Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of
saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided.
Saxitoxin (STX), gonyautoxin (GTX), and zetekitoxin, and variant STX compounds bind to
sodium channels and are effective to reduce or block flow of
sodium ions through such channels. Such channel block affects nerve and
muscle action, and may be effective to reduce or block
pain sensations, relax muscles, reduce
muscle spasm, and reduce wrinkles. STX analogue binding to
sodium channels may also be useful to locate, image, or mark sodium channels, and so be useful in studying sodium channels and
sodium channel disorders, and in the diagnosis and treatment of patients suffering from
sodium channel disorders. In embodiments, the variant STX compounds include conjugates having increased serum half-life as compared to STX when administered to a subject. In embodiments, the present disclosure provides a method for alleviating pain in a subject in need of treatment, the method comprising administering to the subject an effective amount of a
saxitoxin analogue compound, or a pharmaceutically acceptable salt, isomer,
tautomer or
prodrug thereof, whereby pain in said subject is alleviated.