Table 2.
Dissociation t1/2 (in min) | |||
---|---|---|---|
Antagonist | ‘Two-step competition’ | Delayed association | Radioligand dissociation |
D2S receptors (Figure 4) | |||
Raclopride | 10.3 (8.7–12.1) | 13.5 | 8.9 |
Spiperone | ≫30 | ≫45 | ≫120 |
D2L receptors (Figure 5) | |||
Raclopride | 10.2 (8.4–12) | 9.2–9.5* | 5.8* |
Spiperone | ≫30 | ≫45* | ≫120* |
CB1 receptors (Figure 6) | |||
Taranabant | 90 (75–109) | 122 | |
Rimonabant | <<60 | 6.4 |
Experiments are shown in Figures 4 and 5 or published
(Packeu et al., 2008) for the D2 receptor antagonists raclopride and spiperone and in Figure 6 for the CB1 receptor antagonists taranabant and rimonabant. Data from the TSC approach were calculated according to Equation 5 based on the obtained values of [LR]cmax and [LR]c=0 and knowledge of [L], t', k1 and k2 (see Methods). Values in brackets account for a 5% error margin of the [LR]cmax/[LR]c=0 ratio. Data from the delayed radioligand association approach were calculated according to Equation 4 by the non-linear regression fitting procedure developed by Malany et al. (2009). Data from radioligand dissociation curves were calculated by non-regression analysis of the curve based on a mono-exponential decline.
TSC, two-step competition.