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Synthesis of [ 3 H]fenobam, a radioligand for the mGlu5 receptor
Author(s) -
Hartung Thomas,
Peters JensUwe,
Wichmann Jürgen,
Hubschwerlen Christian,
Jaeschke Georg
Publication year - 2008
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1470
Subject(s) - allosteric regulation , radioligand , chemistry , pharmacology , metabotropic receptor , metabotropic glutamate receptor 5 , allosteric modulator , metabotropic glutamate receptor , radioligand assay , receptor , binding site , glutamate receptor , anxiolytic , stereochemistry , biochemistry , medicine
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.