TABLE 2

IC50 values for steady state PAA block of hKv1.3 (H399T) and hKv1.3 (H399T/A413C) currents

All values were obtained from at least four independent experiments and are given as mean ± S.D.

PAA hKv1.3 (H399T) hKv1.3 (A413C/H399T)
μM
(±)-Verapamil 2.4 ± 0.2 267 ± 22
(-)-Verapamil 1.2 ± 0.2 258 ± 24
(+)-Verapamil 4.3 ± 0.5 356 ± 47
(-)-Devapamil 0.7 ± 0.1 66 ± 8
(±)-Emopamil 2.0 ± 0.2 25 ± 2a
(±)-Gallopamil 3.4 ± 0.4 314 ± 29
(±)-Norverapamil 1.5 ± 0.3 228 ± 25
(±)-Acyanoverapamil 1.9 ± 0.2 246 ± 34
  • a Hill coefficient = 2.