Retigabine dihydrochloride

D-23129, Ezogabine, Trobalt®, Potiga®
A Potent and Selective Modulator of KCNQ Channels
    Cat #: R-101
    Alternative Name D-23129, Ezogabine, Trobalt®, Potiga®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 376.2
    Purity: >98%
    Effective concentration 0.1-100 µM
    Structure
    • Retigabine dihydrochloride
    Chemical name Ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate dihydrochloride.
    Molecular formula C16H20Cl2FN3O2.
    CAS No.: 150812-13-8.
    Activity Retigabine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1.
    References-Activity
    1. Main, M.J. et al. (2000) Mol. Pharmacol. 58, 253.
    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 Water. 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
    • Retigabine dihydrochloride
      Alomone Labs Retigabine dihydrochloride modulates KCNQ2/KCNQ3 voltage-gated K+ currents expressed in Xenopus oocytes.
      A. Time course of KCNQ2/KCNQ3 current enhancement by 10 and 100 µM Retigabine dihydrochloride (#R-101) as measured at -50 mV. Currents were elicited by application of voltage ramp from a holding potential of -100 mV to 0 mV (800 msec). B. Superimposed example traces of current responses before and during perfusion of 10 and 100 µM Retigabine dihydrochloride, as indicated.
    References - Scientific background
    1. Kullmann, D.M. (2002) 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. (2001) 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 5 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, KCNQ4 K+ channels
    Last update: 24/01/2020

    Retigabine dihydrochloride (#R-101) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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