Table 1. Potency and maximum effect values of Kv7 channel modulators on spontaneous phasic and tonic contractions of guinea pig DSM isolated strips.
Compound | Amplitude | Muscle Force | Frequency | Duration | Muscle Tone |
---|---|---|---|---|---|
IC50/EC50: Mean (95% Confidence Interval) | |||||
Maximum Efficacy: Mean ± SEM | |||||
L-364373 | 4.8 (2.0-11.7)µM | 4.1 (1.2-13.9)µM | 53.5 (6.0-480.4)µM | >100µM | 22.4 (4.0-126.9)µM |
16.0±6.8%### | 13.2±6.0%### | 46.4±12.2%## | 46.8±12.7%## | 54.4±7.7%## | |
Retigabine | 2.3 (1.4–3.5)µM | 2.1 (1.3–3.4)µM | 14.0 (4.3–46.1)µM | 8.7 (5.6-13.4)µM | 3.5 (0.1–17.3)µM |
0.7±0.7%### | 0.2±0.2%### | 11.2±11.2%### | 0.4±0.4%### | 76.4±14.9%$ | |
XE991 | 4.5 (0.4–54.6)µM | 2.3 (0.1–49.3)µM | — | — | — |
212.9±42.2%# | 233.3±66.2%# | 101.0±11.5% | 115.7±15.3% | 139.9±54.0% | |
Linopiridine | 11.5 (1.0–127.0)µM | 10.7 (0.9-132.5)µM | — | — | — |
415.1±75.9%## | 415.1±110.4%# | 90.7±15.0% | 126.8±21.5% | 140.0±11.4%## |
Maximum effects are reported in comparison to control (taken to be 100%). Each data point is n=7-8, N=4-6; #P<0.05, ##P<0.01, ###P<0.001, $P=0.07 vs. control.