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

✍ Scribed by Johnny VERCOUILLIE; Jari TARKIAINEN; Christer HALLDIN; Patrick EMOND; Sylvie CHALON; Johan SANDELL; Oliver LANGER; Denis GUILLOTEAU

Publisher: John Wiley and Sons
Year: 2001
Tongue: French
Weight: 350 KB
Volume: 44
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.436

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✦ Synopsis

Abstract

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 [^11^C]N,N‐dimethyl‐2‐(2‐amino‐4‐iodophenylthio)‐benzylamine ([^11^C]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. [^11^C]ADAM was synthesised by N‐alkylation of the precursor using [^11^C]methyl iodide in DMF. The incorporation yield of [^11^C]methyl iodide was in the range of 50 to 70%. Finally [^11^C]ADAM was obtained in 30 minutes synthesis time including HPLC and with a radiochemical purity better than 99%. Copyright © 2001 John Wiley & Sons, Ltd.

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