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Preparation of 6—[^18F]fluoro—L—DOPA and its biodistribution in normal and unilateral PD model rats
作者姓名:ZHANG Lan  TANG Gang-Hua  WANG Yong-Xian  YIN Duan-Zhi
作者单位:1 Center of Radiopharmaceutical Research,Shanghai Institute of Nuclear Research,the,ChineseAcademy of Sciences,Shanghai 201800;2Nanfang PET Center,Nanfang Hospital,The First Military Medical University,Guangzhou 510515
基金项目:Supported by the National Nature Sciences Foundation(10075073)
摘    要:No-carrier-added 6-18F]fluoro-L-DOPA (6-FDOPA) was synthesized via a multistep procedure from a commercial available precursor, 6-nitroveratraldehyde. The total synthesis time was 75min, with a radiochemical yield of (10±3)%, high radiochemical purity (>99%) and high enantiomeric purity (>95%). The biodistri-butions of 6-FDOPA in normal and unilateral PD model rats were measured. The results from normal rats showed the expected high concentration of radioactivity in striatum and low distributions in cerebrum, cortex and cerebellum. The ratio of the radioactivity in striatum to cerebellum reached a peak value (5.9) at 60min. In unilateral PD model rats, whose substania nigra of the right side had been damaged by pre-treated with 6-OHDA, the radioactive concentration in striatum of the damaged side was significantly lower than that of the undamaged side or that of both sides in striatum of control groups.

关 键 词:药物学  PET示踪  生物体内分布  PD模型

Preparation of 6-[18F]fluoro-L-DOPA and its biodistribution in normal and unilateral PD model rats
ZHANG Lan,TANG Gang-Hua,WANG Yong-Xian,YIN Duan-Zhi.Preparation of 6-[18F]fluoro-L-DOPA and its biodistribution in normal and unilateral PD model rats[J].Nuclear Science and Techniques,2002,13(4):244-250.
Authors:ZHANG Lan  TANG Gang-hua  WANG Yong-xian  YIN Duan-Zhi
Abstract:No-carrier-added 6-18F]fluoro-L-DOPA (6-FDOPA) was synthesized viaa multistep procedure from a commercial available precursor, 6-nitroveratraldehydc.The total synthesis time was 75min, with a radiochemical yield of (10±3)%, highradiochemical purity (>99%) and high enantiomeric purity (>95%). The biodistri-butions of 6-FDOPA in normal and unilateral PD model rats were measured. Theresults from normal rats showed the expected high concentration of radioactivity instriatum and low distributions in cerebrum, cortex and cerebellum. The ratio of theradioactivity in striatum to cerebellum reached a peak value (5.9) at 60 min. In uni-lateral PD model rats, whose substania nigra of the right side had been damaged bypre-treated with 6-OHDA, the radioactive concentration in striatum of the damagedside was significantly lower than that of the undamaged side or that of both sides instriatum of control groups.
Keywords:6-[18F]fluoro-L-DOPA  Biodistribution  Rats  Unilateral PD model
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