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Lkt Laboratories CAS 79580-28-2, ≥95%, Polyether neurotoxin found in Karenia brevis; Nav1.4/1.5 Na+ channel activator.

Supplier: Lkt Laboratories B6917

Brevetoxins are lipid-soluble polyether neurotoxins initially produced by the dinoflagellate Karenia brevis. Brevetoxins act as agonists, binding the neurotoxin site 5 on SCN4A/Nav1.4 and SCN5A/Nav1.5 voltage-gated Na+ channels in skeletal muscle and cardiac tissue, producing a channel opening effect; this activity results in bronchoconstriction and airway inflammation in vivo. Stimulation of the voltage-gated Na+ channels also induces NMDA receptor-mediated release of L-glutamate and L-aspartate in neurons. Activity at these channels also activates Pyk2 and Src, inducing downstream signaling cascades. Brevetoxin 2 forms DNA adducts with cytidine in isolated lung cells and with adenosine and guanosine in vivo, indicating carcinogenic activity.
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