Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

Fenobam 3-(3-chlorophenyl)-1-(1- methyl-4-oxo-5H...

Synonyms: Fenobamum, CHEMBL239800, SureCN111562, McN-3377, NPL-2009, ...

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High impact information on Fenobam

In the present study, we have used the site-directed mutagenesis coupled with three-dimensional receptor-based pharmacophore modelling to elucidate the interacting mode of fenobam within the seven-transmembrane domain (7TMD) of mGlu5 receptor and its comparison with that of 2-methyl-6-(phenylethynyl)pyridine (MPEP), the prototype antagonist [1].
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity [2].

Biological context of Fenobam

Herein, we present the structure-activity relationship of fenobam and its analogues and similarities between the SAR of mGluR5 antagonism and the SAR of CNS properties originally reported by McNeil are discussed [3].

References

Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP. Malherbe, P., Kratochwil, N., Mühlemann, A., Zenner, M.T., Fischer, C., Stahl, M., Gerber, P.R., Jaeschke, G., Porter, R.H. J. Neurochem. (2006) [Pubmed]
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. Porter, R.H., Jaeschke, G., Spooren, W., Ballard, T.M., Büttelmann, B., Kolczewski, S., Peters, J.U., Prinssen, E., Wichmann, J., Vieira, E., Mühlemann, A., Gatti, S., Mutel, V., Malherbe, P. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues. Wållberg, A., Nilsson, K., Osterlund, K., Peterson, A., Elg, S., Raboisson, P., Bauer, U., Hammerland, L.G., Mattsson, J.P. Bioorg. Med. Chem. Lett. (2006) [Pubmed]

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