Potent Nav1.7 blocker; analgesic
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Potent Nav1.7 blocker (IC50 = 2.5 nM). Also inhibits Nav1.1, Nav1.2, Nav1.3 and Nav1.6 in the nanomolar range. Exhibits no effects on Cav channels or nAChR at 5 μM. Demonstrates analgesic activity in vivo; antagonizes effects of scorpion-venom toxin OD1 at Nav1.7.
Cardoso et al (2015) Identification and characterization of ProTx-III [μ-TRTX-Tp1a], a new voltage-gated sodium channel inhibitor from venom of the tarantula thrixopelma pruriens. Mol.Pharmacol. 88 291 PMID:25979003
5-Iodo-A-85380 dihydrochloride
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