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- Title
In vivo studies of opiate receptors.
- Authors
Frost, J. James; Dannals, Robert F.; Duelfer, Timothy; Burns, H. Donald; Ravert, Hayden T.; Langströ, Bengt; Balasubramanian, V.; Wagner, Henry N.
- Abstract
To study opiate receptors noninvasively in vivo using positron emission tomography, techniques for perferentially labeling opiate receptors in vivo can be used. The rate at which receptor-bound ligand clears from the brain in vivo can be perdicted by measuring the equilibrium dissociation constant (KD) at 37°C in the presence of 100 mM sodium chloride and 100 μM guanyl-5′-imidodiphosphate, the drug distribution coeffcient, and the molecular weight. A suitable ligand for labeling opiate receptors in vivo is dipernorphine, which binds to μ, δ and k receptors with apporximately equal affinity in vitro. However, in vivo diprenorphine may bind predominantly to one opiate receptor subtype, possibly the μ receptor. To predict the affinity for binding to the opiate receptor, a Hansch correlation was determined between the 50% inhibitory concentration for a series of halogen-substituted fentanyl analogs and electronic, lipophilic, and steric parameters. Radiochemical methods for the synthesis of carbon-11-labeled diprenorphine and lofentanil are presented.
- Publication
Annals of Neurology, 1984, Vol 15, Issue S1, p85
- ISSN
0364-5134
- Publication type
Article
- DOI
10.1002/ana.410150716