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. 2010 Nov;161(6):1311–1328. doi: 10.1111/j.1476-5381.2010.00931.x

Table 2.

Antagonist dissociation half-lives calculated by different approaches

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.