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Synthesis of [3H]fenobam, a radioligand for the mGlu5 receptor

✍ Scribed by Thomas Hartung; Jens-Uwe Peters; Jürgen Wichmann; Christian Hubschwerlen; Georg Jaeschke

Publisher
John Wiley and Sons
Year
2008
Tongue
French
Weight
102 KB
Volume
51
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Fenobam is a clinically efficacious anxiolytic that acts as metabotropic glutamate receptor 5 (mGlu5) antagonist by binding to an allosteric site. Other mGlu5 receptor antagonists such as MPEP and MTEP bind to the same allosteric site and are efficacious in preclinical models of anxiety and depression. Consequently, the allosteric‐binding site of the mGlu5 receptor is an attractive target for the discovery of novel psychiatric therapies. Radioligands of this binding site can be used for in vitro and in vivo pharmacodynamic studies. We report here a short synthesis of such a radioligand for the allosteric mGlu5 receptor‐binding site, [^3^H]fenobam. Copyright © 2008 John Wiley & Sons, Ltd.

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