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 1Kβ-Pompilidotoxin 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 200 µM 1Kβ-Pompilidotoxin (#P-182) 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 200 µM 1Kβ-PMTX (as indicated).
Alomone Labs 1Kβ-Pompilidotoxin enhances NaV1.6 currents heterologously expressed in Xenopus oocytes.NaV1.6 currents were elicited by a 100 ms voltage step from a holding potential of -100 mV to 0 mV applied every 10 sec, using two electrode voltage clamp. A. Time course, showing the effect of 20 µM, 50 µM and 100 µM 1Κβ-Pompilidotoxin (#P-182) application (horizontal bars) on current area. B. Superimposed traces of NaV1.6 current under control conditions and after 2 min perfusion with 20 µM, 50 µM and 100 µM 1Κβ-Pompilidotoxin (as indicated).
1Kβ-PMTX is a mutated form of the β-PMTX (#P-180), originally isolated from the solitary wasp (Batozonellus maculifrons) venom and is a synthetic version of the peptide1. Pompilidotoxins (PMTX, α and β) are small peptides consisting of 13 amino acids.
β-PMTX induces a unique pattern of repetitive action potentials previous seen with other neurotoxins and thus facilitates 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. It is effective at concentrations of 10 nM in cultured rat cortical neurons5.
1Kβ-PMTX is mutated at position 1 with Arginine to Lysine transition, which enhances its activity on voltage-gated human Nav1.6 Na+ channels relative to native β-PMTX1,3.
