Flupirtine Maleate

Katadolon®, Trancolong®, Awegal®, Efiret®, Trancopal Dolo®, Metanor®
A Potent and Selective Modulator of KCNQ Channels
Cat #: F-150
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 420.4
    Purity: >99.5%
    Effective concentration 1-100 µM.
    Structure
    Chemical name N-[2-Amino-6-[[4-fluorophenyl)methyl]amino]-3-pyridinyl]carbamic acid ethyl ester maleate.
    Molecular formula C15H17FN4O2●C4H4O4.
    CAS No.: 75507-68-5.
    Activity Flupirtine is a potent and selective KCNQ (KV7, M-) channel modulator (enhancer)1.
    References - Activity
    1. Brueggemann, L.I. et al. (2012) Am. J. Physiol. 302, L120.

    Storage before reconstitution 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.
    Reconstitution DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs Flupirtine Maleate modulates KCNQ2/KCNQ3 voltage-gated K+ currents expressed in  Xenopus oocytes.
    A. Time course of KCNQ2/KCNQ3 current enhancement by 10 and 100 µM Flupirtine Maleate (#F-150) 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 Flupirtine Maleate as indicated.
    References - Scientific Background
    1. Fleckenstein J. et al.  (2013) J. Transl. Med. 11, 34.
    2. Hadley, J.K. et al.  ) 2003) J. Neurosci. 23, 5012.
    3. Kornhuber, J. et al. (1999) J. Neural Transm. 106, 857.
    4. Singal, R. et al. (2012) Maedica 7, 163.
    Scientific background

    K+ channels (KCNQ/KV7) are expressed along myelinated and unmyelinated peripheral axons where their activation is expected to reduce axonal excitability1. Neurons express four KCNQ subunits that co-assemble to form either homo- or hetero-tetrameric voltage-gated channels2.

    Flupirtine maleate is a centrally-acting, non-opioid analgesic with N-methyl-D-aspartate (NMDA) receptor antagonist property. Flupirtine maleate is an analgesic with muscle-relaxing properties that activates KCNQ channels. Flupirtine maleate is as effective as opioids to settle the pain in post-surgical cases, cancer related, neuropathic and myofascial in origin. The analgesic effect of flupirtine maleate does not appear to be associated with any central opioid effect3. The clinical use of flupirtine maleate is more appropriate as it lacks the typical side effects of the opioid drugs4.

    Target KCNQ K+ channels
    Last update: 10/03/2019

    Flupirtine Maleate (#F-150) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use