Phenyl ureas of creatinine as mGluR5 antagonists. A structure–activity relationship study of fenobam analogues

Structure–activity relationship of the mGluR5 antagonist fenobam is reported. Fenobam ( 1) was developed by McNeil Laboratories as an anxiolytic agent with an unknown molecular target in the late 1970s. In a recent publication, it was revealed that fenobam is a non-competitive mGluR5 antagonist. Her...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 16; no. 5; pp. 1142 - 1145
Main Authors:	Wållberg, Andreas, Nilsson, Karolina, Österlund, Krister, Peterson, Alecia, Elg, Susanne, Raboisson, Patrick, Bauer, Udo, Hammerland, Lance G., Mattsson, Jan P.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 01-03-2006 Elsevier
Subjects:	Amides - chemistry Anxiolytic Biological and medical sciences Chlorides - chemistry Creatinine - chemistry Creatinine - pharmacology Fenobam Glutamatergic system (aspartate and other excitatory aminoacids) Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Inhibitory Concentration 50 Medical sciences Metabotropic glutamate receptor mGluR5 Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate - antagonists & inhibitors Receptors, Metabotropic Glutamate - metabolism Structure-Activity Relationship Urea - chemistry Fenobam mGluR5 Anxiolytic Metabotropic glutamate receptor Human Five membered ring Group I mglu glutamate receptor mglu5 glutamate receptor Nitrogen heterocycle Central nervous system Benzene derivatives Selectivity In vitro Encephalon Fenobam: Metabotropic glutamate receptor Phenylureas Structure activity relation Metabotropic receptor Chlorine Organic compounds Affinity Benzamide derivatives Antagonist Chemical synthesis
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