Table 2.
Schild analysis for the antagonism of 5-CT-stimulated cAMP signaling by MEL-9 and LP-211 in HEK-hu5-HT7 cells
| MEL-9 | LP-211 | |||
|---|---|---|---|---|
| [Compound] | 5-CT EC50 (nmol/L) | 5-CT Emax (% reduction) | 5-CT EC50 (nmol/L) | 5-CT Emax (% reduction) |
| Control (no compound) | 13.34 ± 3.00 | 0 | 13.34 ± 3.00 | 0 |
| 10 nmol/L | 13.67 ± 1.70 | 37.10 ± 0.47* | 12.24 ± 5.75 | 58.97 ± 16.42** |
| 100 nmol/L | 48.21 ± 6.40 | 96.02 ± 2.15** | 134.7 ± 17.2 | 89.17 ± 7.31** |
| 1 μmol/L | n.d. | 101.6 ± 3.14** | n.d. | 93.17 ± 3.87** |
The table shows the EC50 of 5-CT and the percent reduction in Emax for each concentration of the compounds studied. Data are the mean values ± SEM from three independent experiments performed in duplicate. (*P < 0.05, **P < 0.01, relative to control; One-way ANOVA and Dunnett's Multiple Comparison Test). n.d., not determined; MEL-9, N-benzyl-4-(2-diphenyl)-1-piperazinehexanamide; LP-211, N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide; 5-CT, 5-carboxamidotryptamine; Emax, maximal response.