacol. 336, 243.
- Wickenden, A.D. et al. (2000) Mol. Pharmacol. 58, 591.
- Tatulian, L. et al. (2000) J. Neurosci. 21, 5535.
- Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.
- Brodie, M.J. et al. (2010) Neurology 75, 1817.
The KCNQ family of voltage-gated K+ channels includes five known members: KCNQ1 to KCNQ5. Structurally, the KCNQ family belongs to the six transmembrane domain category of K+ channels. KCNQ family members can form either homomultimeric or heteromultimeric channels with different functional consequences. For example, KCNQ2 and KCNQ3 heteromultimers give rise to a much larger channel current than when either protein is expressed alone. Indeed, KCNQ2/KCNQ3 heteromultimers are believed to be the molecular correlates of the so-called M current. This current is a K+ neuronal current that is strongly inhibited by the activation of the M1 subtype of the muscarinic acetylcholine receptor. Mutations in either KCNQ2 or KCNQ3 are associated with a form of epilepsy known as benign familial neonatal convulsions (BNFC)1-3.
Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)4-7, which is used in the clinic to treat epilepsy8. Retigabine (0.1 to 10 µM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells5 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.46. Similar effects were seen with 10 µM retigabine in oocytes expressing the KV7.2/3 heteromeric channel7.
Alomone Labs Retigabine activates KCNQ2/KCNQ3 channels in HEK 293 transfected cells.A. Retigabine (#R-100) activates KCNQ2/KCNQ3 channels in a concentration-dependent manner. B. Increasing concentrations of Retigabine causes a gradual hyperpolarization shift. C. Concentration-effect curve plotted as the shift in the voltage dependence of activation normalized, as a function of the concentration of Retigabine.
Adapted from Stas, J.I. et al. (2016) Sci. Rep. 6, 35080. with permission of NATURE SPRINGER.
Retigabine (#R-100) is a highly pure, synthetic, and biologically active compound.
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- Brueggemann, L.I. et al. (2018) Int. J. Mol. Sci. 19, 2223.
- Ghezzi, F. et al. (2018) J. Physiol. 596, 2611.
- Hu, W. and Bean, B.P. (2018) Neuron 97, 1315.
- Paz, R.M. et al. (2018) Neuropharmacology 137, 309.
- Tirko, N.N. et al. (2018) Neuron 100, 593.
- Vanhoof-Villalba, S.L. et al. (2018) Epilepsia 59, 358.
- Ghezzi, F. et al. (2017) Neuroscience 340, 62.
- Greene, D.L. et al. (2017) J. Pharmacol. Exp. Ther. 362, 177.
- Kang, S. et al. (2017) Neuropsychopharmacology 42, 1813.
- Krukowski, K. et al. (2017) Pain 158, 1126.
- Laumet, G. et al. (2017) Brain Behav. Immun. 66, 94.
- Lee, C. et al. (2017) J. Neurophysiol. 118, 2991.
- Nassoiy, S.P. et al. (2017) J. Biomed. Sci. 24, 8.
- Rubi, L. et al. (2017) Toxicol. Appl. Pharmacol. 329, 309.
- Corbin-Leftwich, A. et al. (2016) J. Gen. Physiol. 147, 229.
- Kim, K.S. et al. (2016) Biophys. J. 110, 1089.
- Stas, J.I. et al. (2016) Sci. Rep. 6, 35080.
- Liu, C. et al. (2015) Proc. Natl. Acad. Sci. U.S.A. 112, 14723.
- Sheppard, A.M. et al. (2015) Hear. Res. 327, 1.
- Sobieski, C. et al. (2015) J. Neurosci. 35, 11105.
- Treven, M. et al. (2015) Epilepsia 56, 647.
- Mateos-Aparicio, P. et al. (2014) J. Physiol. 592, 669.
- Nigro, M. et al. (2014) J. Neurosci. 34, 6807.
- Qi, Y. et al. (2014) Neuron 83, 1159.
- Vetter, I. et al. (2013) J. Neurosci. 33, 16627.
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