Non-invasive methods to study drug disposition: positron emission tomography. Detection and quantification of brain receptors in man.

Positron emission tomography (PET) has been used mostly for the study of brain blood flow and metabolism in normal controls and in a variety of neurological and psychiatric conditions. With the appropriate radiotracers, PET also allows non-invasive imaging and quantification of a growing list of neuroreceptors, the target of most psychotropic drugs. For example, 11C-carfentanil and 11C-diprenorphine, two potent opiate ligands, have been used to label opiate receptors in vivo in man. Methods have been developed to quantify receptor studies with PET in terms of receptor density and affinity. PET is a unique tool that now allows measurement of receptor occupancy in vivo and could be used by the pharmacologist to optimize drug treatment.