Kinetic binding parameters for association and dissociation of [3H]almorexant and [3H]Cp-1 in hOX1 and hOX2 membranes and of [3H]SB-674042 in the hOX1 membranes
The Kob, Koff, Kon, t½, and Kd values are mean ± S.E. calculated from three independent experiments (each performed in quadruplet) as described under Materials and Methods.
| Radioligand and Receptor | Association Kinetic | Dissociation Kinetic | Apparent Kd | |||
|---|---|---|---|---|---|---|
| Kob | Kon | t½ | Koff | t½ | ||
| min −1 | nM−1 · min−1 | min | min −1 | min | nM | |
| [3H]Almorexant (37°C) | ||||||
| hOX1 | 0.225 ± 0.02 | 0.051 ± 0.01 | 3.07 ± 0.23 | 0.140 ± 0.01 | 4.95 ± 0.22 | 2.73 ± 0.23 |
| hOX2 | 0.130 ± 0.01 | 0.064 ± 0.00 | 5.34 ± 0.37 | 0.007 ± 0.00 | 104.60 ± 4.56 | 0.10 ± 0.01 |
| [3H]Cp-1 (37°C) | ||||||
| hOX1 | 0.628 ± 0.03 | 0.024 ± 0.00 | 1.11 ± 0.04 | 0.550 ± 0.02 | 1.25 ± 0.04 | 22.66 ± 1.12 |
| hOX2 | 0.171 ± 0.01 | 0.047 ± 0.00 | 4.07 ± 0.15 | 0.027 ± 0.01 | 26.15 ± 3.43 | 0.56 ± 0.24 |
| [3H]SB-674042 (23°C) | ||||||
| hOX1 | 0.122 ± 0.01 | 0.033 ± 0.01 | 5.71 ± 0.61 | 0.022 ± 0.01 | 31.57 ± 3.0 | 0.66 ± 0.15 |