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The necessary parameters for estimating the time-course of receptor occupancy.

The dissociation of the kinetics between plasma and the brain has been reported for antipsychotic drugs such as risperidone and olanzapine (Tauscher et al., 2002), and the kinetic profile of antipsychotics at receptor sites has been viewed as an important profile for antipsychotic actions and dosing schedule (Tauscher et al., 2002). Our recent report in this Journal (Takano et al., 2004) showed that the time-course of receptor occupancy could be estimated using plasma pharmacokinetics and drug-affinity parameters.