Synthesis of [3H]fenobam,a radioligand for the mGlu5 receptor |
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| Authors: | Thomas Hartung Jens‐Uwe Peters Jürgen Wichmann Christian Hubschwerlen Georg Jaeschke |
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| Affiliation: | 1. Pharma Research Basel, Technical Sciences, F. Hoffmann‐La Roche Ltd., CH‐4070 Basel, Switzerland;2. Pharma Research Basel, Discovery Chemistry, F. Hoffmann‐La Roche Ltd., CH‐4070 Basel, Switzerland;3. Actelion Pharmaceuticals Ltd., Gewerbestrasse 16, CH‐4123 Allschwil, Switzerland |
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| 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, [3H]fenobam. Copyright © 2008 John Wiley & Sons, Ltd. |
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| Keywords: | radioligand fenobam mGlu5 allosteric binding tritium |
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