Table 3.
Effect of UCB1244283 on the affinities of UCB30889 and LEV for sites labelled with [3H]UCB30889 on rat cortex and human recombinant SV2A expressed in HEK cells at 4°C and 37°C
| Rat cortex pKi ± SD | Human recombinant SV2A pKi ± SD | |||
|---|---|---|---|---|
| + UCB1244283 | + UCB1244283 | |||
| 4°C | ||||
| LEV | 5.75 ± 0.14 | 5.48 ± 0.10 | 5.47 ± 0.04 | 5.38 ± 0.03* |
| UCB30889 | 7.03 ± 0.06 | 7.36 ± 0.08*** | 6.85 ± 0.43 | 7.79 ± 0.05** |
| 37°C | ||||
| LEV | 5.32 ± 0.03 | 5.19 ± 0.04** | 5.16 ± 0.07 | 5.23 ± 0.03 |
| UCB30889 | 6.46 ± 0.16 | 7.07 ± 0.08*** | 6.37 ± 0.48 | 7.31 ± 0.05* |
Data are presented as mean ± SD (n = 3 to 6) and were obtained by analysis of competition curves as presented in Figure 4, using a non-linear regression model with variable slope as described in materials and methods. Hill slopes were not significantly different from unity. *P < 0.05, **P < 0.01, ***P < 0.001 (unpaired Student's t-test between condition with and without UCB1244283).