Table 3.
Secondary in vitro pharmacological properties of GSK1440115 and GSK1562590 (potency determination)
| Potency | Selectivity relative to human UT pKi | |||
|---|---|---|---|---|
| Recombinant human receptor target | GSK1440115 | GSK1562590 | GSK1440115 | GSK1562590 |
| D2S (pKi) | – | 7.02 ± 0.03 (n= 3) | – | 194 |
| κ opioid (pEC50) | 5.63 ± 0.27 (n= 7) | 6.94 ± 0.05 (n= 9) | 2113 | 242 |
| 5-HT1A (pKi) | – | 6.83 ± 0.03 (n= 3) | – | 444 |
| NK2 (pKi) | – | 5.71 ± 0.25 (n= 2) | – | 356 |
| NK2 (pKb) | 5.31 ± 0.04 (n= 2) | 5.65 ± 0.08 (n= 2) | 1988 | 4596 |
GSK1440115 and GSK1562590 did not antagonize the κ opioid receptor (pKb < 5.12). Relative affinities/activities for GSK1440115 and GSK1562590 are expressed relative to their respective human UT pKi values. All values are expressed as mean ± SEM.