Abstract
17- Cydopropylmethyl -3,14- dihydroxy -4,5- alpha-epoxy-6-beta -fluoromorphinan(cycloFOXY) is a fluorinated derivative of naltrexone suitable for labeling opiate receptors using positron emission transaxial tomography. Using the quantitative ligand binding method “binding surface analysis,” in vitro autoradiography, and site-directed alkylating agents, [ 3H]cycloFOXY is shown to label mu and kappa opiate binding sites in vitro. Similar results were obtained using [ 3H]naloxone. Additional experiments demonstrate that [ 3H]cycloFOXY administered in vivo also labels mu and kappa binding sites. The relevance of these findings are discussed from clinical and basic science perspectives.
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