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Tritiated-6-beta-fluoro-6-desoxy-oxymorphone ([3H]FOXY): a new ligand and photoaffinity probe for the mu opioid receptors.

Abstract：

:6-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.

journal_name

Neuropeptides

journal_title

Neuropeptides

authors

Rothman RB,Bykov V,Rice KC,Jacobson AE,Kooper GN,Bowen WD

doi

10.1016/0143-4179(88)90020-0

subject

Has Abstract

pub_date

1988-01-01 00:00:00

pages

1-6

issue

1

eissn

0143-4179

issn

1532-2785

pii

0143-4179(88)90020-0

journal_volume

11

pub_type

杂志文章

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