Cumming P, Boyes B E, Martin W R, Adam M, Grierson J, Ruth T, McGeer E G
J Neurochem. 1987 Feb;48(2):601-8. doi: 10.1111/j.1471-4159.1987.tb04135.x.
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 micrograms/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 greater than or equal to 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 approximately 10% of the total radioactivity, and traces of two radiolabeled compounds, tentatively identified as fluorohomovanillic acid and fluoro-3-methoxytyramine.
在预先给予卡比多巴的雄性带帽大鼠中研究了正电子发射化合物[18F]6-氟-L-3,4-二羟基苯丙氨酸（F-DOPA）的代谢情况。腹腔注射卡比多巴（5mg/kg）30分钟后，动物经颈静脉推注给予F-DOPA（500μg/kg；比活度，175 - 230Ci/mol）。在5至90分钟的不同时间采集血样，血浆通过高效液相色谱法结合各馏分的γ计数进行分析。*F-DOPA与3-O-甲基化代谢产物Me-*F-DOPA的形成同步迅速从血浆中消失。在注射后5至120分钟处死动物，并迅速解剖大脑。*F-DOPA从小脑蚓部和纹状体样本中均迅速消失。Me-*F-DOPA是在小脑蚓部观察到的唯一代谢产物，在注射后大于或等于20分钟时是纹状体中的主要标记物质。氟多巴胺是纹状体中的一种重要代谢产物，在早期占总放射性的25%。纹状体样本中还含有氟-3,4-二羟基苯乙酸，约占总放射性的10%，以及两种放射性标记化合物的痕量，初步鉴定为氟高香草酸和氟-3-甲氧基酪胺。
