Abstract: The metabolism of the positron‐emitting compound (18F)6‐fluoro‐l‐3,4‐dihydroxyphenylalanine (*F‐DOPA) was studied in carbidopa‐pretreated male hooded rats. Thirty minutes following carbidopa administration (5 mg/kg i.p.), animals received *F‐DOPA (500 μg/kg; specific activity, 175–230 Ci/mol) as an intrajugular bolus. Blood samples were taken at various times between 5 and 90 min, and the plasma was analyzed by HPLC with gamma counting of fractions. *F‐DOPA disappeared rapidly from plasma in concert with the formation of the 3‐O‐methylated metabolite, Me‐*F‐DOPA. Animals were killed from 5 to 120 min after injection, and the brains were rapidly dissected. The disappearance of *F‐DOPA from both vermis and striatal samples was rapid. Me‐*F‐DOPA, the sole metabolite observed in the vermis, was the major labeled material in the striatum at ≥20 min after injection. Fluorodopamine was an important metabolite in the striatum, making up 25% of total radioactivity at early intervals. Striatal samples also contained fluoro‐3,4‐dihydroxyphenylacetic acid, which constituted ∼10% of the total radioactivity, and traces of two radiolabeled compounds, tentatively identified as fluorohomovanillic acid and fluoro‐3‐methoxytyramine.
Journal of Neurochemistry – Wiley
Published: Feb 1, 1987
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