Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases peak currents at all voltages and stimulates a persistent Na+ current at hNav1.7 channel. Increases hyperpolarization at Nav1.4 and Nav1.6 channels. Induces spontaneous pain in vivo.
Durek et al (2013) Chemical engineering and structural and pharmacological characterization of the α-scorpion toxin OD1. ACS Chem.Biol. 8 1215 PMID:23527544 |Jalali et al (2005) OD1, the first toxin isolated from the venom of the scorpion Odonthobuthus doriae active on voltage-gated Na+ channels. FEBS Lett. 579 4181 PMID:16038905 |Maertens et al (2006) Potent modulation of the voltage-gated sodium channel Nav1.7 by OD1, a toxin from the scorpion Odonthobuthus doriae. Mol.Pharmacol. 70 405 PMID:16641312