Receptor localization, native tissue binding and <i>ex vivo</i> occupancy for centrally penetrant P2X7 antagonists in the rat

Abstract

The present study describes the development of an assay that allows localization of P2X7 receptors, the measurement of the binding affinity of P2X7 receptor antagonists in native tissue, and provides a means of determining central P2X7 receptor occupancy. These assays could form an important part of a P2X7 drug discovery programme.