143994-93-8Relevant articles and documents
Synthesis of the Photoaffinity-labeled Grayanotoxins for Studying the Gating Mechanism of Na Channel
Iwasa, Junkichi,Kamano, Hideki,Tsuji, Katsuo,Seyama, Issei,Baba, Naomichi,Nakajima, Shuhei
, p. 1169 - 1171 (2007/10/02)
Grayanotoxin loosely binds to the neurotoxin receptor site 2 on Na channels. 14R-N-benzyliminograyanotoxane-3β,5,6β,16-tetraol (4) and 17-N-benzyliminograyanotox-15-ene-3β,5,6β,14R-tetraol (5) were synthesized and applied intracellularly to squid axons.On UV irradiation, their membrane potential produced by a dose of 4 or 5 rose to higher level than that in the dark.However, in the case of 5, even when the axons were internally perfused with toxin-free solution after the dose, the potential level didnot fall in contrast to 4.It suggested that 5 covalently bound to the receptor involved in the gating mechanism of Na channels.