Table 4.
Efficacy and potency of F15599 and comparators for stimulation of signal transduction responses in cell lines stably expressing h5-HT1A receptors
| Efficacy model |
F15599 |
F13714 |
(+)8-OH-DPAT |
5-HT |
||||
|---|---|---|---|---|---|---|---|---|
| Emax (%) | pEC50 | Emax (%) | pEC50 | Emax (%) | pEC50 | Emax (%) | pEC50 | |
| Total G-proteina | 102 ± 3 | 6.97 ± 0.08 | 73 ± 14 | 9.02 ± 0.12 | 107 ± 3 | 7.17 ± 0.05 | 101 ± 9 | 7.32 ± 0.05 |
| cAMP inhibition | 95 ± 1 | 6.46 ± 0.10 | 100 ± 1 | 8.67 ± 0.02 | 99 ± 1 | 7.77 ± 0.38 | 100 ± 1 | 7.45 ± 0.18 |
| ERK1/2 phosphorylation | 102 ± 9 | 7.81 ± 0.13 | 108 ± 13 | 9.07 ± 0.11 | 100 ± 3b | 8.74 ± 0.06b | 95 ± 8b | 6.86 ± 0.09b |
| Receptor internalization | 93 ± 7 | 6.80 ± 0.04 | 92 ± 7 | 9.06 ± 0.16 | 101 ± 3 | 7.38 ± 0.02 | 108 ± 6c | 6.80 ± 0.12c |
Efficacy (Emax) values are expressed as % of the stimulation induced by saturating concentrations (10 µmol·L−1) of 5-HT.
a
‘Total’ G-protein activation refers to [35S]-GTPγS binding that does not distinguish between the G-protein subtypes involved: compare with data in Table 6 on Gαi and Gαo activation.