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Retigabine

D-23129, Ezogabine, Trobalt®, Potiga®

A Potent and Selective Modulator of KCNQ Channels

Cat #: R-100
Alternative Name D-23129, Ezogabine, Trobalt®, Potiga®
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 303.3
    Purity: >99% (HPLC)
    Effective concentration 0.1-100 µM.
    Structure
    Chemical name Ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate.
    Molecular formula C16H18FN3O2.
    CAS No.: 150812-12-7
    Activity Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1-4, which is used in the clinic to treat epilepsy5. Retigabine (0.1 to 10 μM) induced a K+ current and hyperpolarized CHO cells expressing KV7.2/3 cells2 as well as other channels in the following order: KV7.3 > KV7.2/3 > KV7.2 > KV7.43. Similar effects were seen with 10 μM retigabine in oocytes expressing the KV7.2/3 heteromeric channel4.
    References-Activity
    1. Rundfeldt, C. (1997) Eur. J. Pharmacol. 336, 243.
    2. Wickenden, A.D. et al. (2000) Mol. Pharmacol. 58, 591.
    3. Tatulian, L. et al. (2000) J. Neurosci. 21, 5535.
    4. Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.
    5. Brodie, M.J. et al. (2010) Neurology  75, 1817.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Retigabine enhances KCNQ2/3 (KV7.2/7.3) currents in Xenopus oocytes.
      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.
    References - Scientific background
    1. Kullmann, D.M. (2002) J. Mol. Brain 125, 1117.
    2. Robbins, J. (2001) Pharmacol. Ther. 90, 1.
    3. Wang, H.S. et al. (1998) Science 282, 1890.
    4. Rundfeldt, C. (1997) Eur. J. Pharmacol. 336, 243.
    5. Wickenden, A.D. et al. (2000) Mol. Pharmacol. 58, 591.
    6. Tatulian, L. et al. (2000) J. Neurosci. 21, 5535.
    7. Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.
    8. Brodie, M.J. et al. (2010) Neurology  75, 1817.
    Scientific background

    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.

    Target KCNQ2, KCNQ3, and KCNQ4 K+ channels
    Lyophilized Powder
    Image & Title

    Retigabine
    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.

    Last update: 21/10/2021

    Retigabine (#R-100) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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    Citations

    Citations
    Product citations
    1. Brueggemann, L.I. et al. (2018) Int. J. Mol. Sci. 19, 2223.
    2. Ghezzi, F. et al. (2018) J. Physiol. 596, 2611.
    3. Hu, W. and Bean, B.P. (2018) Neuron 97, 1315.
    4. Paz, R.M. et al. (2018) Neuropharmacology 137, 309.
    5. Tirko, N.N. et al. (2018) Neuron 100, 593.
    6. Vanhoof-Villalba, S.L. et al. (2018) Epilepsia 59, 358.
    7. Ghezzi, F. et al. (2017) Neuroscience 340, 62.
    8. Greene, D.L. et al. (2017) J. Pharmacol. Exp. Ther. 362, 177.
    9. Kang, S. et al. (2017) Neuropsychopharmacology 42, 1813.
    10. Krukowski, K. et al. (2017) Pain 158, 1126.
    11. Laumet, G. et al. (2017) Brain Behav. Immun. 66, 94.
    12. Lee, C. et al. (2017) J. Neurophysiol. 118, 2991.
    13. Nassoiy, S.P. et al. (2017) J. Biomed. Sci. 24, 8.
    14. Rubi, L. et al. (2017) Toxicol. Appl. Pharmacol. 329, 309.
    15. Corbin-Leftwich, A. et al. (2016) J. Gen. Physiol. 147, 229.
    16. Kim, K.S. et al. (2016) Biophys. J. 110, 1089.
    17. Stas, J.I. et al. (2016) Sci. Rep. 6, 35080.
    18. Liu, C. et al. (2015) Proc. Natl. Acad. Sci. U.S.A. 112, 14723.
    19. Sheppard, A.M. et al. (2015) Hear. Res. 327, 1.
    20. Sobieski, C. et al. (2015) J. Neurosci. 35, 11105.
    21. Treven, M. et al. (2015) Epilepsia 56, 647.
    22. Mateos-Aparicio, P. et al. (2014) J. Physiol. 592, 669.
    23. Nigro, M. et al. (2014) J. Neurosci. 34, 6807.
    24. Qi, Y. et al. (2014) Neuron 83, 1159.
    25. Vetter, I. et al. (2013) J. Neurosci. 33, 16627.

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