Preparation of 6-[¹⁸F]fluoro-L-DOPA and its biodistribution in normal and unilateral PD model rats

Preparation of 6-[ 18 F]fluoro-L-DOPA and its biodistribution in normal and unilateral PD model rats 1 corresp first-author Correspondence author: ZHANG Lan: zhangl@sina.com Correspondence author: ZHANG Lan: zhangl@sina.com zhangl@sina.com 1 2 1 1 1 Center of Radiopharmaceutical Research, Shanghai Institute of Nuclear Research, the Chinese Academy of Sciences, Shanghai 201800 1 Center of Radiopharmaceutical Research, Shanghai Institute of Nuclear Research, the Chinese Academy of Sciences, Shanghai 201800 2Nanfang PET Center, Nanfang Hospital, The First Military Medical University, Guangzhou 510515 2Nanfang PET Center, Nanfang Hospital, The First Military Medical University, Guangzhou 510515 No-carrier-added 6-[ 18 F] 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 biodistributions 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 60 min. 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. 6-[ 18 F]fluoro-L-DOPA Biodistribution Rats Unilateral PD model References Luxen A , Guillaume M , Melega W P et al . Nucl Med Biol , 1992 , 19 : 149 - 158 Nucl Med Biol Dolle F , Denphel S , Hinnen S et al . J Labelled Compd Radiopharm , 1998 , XLI : 105 - 114 J Labelled Compd Radiopharm Lemaire C , Guillaume M , Cantineau R et al . J Nucl Med , 1990 , 31 : 1247 - 1251 J Nucl Med Lemaire C , Damhaut P , Plenevaux A et al . J Nucl Med , 1994 , 35 : 1996 - 2002 J Nucl Med Najafi A. Nucl Med Biol , 1995 , 22 : 395 - 397 Nucl Med Biol Landais P , Bonnefoi F , Kudlyk V et al . J Labelled Compd Radiopharm , 1995 , 37 : 647 - 651 J Labelled Compd Radiopharm Lemaire C , Guillouet S , Brihaye C et al . J Labelled Compd Radiopharm , 1999 , 42 ( suppl 1 ): s113 - s115 J Labelled Compd Radiopharm Guillouet S , Lemaire C , Bonmarchand G et al . J Labelled Compd Radiopharm. 2001 . 44 ( suppl ): s868 - s870 J Labelled Compd Radiopharm. Firnau G , Garnett E S , Chan P K H et al . J Pharm Pharmacol , 1976 , 28 : 584 - 585 J Pharm Pharmacol Home M K , Cheng C H , Wooten G F. Pharmacology , 1984 , 28 : 12 - 26 Pharmacology Javoy-Agid F , Agid Y. Neurology , 1980 , 30 ( 12 ): 1326 - 1330 Neurology Lindvall O , Bjorklund A. Acta Physiol Scand Suppl . 1974 , 412 : 1 - 48 Acta Physiol Scand Suppl Anden N E , Carlsson A , Haggendal J. Annu Rev Pharmacol , 1969 , 9 : 119 - 134 Annu Rev Pharmacol Garnett E S , Firnau G , Nahmias C. Nature , 1983 , 305 ( 8 ): 137 - 138 Nature Corey E J , Xu F , Noc M C. J Am Chem Soc , 1997 , 119 : 12414 - 12415 J Am Chem Soc Keinan E , Perez D , Sahai M et al . J Org Chem , 1990 , 55 : 2927 - 2938 J Org Chem Hoffman J M , Melega W P , Hawk T C et al . J Nucl Med , 1992 , 33 : 1472 - 1477 J Nucl Med O615.3 Supported by the National Nature Sciences Foundation (10075073) 2002-03-05 2002-11-01 2021-02-05 2002 Nuclear Science and Techniques 4 13