- Alomone Labs GTx1-15 inhibits rat NaV1.3 channels heterologously expressed in HEK-293 cells.A. Dose-response of NaV1.3 channel inhibition by GTx1-15 (#STT-300). The inhibition was measured in 3-5 cells for each dose. B. Example of superimposed current traces of rat NaV1.3 channel activity before and during application of 0.3 µM of GTx1-15. Holding potential was -100 mV and currents were stimulated every 10 seconds by a voltage ramp of 40 msec from holding potential to +60 mV.
GTx1-15 is isolated from the Grammostola rosea (Phrixotrichus auratus) spider venom and is a synthetic version of the peptide1,2.
GTx1-15 inhibits voltage-gated rat NaV1.3 and NaV1.7 Na+ channels, as well as T-type Ca2+ channels1,2.
Voltage-gated Na+ channels (VGSC, NaV) play a critical role in excitability of nociceptors (pain-sensing neurons).
The peripheral-specific Na+ channels NaV1.7, NaV1.8 and NaV1.9 are particularly important in the pathophysiology of different pain syndromes and hence, thought to be potential targets for pain therapeutics3-4. The expression and functional properties of NaV channels in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation5.