H. Sada et al., KINETIC MECHANISM OF NA-PIG VENTRICULAR MYOCYTES( CHANNEL DEPRESSION BY TAURINE IN GUINEA), Japanese Journal of Pharmacology, 71(2), 1996, pp. 147-159
To examine effects of taurine on the kinetics of the Na+ channel curre
nt (I-Na), action potentials and whole-cell Na+ currents were recorded
from single ventricular myocytes of guinea pigs. Kinetic parameters f
or the activation and inactivation of I-Na were determined in accordan
ce with the first-order kinetic model. Changes in the kinetic paramete
rs were assessed before and after taurine exposure (5-50 mM). While ta
urine at concentrations higher than 10 mM decreased the peak I-Na by c
a 15%, the agent did not alter the reversal potential and the maximum
Na+ conductance (G(Na)) Taurine shifted the steady-state inactivation
(h(infinity)) curve toward the negative potential direction and decrea
sed the slope of h(infinity). Concomitantly, the slope of the steady-s
tate activation (m(infinity)) was also slightly decreased and the rate
of inactivation in the large potential region (-40 to -30 mV) slightl
y increased, whereas the rate of the activation appeared to remain unc
hanged. It is suggested that taurine alters the surface charge of the
membrane and reduces the number of charges moving upon activation and
inactivation of channels, thereby reducing I-Na.