| Description | Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator. Brevetoxin-3 has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels. |
| In vitro | Brevetoxin-3 (30-500 nM) produces a shift in activation to more negative membrane potentials whereby single-channel activity is observed under steady-state conditions (maintained depolarization at -50 mV) [1]. |
| In vivo | Brevetoxin-3 (intratracheal instillation; 2.8 μg/kg; gestational days 15-18) radioactivity is detected in placentas and fetuses within 0.5 hours. Concentrations of brevetoxin equivalents in fetuses are approximately 0.3 ng/g throughout the 48-h post-dosing, resulting in a calculated dose to fetuses of 19 ng/gh [3]. |
| Target activity | Na+-ATPase: |
| Synonyms | PbTx-3 |
| molecular weight | 897.112 |
| Molecular formula | C50H72O14 |
| CAS | 85079-48-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Jeglitsch G,et al. Brevetoxin-3 (PbTx-3) and its derivatives modulate single tetrodotoxin-sensitive sodium channels in rat sensory neurons.J Pharmacol Exp Ther. 1998 Feb;284(2):516-25. 2. Zaias J,et al. Repeated exposure to aerosolized brevetoxin-3 induces prolonged airway hyperresponsiveness and lung inflammation in sheep.Inhal Toxicol. 2011 Mar;23(4):205-11. 3. Benson JM, et al. Placental transport of brevetoxin-3 in CD-1 mice.Toxicon. 2006 Dec 15;48(8):1018-26. Epub 2006 Aug 18. |