Table 3.
Comparison of the binding kinetics of DPCPX in the absence or presence of 10 μM PD81,723 or BC-1 determined by radioligand association and dissociation assay or by the competition association assay
| kon (M−1·min−1) | koff (min−1) | |||
|---|---|---|---|---|
| k1a | k3b | k2a | k4b | |
| DPCPX | 1.2 ± 0.1 × 108 | 1.7 ± 0.4 × 108 | 0.23 ± 0.01 | 0.26 ± 0.01 |
| +10 μM PD81,723 | 1.4 ± 0.1 × 108 | 1.9 ± 0.4 × 108 | 0.23 ± 0.01 | 0.30 ± 0.07 |
| +10 μM BC-1 | 2.8 ± 0.2 × 108 | 2.7 ± 0.1 × 108 | 0.080 ± 0.004 | 0.072 ± 0.005 |
Values are means ± SEM of three separate experiments each performed in duplicate.
kon (k1) and koff (k2) of unlabelled DPCPX in the absence or presence of 10 μM PD81,723 or BC-1 were determined in [3H]-DPCPX (2.6 nM) association and dissociation assay.
kon (k3) and koff (k4) of unlabelled CCPA in the absence or presence of 10 μM PD81,723 or BC-1 were determined in [3H]-DPCPX (2.6 nM) competition association assays.