Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2.

ABSTRACT:

Background and purpose

APETx2, a toxin from the sea anemone Anthropleura elegantissima, inhibits acid-sensing ion channel 3 (ASIC3)-containing homo- and heterotrimeric channels with IC(50) values < 100 nM and 0.1-2 µM respectively. ASIC3 channels mediate acute acid-induced and inflammatory pain response and APETx2 has been used as a selective pharmacological tool in animal studies. Toxins from sea anemones also modulate voltage-gated Na(+) channel (Na(v) ) function. Here we tested the effects of APETx2 on Na(v) function in sensory neurones.

Experimental approach

Effects of APETx2 on Na(v) function were studied in rat dorsal root ganglion (DRG) neurones by whole-cell patch clamp.

Key results

APETx2 inhibited the tetrodotoxin (TTX)-resistant Na(v) 1.8 currents of DRG ne

SUBMITTER: Blanchard MG 

PROVIDER: S-EPMC3413854 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature