Maleimide Conjugates of Saxitoxin as Covalent Inhibitors of Voltage-Gated Sodium Channels

(+)-Saxitoxin, a naturally occurring guanidinium poison, functions as a potent, selective, and reversible inhibitor of voltage-gated sodium ion channels (NaVs). Modified forms of this toxin bearing cysteine-reactive maleimide groups are available through total synthesis and are found to irreversibly...

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Veröffentlicht in:	Journal of the American Chemical Society 2013-07, Vol.135 (29), p.10582-10585
Hauptverfasser:	Parsons, William H, Du Bois, J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CHO Cells Cricetulus Humans Maleimides - chemistry Maleimides - pharmacology Models, Molecular Neurons - drug effects Rats Saxitoxin - chemistry Saxitoxin - pharmacology Sodium Channel Blockers - chemistry Sodium Channel Blockers - pharmacology Sodium Channels - metabolism
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