Table 1

Parameters for inactivation kinetics of μ1 wild-type and mutant Na+ channels

ChannelControlControlR(+)-BupivacaineS(−)-Bupivacaine
V0.5kS′0.5kS′S′0.5kS′S′0.5kS′
mV
Wild-type−82.1  ± 1.45.4  ± 0.1−63.0  ± 2.512.7  ± 1.1−102.3  ± 0.57.6  ± 0.4−102.5  ± 0.67.9  ± 0.5
(n  = 10)(n  = 22)(n  = 11)(n  = 11)
N434A−69.5  ± 1.46.8  ± 0.4−71.4  ± 0.15.5  ± 0.9−97.9  ± 1.95.3  ± 1.7−94.9  ± 1.64.9  ± 1.3
(n  = 4)(n  = 21)(n  = 10)(n  = 11)
N434F−96.3  ± 1.86.3  ± 0.2−82.2  ± 0.711.7  ± 0.6−111.5  ± 2.76.8  ± 2.4−113.8  ± 4.37.1  ± 3.7
(n  = 11)(n  = 17)(n  = 4)(n  = 4)
N434W−98.2  ± 0.47.4  ± 0.3−74.4  ± 2.016.0  ± 1.2−115.7  ± 1.69.2  ± 1.5−115.5  ± 2.67.1  ± 2.3
(n  = 5)(n  = 9)(n  = 5)(n  = 4)
N434Y−114.2  ± 2.78.6  ± 0.1−36.6  ± 30.636.8  ± 8.7−133.5  ± 3.49.1  ± 2.7−139.0  ± 5.39.3  ± 3.7
(n  = 7)(n  = 8)(n  = 4)(n  = 4)
N434T−78.9  ± 1.27.3  ± 0.2−65.2  ± 0.36.2  ± 0.2−105.5  ± 2.38.5  ± 2.1−99.5  ± 1.97.8°1.7
(n  = 7)(n  = 11)(n  = 5)(n  = 6)
N434C−98.8  ± 1.96.4  ± 0.2−86.9  ± 0.39.7  ± 0.3−124.0  ± 7.56.8  ± 6.5−119.5  ± 5.74.2  ± 5.8
(n  = 10)(n  = 25)(n  = 11)(n  = 10)
N434D−87.3  ± 0.85.6  ± 0.4−53.3  ± 9.116.8  ± 2.7−110.9  ± 0.89.2  ± 0.7−111.6  ± 0.68.4  ± 0.5
(n  = 5)(n  = 20)(n  = 11)(n  = 9)
N434K−77.7  ± 1.37.0  ± 0.4−54.0  ± 6.614.4  ± 2.0−88.9  ± 1.15.9  ± 1.0−92.6  ± 1.67.3  ± 1.4
(n  = 9)(n  = 15)(n  = 8)(n  = 7)
N434R−83.3  ± 0.56.1  ± 0.1−62.6  ± 5.915.8  ± 2.5−97.1  ± 0.69.6  ± 0.5−92.2  ± 0.79.8  ± 0.6
(n  = 9)(n  = 16)(n  = 8)(n  = 8)

The values for the voltage dependence of fast inactivation V0.5and k (mean ± S.E., n = number of experiments) and the slow inactivation S′0.5 and ks′ (fitted values ± S.E.) in the absence and presence of 100 μM (μl wild-type, μl-N434A, μl-N434T, μl-N434D, μl-N434K, μl-N434R) or 10 μM (μl-N434C, μl-N434F, μl-N434Y, μl-N434W) bupivacaine enantiomers were determined as described in Fig. 2.