Table 2. Potency and maximum effect values of Kv7 channel modulators on 10 Hz EFS-induced contractions of guinea pig DSM isolated strips.
Compound | Amplitude | Muscle Force | Duration | Muscle Tone |
---|---|---|---|---|
IC50/EC50: Mean (95% Confidence Interval) | ||||
Maximum Efficacy: Mean±SEM | ||||
L-364373 | 23.1 (8.7–61.2)µM | 24.9 (7.3–84.3)µM | — | — |
28.0±6.0%### | 37.2±10.7%## | 106.7±8.7% | 79.5±14.1% | |
Retigabine | 9.7 (6.9–13.9)µM | 10.1 (6.7–15.1)µM | 40.6 (19.2–86.0)µM | — |
1.0±0.7%### | 0.3±0.2%### | 1.1±0.7%### | 96.7±16.6% | |
XE991 | 0.6 (0.1–5.6)µM | 1.4 (0.2–9.8)µM | — | 4.8 (0.3-76.6)µM |
155.3±16.4%## | 180.5±24.2%## | 104.8±5.2% | 132.9±7.0%## | |
Linopiridine | >30µM | 6.3 (0.5-79.0)µM | — | >30µM |
144.0±20.1%# | 130.1±13.1%# | 94.3±4.0% | 159.3±28.6%# |
Maximum effects are reported in comparison to control (taken to be 100%). Each data point is n=6-9, N=4-8; #P< 0.05, ##P< 0.01, ###P<0.001 vs control.