Batrachotoxins as Unique Activators of Sodium Channels


Natural products provide a wide range of biologically active agents, many of which have unique pharmacological activity and therapeutic potential. The present invention relates to the identification and characterization of two alkaloids, namely, 'batrachotoxin' and 'homobatrachotoxin,' isolated from extracts of amphibian skin. Biologically, both these agents are potent activators of sodium channels. The sodium channels are primarily expressed in peripheral nerve cells in pain pathways, where they regulate cellular excitability. Thus, these channels are drug targets for the treatment of pain and/or peripheral neuropathies. The use of batrachotoxin or homobatrachotoxin as research tools is applicable to sodium channel studies related to the effects of local anesthetics, analgesics, antiarrythmics and anticonvulsants. Further, advancement of these studies and target validation present commercial opportunities to expand ion channel drug discovery into new therapeutic areas.

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Updated: Sep 1, 2001