Precursor synthesis and radiolabelling of [11C]ADAM:: A potential radioligand for the serotonin transporter exploration by PET

被引:28
作者
Vercouillie, J
Tarkiainen, S
Halldin, C
Emond, P
Chalon, S
Sandell, J
Langer, O
Guilloteau, D
机构
[1] Univ Tours, Fac Pharmaceut Sci, Lab Biophys Med & Pharmaceut, INSERM U316, F-37200 Tours, France
[2] Karolinska Hosp, Psychiat Sect, Dept Clin Neurosci, Karolinska Inst, S-17176 Stockholm, Sweden
关键词
N; N-dimethyl-2-(2-amino-4-iodophenylthio)benzylamine; serotonin transporter; carbon-11; PET;
D O I
10.1002/jlcr.436
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The serotoninergic system is involved in a variety of neurological and psychiatric disorders. Exploration of the serotonin transporters (5-HTT) in living human brain by PET would be of great value for better understanding, diagnosis and therapeutic follow up of these diseases. In order to obtain a selective radioligand to explore the 5-HTT by PET we report the synthesis of [C-11]N,N-dimethyl-2-(2-amino-4-iodophenylthio)-benzylamine ([C-11]ADAM). The precursor for labelling N-demethyl ADAM, was obtained in five steps using 2,5-dibromonitrobenzene and 2-thio-N-methylbenzamide as starting material. [C-11]ADAM was synthesised by N-alkylation of the precursor using [C-11]methyl iodide in DMF. The incorporation yield of [C-11]methyl iodide was in the range of 50 to 70%. Finally [C-11]ADAM was obtained in 30 minutes synthesis time including HPLC and with a radiochemical purity better than 99%.
引用
收藏
页码:113 / 120
页数:8
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