Pain and opiate receptors: Considerations for the design of positron emission tomography studies

Opiate receptors in the brain are the target of endogenous opioids and of exogenous synthetic opiates. These receptors play a major role in the modulation of pain perception. Using the appropriate ligands, positron emission tomography now allows investigators to monitor neuroreceptors in vivo. We have used ¹¹C-diprenorphine and the extremely potent mu opiate receptor agonist, ¹¹C-carfentanil, to image the distribution of opiate receptors in the brain and to quantify their density, their affinity, and their occupancy. Several important aspects of the in vivo opiate receptor labeling with positron emission tomography in relation to the study of pain are considered in this paper. Monitoring receptor occupancy by opiate drugs as a function of pain relief has the potential to reveal better ways to treat pain.