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The poison Dart frog's batrachotoxin modulates Na v 1.8
Author(s) -
Bosmans Frank,
Maertens Chantal,
Verdonck Fons,
Tytgat Jan
Publication year - 2004
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2004.10.017
Subject(s) - batrachotoxin , sodium channel , chemistry , biophysics , ion channel , depolarization , membrane potential , aconitine , sodium , biochemistry , biology , receptor , organic chemistry , chromatography
Batrachotoxin is a potent modulator of voltage‐gated sodium channels, leading to irreversible depolarisation of nerves and muscles, fibrillation, arrhythmias and eventually cardiac failure. Since its discovery, field researchers also reported numbness after their skin came into contact with this toxin. Intrigued by this phenomenon, we determined the effect of batrachotoxin on the voltage‐gated sodium channel Na v 1.8, which is considered to be a key player in nociception. As a result, we discovered that batrachotoxin profoundly modulates this channel: the inactivation process is severely altered, the voltage‐dependence of activation is shifted towards more hyperpolarised potentials resulting in the opening of Na v 1.8 at more negative membrane potentials and the ion selectivity is modified.