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Receptor occupancy and brain free fraction

Jeanette Watson1, Sara Wright, Adam Lucas

  • 1Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, Dundee, DD1 5EH, Scotland, UK.

Drug Metabolism and Disposition: the Biological Fate of Chemicals
|January 23, 2009
PubMed
Summary

Brain unbound concentration (C(u,brain)) better predicts dopamine D(2) receptor occupancy in rats than other measures. This finding is crucial for understanding antipsychotic drug efficacy and brain penetration.

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