The synthesis of a benzamidine-containing NR2B-selective NMDA receptor ligand labelled with tritium or fluorine-18

被引：24

作者：

Hamill, TG

McCauley, JA

Burns, HD

机构：

[1] Merck Res Labs, Imaging Res Dept, W Point, PA 19486 USA

[2] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2005年 / 48卷 / 01期

关键词：

fluorine-18; tritium; PET; NR2B; deuterium;

D O I：

10.1002/jlcr.871

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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 (2916Ci/mmol), which was deuterated in the fluoromethoxy group to aid in metabolic stability, was synthesized by alkylating a phenolic precursor with [F-18]fluoromethylbromide-d(2). Copyright (C) 2004 John Wiley Sons, Ltd.

引用

页码：1 / 10

页数：10

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