- Alomone Labs α-Conotoxin PeIA inhibits α3/β2 nAChR heterologously expressed in Xenopus oocytes.A. Time course of α-Conotoxin PeIA (#STC-970) action on α3/β2 nAChR. Current amplitude were plotted as a function of time. Membrane potential was held at -80 mV and oocytes were stimulated by exposing them to 100 µM acetylcholine (Ach) every 100 sec. 50 nM (for 300 sec), 100 nM (for 300 sec) and 200 nM (for 200 sec) α-Conotoxin PeIA were perfused during the period marked by the bar. B. Superimposed traces of α3/β2 nAChR channel current in the absence (black) and presence of different concentrations of α-Conotoxin PeIA (taken from experiment in A).
α-Conotoxin PeIA is a peptide toxin originally isolated from the Conus pergrandis (Grand cone) venom1. This toxin belongs to the α-Conotoxin family which acts on the postsynaptic membrane by binding and inhibiting nicotinic acetylcholine receptors (nAChR)1.
It potently and reversibly blocks α9/α10 nAChR (IC50 = 6.9 nM) and α3/β2 (IC50 = 23 nM) and discriminates between rat α9/α10 and α7 nACh recetors1. It also inhibits N-type Ca2+ channels (CaV2.2) (IC50 = 1.1 nM) via the activation of the GABA(B) G-protein coupled receptor in DRG neurons2.