title: Synthesis and mode of action on axonal membranes of photoactivable derivatives of tetrodotoxin.
abstract: Two photoactivable derivatives of tetrodotoxin have been synthesized. Electrophysiological experiments on crab giant axons and competitive binding with [3H]-tetrodotoxin for the tetrodotoxin receptor indicate that they are only 4.5 to 7.5 times less active than tetrodotoxin itself. These compounds give a reversible block of the sodium channel in the dark but after ultraviolet irradiation they provoke an irreversible blockade of the channel.
mesh_terms: D000818:Animals; D001369:Axons / Q000378:metabolism*; D001667:Binding, Competitive; D003386:Brachyura; D002462:Cell Membrane / Q000378:metabolism; D007700:Kinetics; D011485:Protein Binding; D011955:Receptors, Drug / Q000378:metabolism; D013779:Tetrodotoxin / Q000378:metabolism / Q000528:radiation effects*; D014466:Ultraviolet Rays
chemical_list: D011955:Receptors, Drug; D013779:Tetrodotoxin