1fyg

Structural highlights

Function

O16O3_CONST Omega-conotoxins act at presynaptic membranes, they bind and block voltage-gated calcium channels (Cav). This peptide selectively targets Cav2.2/CACNA1B (IC(50)=160 nM) voltage-gated calcium channels (PubMed:26344359). When tested in mammals, this toxin displays an analgesic potency similar to MVIIA in a range of acute and chronic pain models in rodents, but has less adverse effects (tremor, diminution of spontaneous locomotor activity and bad coordinated locomotion) compared with identical dosages of MVIIA injected intrathecally.^{[1] [2]}

References

1. ↑ Wen L, Yang S, Qiao H, Liu Z, Zhou W, Zhang Y, Huang P. SO-3, a new O-superfamily conopeptide derived from Conus striatus, selectively inhibits N-type calcium currents in cultured hippocampal neurons. Br J Pharmacol. 2005 Jul;145(6):728-39. PMID:15880145 doi:http://dx.doi.org/0706223
2. ↑ Wang F, Yan Z, Liu Z, Wang S, Wu Q, Yu S, Ding J, Dai Q. Molecular basis of toxicity of N-type calcium channel inhibitor MVIIA. Neuropharmacology. 2016 Feb;101:137-45. PMID:26344359 doi:10.1016/j.neuropharm.2015.08.047