Pain activation of human supraspinal opioid pathways as demonstrated by [11C]-carfentanil and positron emission tomography (PET)

&NA; The role of the supraspinal endogenous opioid system in pain processing has been investigated in this study using positron emission tomography imaging of [11C]‐carfentanil, a synthetic, highly specific &mgr; opioid receptor (&mgr;‐OR) agonist. Eight healthy volunteers were studied during a baseline imaging session and during a session in which subjects experienced pain induced by applying capsaicin topically to the dorsal aspect of the left hand. A pain‐related decrease in brain &mgr;‐OR binding was observed in the contralateral thalamus consistent with competitive binding between [11C]‐carfentanil and acutely released endogenous opioid peptides. This decrease varied directly with ratings of pain intensity. These results suggest that the supraspinal &mgr;‐opioid system is activated by acute pain and thus may play a substantial role in pain processing and modulation in pain syndromes.

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