Overview
- Schiavon, E. et al. (2010) FEBS J. 277, 918.
- Sahara, Y. et al. (2000) Eur. J. Neurosci. 12, 1961.
- Konno, K. et al. (2000) Neurosci. Lett. 285, 29.
Alomone Labs 3R12Rα-PMTX enhances native NaV currents in ND7-23 cells.Native TTX-sensitive NaV currents in ND7-23 cells were elicited by a 50 ms voltage ramp from the holding potential of -100 mV to +60 mV, applied every 10 sec using whole-cell voltage clamp. A. Time course, showing the effect of 100 µM 3R12Rα-Pompilidotoxin (#P-176) application (horizontal bar) on current area, indicative of a toxin-dependent decrease in NaV currents inactivation. B. Superimposed traces of NaV currents in ND7-23 cells under control conditions and after 2 min perfusion with 100 µM 3R12Rα-Pompilidotoxin.
Pompilidotoxins (PMTX, α and β) are small peptides consisting of 13 amino acids.
α-PMTX (#P-170) induces a unique pattern of repetitive action potentials previous seen with other neurotoxins and thus facilitate both excitatory and inhibitory synaptic transmission.
Recently it was found that this toxin slows the Na+-channel inactivation, without changing the peak current-voltage relationship or the activation time course of the TTX-sensitive Na+ currents in the neuromuscular synapse of the lobster walking leg and in the rat trigeminal ganglion neurons2-4. Effective at concentrations of 10 nM in cultured rat cortical neurons5.
3R12Rα-Pompilidotoxin (3R12Rα-PMTX) is a mutated form of the α-PMTX, originally isolated from the solitary wasp (Anoplius samariensis) venom1 and is a synthetic version of the peptide.
3R12RKα-PMTX is mutated at position 3 as well as 12 with Lysine to Arginine transition, which enhanced its activity on voltage-gated Na+ channels 5-fold relative to α-PMTX1,3.
