TABLE 1

Summary of fractional block and IC50 values for block by vernakalant of wild-type and mutant Kv1.5 channels Fractional block was measured at 10 μM vernakalant. Values are expressed as mean ± S.E.M.

Fractional Block
Significance
n
IC50
Hill Coefficient
-Fold change
n
μM
WT 0.45 ± 0.03 23 13.35 ± 0.93 1.00 5–23
T479A 0.77 ± 0.05 P < 0.01 9 1.63 ± 0.09 0.6 8.31 5–10
T479S 0.23 ± 0.04 P < 0.01 7 41.02 ± 3.54 0.95 3.07 3–8
T480A 0.23 ± 0.04 P < 0.01 12 52.59 ± 7.85 0.88 3.94 3–12
T480S 0.25 ± 0.07 P < 0.05 6 52.83 ± 12.46 0.64 3.96 4–7
V481L 0.36 ± 0.03 6
C500A 0.21 ± 0.04 P < 0.01 10 45.63 ± 4.06 0.95 3.42 3–10
A501V 0.69 ± 0.04 P < 0.01 8 3.49 ± 0.19 0.85 3.81 4–8
I502A 0.07 ± 0.03 P < 0.01 9 329.26 ± 18.97 0.65 24.66 4–10
I502L 0.33 ± 0.07 6 24.84 ± 3.14 0.96 1.86 3–6
I502F 0.10 ± 0.01 P < 0.01 4 149.29 ± 8.36 0.84 11.11 4
I502K D.N.E. 6
I502D D.N.E. 5
V505A 0.21 ± 0.04 P < 0.01 10 45.54 ± 2.56 0.95 3.41 3–10
V505L 0.22 ± 0.07 P < 0.05 4 57.70 ± 4.63 0.77 4.32 3–5
V505F 0.27 ± 0.05 P < 0.05 6 28.79 ± 0.79 0.96 2.16 5–6
V505K D.N.E. 5
V505D D.N.E. 5
I508A 0.21 ± 0.03 P < 0.01 8 42.44 ± 0.94 0.87 3.18 3–8
I508L 0.38 ± 0.05 4 16.84 ± 0.48 1.00 1.26 3–4
I508Y 0.21 ± 0.03 P < 0.01 7 24.70 ± 0.63 1.46 1.85 4–7
I508F 0.94 ± 0.02 P < 0.01 5 0.61 ± 0.03 1.23 21.80 4–8
I508K D.N.E. 5
I508D D.N.E. 5
A509G 0.33 ± 0.07 9
A509V D.N.E. 12
V512L 0.56 ± 0.04 9
P532L
0.26 ± 0.03
P < 0.01
16
32.02 ± 1.83
0.96
2.40
3–16

  • D.N.E., did not express