IC50 and maximal efficacy values for the effects of ML213 on spontaneous phasic, KCl-induced (20 mM), CCh-induced (0.1 or 1 µM), and EFS-induced (10 or 20 Hz) phasic contractions in guinea pig DSM isolated strips
IC50 values are presented as the mean (95% confidence interval). Maximal efficacy is presented as the mean ± S.E.M. and is normalized to the control on a scale from 100% to 0% (full relaxation); n/a=not applicable (negligible effect on parameter).
| Condition | Amplitude | Muscle Force | Duration | Frequency | n/N |
|---|---|---|---|---|---|
| Spontaneous phasic contractions | 1.1 (0.5–2.4) μM; 95.6% ± 4.4% | 0.7 (0.2–2.8) μM; 96.8% ± 3.2% | 1.6 (0.8–2.9) μM; 91.6% ± 8.41% | 3.9 (0.8–20.3) μM; 85.4% ± 14.6% | 6/6 |
| KCl (20 mM)-induced contractions | 2.7 (1.4–5.1) μM; 99.2% ± 0.8% | 2.5 (1.2–5.3) μM; 99.1% ± 0.9% | 3.9 (1.9–8.2) μM; 90.3% ± 9.7% | n/a; 87.6% ± 8.2% | 7/7 |
| CCh (0.1 μM)-induced contractions | 3.5 (1.9–6.4) μM; 100% inhibition | 2.1 (1.1–3.9) μM; 100% inhibition | 3.0 (1.8–5.3) μM; 99.7% ± 0.29% | n/a; 100% inhibition | 6/6 |
| CCh (1 μM)-induced contractions | 6.2 (1.2–30.7) μM; 84% ± 9.1% | 4.4 (0.8–22.3) (micro)M; 92.1% ± 4.2% | 11.3 (2.1–61.2) (micro)M; 68% ± 9.5% | n/a; 47.1% ± 15.4% | 6/6 |
| 10-Hz EFS-induced contractions | 2.2 (1.3–3.7) μM; 83.6% ± 7.6% | 2.3 (1.3–4.1) μM; 83.9% ± 8.2% | n/a; 32.78% ± 13.5% | n/a | 7/6 |
| 20-Hz EFS-induced contractions | 5.1 (3.1–8.2) μM; 86.9% ± 6.4% | 4.7 (2.7–8.1) μM; 89.1% ± 6.0% | n/a; 37.46% ± 9.3% | n/a | 6/6 |