Tritiated-6-beta-fluoro-6-desoxy-oxymorphone ([3H]FOXY): a new ligand and photoaffinity probe for the mu opioid receptors.
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.
Rothman
R B
RB
Laboratory of Clinical Science, NIMH, Bethesda, MD 20892.
Bykov
V
V
Rice
K C
KC
Jacobson
A E
AE
Kooper
G N
GN
Bowen
W D
WD
D000345:Affinity Labels / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002712:Chlorides; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004745:Enkephalins / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008297:Male; D008345:Manganese / Q000494:pharmacology; D017895:Manganese Compounds; D008566:Membranes / Q000378:metabolism; D010111:Oxymorphone / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D010777:Photochemistry; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017450:Receptors, Opioid, mu; D014316:Tritium
D000345:Affinity Labels; D002712:Chlorides; D004745:Enkephalins; D017895:Manganese Compounds; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D014316:Tritium; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D008345:Manganese; C042285:6-fluoro-6-desoxyoxymorphone; D010111:Oxymorphone; C025340:manganese chloride