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- W2243353994 abstract "A convenient method for the preparation of F-18-3-acetylcyclofoxy (3-acetyl-6-deoxy-6-beta-F-18-fluoronaltrexone was developed. The method uses reactor-produced F-18-fluoride as its tetraethylammonium salt. F-18 fluoride is produced at the National Bureau of Standards nuclear reactor by the Li-6(n,..cap alpha..)H-3, 0-16(H-3,n) F-18 nuclear reaction. A sealed quartz tube containing enriched lithium carbonate (0.4 g) was irradiated in a neutron flux of 1.1 x 10/sup 14/ n/cm/sup 2//s for 2h to produce 80 mCi. The lithium is removed by cation exchange resin. The fluoride is then adsorbed on a strong anion exchange column which is rinsed to remove H-3 and any remaining cations. The F-18 is then eluted with tetraethylammonium hydroxide to produce tetraethylammonium fluoride (TEAF). The triflate of 3-acetyl-6-alpha-naltrexol, synthesized by reaction of the alcohol with trifluoromethanesulfonic anhydride was added in anhydrous acetonitrile to the dry F-18 TEAF containing 0.2 ..mu..mol F-19 TEAF. The mixture was refluxed for 15 minutes after which the product was purified by reversed phase chromatography. F-18-acetylcyclofoxy was prepared in 35% radiochemical yield. About 55% of the F-18 was lost by decay (36%) and by incomplete transfer (19%). The specific activity of the final product was approximately 50 Ci/mmol but the effective specific activity was approximately 25 Ci/mmol. Visualization ofmore » the basal ganglia in baboons was possible using PET. F-18 3-acetylcyclofoxy is the first positron-emitting opiate for which the active and inactive forms of naloxone were used to unequivocially demonstrate stereospecific displacement from opiate receptor-rich regions.« less" @default.
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- W2243353994 date "1985-05-01" @default.
- W2243353994 modified "2023-09-23" @default.
- W2243353994 title "Radiosynthesis of F-18-3-acetylcyclofoxy: A high affinity opiate antagonist" @default.
- W2243353994 hasPublicationYear "1985" @default.
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