The synthesis of a benzamidine-containing NR2B-selective NMDA receptor ligand labelled with tritium or fluorine-18
✍ Scribed by Terence G. Hamill; John A. McCauley; H. Donald Burns
- Publisher
- John Wiley and Sons
- Year
- 2005
- Tongue
- French
- Weight
- 118 KB
- Volume
- 48
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.871
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✦ Synopsis
Abstract
A novel tritium or flourine‐18‐labelled benzamidine‐containing NR2B‐selective NMDA receptor ligand has been synthesized. This compound was designed to contain the fluoromethoxy group to allow for the synthesis of a high specific activity, fluorine‐18‐labelled PET tracer for imaging studies of the NR2B receptor. In addition to the fluorine‐18‐labelled compound, this compound was also tritium labelled. The tritiated ligand (11 Ci/mmol) was synthesized by a gas tritiation reaction of an aryl bromide precursor. The fluorine‐18 ligand (2916 Ci/mmol), which was deuterated in the fluoromethoxy group to aid in metabolic stability, was synthesized by alkylating a phenolic precursor with [^18^F]fluoromethylbromide‐d~2~. Copyright © 2004 John Wiley & Sons, Ltd.