Tritiated-6-beta-fluoro-6-desoxy-oxymorphone 〈[3H] FOXY〉: a new ligand and photoaffinity probe for the MU opioid receptors
1988; Elsevier BV; Volume: 11; Issue: 1 Linguagem: Inglês
10.1016/0143-4179(88)90020-0
ISSN1532-2785
AutoresRichard B. Rothman, Victor Bykov, Kenner C. Rice, Arthur E. Jacobson, Grace N. Kooper, Wayne D. Bowen,
Tópico(s)Pharmacological Receptor Mechanisms and Effects
Resumo6-Beta-fluoro-6-desoxy-oxymorphone (FOXY) is a fluorinated derivative of oxymorphone originally developed as a potential PET scanning ligand. Preliminary work (Rothman et al., Neuropeptides 4: 311–317, 1984) demonstrated that [3H]FOXY selectively labeled mu opioid binding sites with low levels of nonspecific binding. In this study the opiate receptor subtypes labeled by [3H]FOXY and [3H]D-ala2-MePhe4, Gly-ol5-enkephalin 〈[3H] DAGO〉 were compared using site directed acylating agents and binding surface analysis. Although the data indicated that both ligands selectively label mu opiate receptors, other experiments demonstrated that [3H]DAGO and [3H]FOXY labeled mu binding sites differently. Additional experiments demonstrated that [3H]FOXY can be used as a high yield photoaffinity label for the mu opiate receptor subtype.
Referência(s)