Overview
- Brueggemann, L.I. et al. (2012) Am. J. Physiol. 302, L120.
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.
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.
