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Vol. 280, Issue 2, 521-526, 1997
Institut National de la Santé et de la Recherche
Médicale U374, Institut Jean Roche, Faculté de
Médecine, F13916 Marseille, Cedex 20 France (C.P., E.C., B.D.,
F.C.) and
Roussel-Uclaf, 93230 Romainville, France (D.G.)
Genistein, an isoflavone inhibitor of tyrosine-specific protein
kinases, was shown to specifically block the
22Na+ influx through voltage-sensitive
Na+ channels in cultured rat brain neurons, whereas other
tyrosine kinase antagonists such as lavendustin A, compound 5, tyrphostin A47 and an erbstatin analog were inactive at
concentrations known to block kinase activity in other neuronal
systems. Dose-response curves for genistein indicated a half-maximum
effect at 60 µM. Daidzein, an inactive analog of genistein, had a
similar inhibitory effect on the 22Na+ influx
with a half-maximum effect at 195 µM. The time course of genistein
action was rapid, because maximum effect on
22Na+ influx was obtained in less than 20 s at 100 µM. Analysis of Na+ currents by the whole-cell
recording technique showed that 20 µM genistein reduced the sodium
current and shifted the voltage dependence of both activation and
inactivation curves. No competition with [3H]saxitoxin
binding was observed, whereas the binding of
[3H]batrachotoxinin A 20-
-benzoate to rat brain
synaptosomal membranes was partially inhibited, which suggested a
direct or allosteric interaction with neurotoxin binding site 2. These
data taken together clearly indicate that the inhibition of
voltage-sensitive sodium channels by genistein is not mediated by
tyrosine kinase inhibition.
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