TABLE 3.
Dissociation kinetics of [3H]VU6013720 induced by multiple ligands
Dissociation was performed by adding 10 μM of atropine, VU6013719, or VU0467154 at designated times. Data were fit with both one- and two-phase decay curves. For atropine and VU6013719, two-site fits were the preferred model; for VU0467154, a one-site model was preferred. *P < 0.05, **P < 0.01, ***P < 0.001 between atropine and VU6013719.
| % Fast | Koff fast (min−1) |
Koff slow (min−1) |
Half-life fast (min) | Half-life slow (min) | Plateau | R2 | |
|---|---|---|---|---|---|---|---|
| Atropine | 51 ± 5 | 0.56 ± 0.39 | 0.05 ± 0.01 | 1.6 ± 0.9 | 15 ± 3 | 1.0 ± 0.7 | 0.98 ± 0.02 |
| VU6013719 | 44 ± 8 | 2.0 ± 0.5* | 0.17 ± 0.02*** | 0.40 ± 0.10 | 4.2 ± 0.5** | −2.2 ± 3.2 | 0.98 ± 0.01 |
| Koff (min−1) | Half-life (min) | Plateau | R2 | ||||
|---|---|---|---|---|---|---|---|
| VU0467154 | 0.60 ± 0.18 | 1.2 ± 0.3 | 58 ± 5 | 0.84 ± 0.05 |
Koff, dissociation off rate.