Table 6.
Efficacy and potency of F15599 and comparators for stimulation of [35S]-GTPγS binding to Gαi and Gαo subunits
| Tissue/cell line |
F15599 |
F13714 |
(+)8-OH-DPAT |
5-HT |
||||
|---|---|---|---|---|---|---|---|---|
| Emax (%) | pEC50 | Emax (%) | pEC50 | Emax (%) | pEC50 | Emax (%) | pEC50 | |
| Gαi (HeLa-h5-HT1A membranes) | 122 ± 8 | 6.96 ± 0.08 | 111 ± 6 | 9.15 ± 0.08 | 90 ± 8 | 7.79 ± 0.13 | 100 ± 1 | 7.63 ± 0.04 |
| Gαo (hippocampus) | 103 ± 8 | 6.07 ± 0.06 | 83 ± 6 | 9.11 ± 0.16 | 82 ± 4 | 7.37 ± 0.06 | 100 ± 1 | 7.18 ± 0.07 |
Efficacy (Emax) values are expressed as % of the stimulation induced by saturating concentrations (10 µmol·L−1) of 5-HT.