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ID: ALA1138162
Journal: Bioorg Med Chem Lett
Title: Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues.
Authors: Wållberg A, Nilsson K, Osterlund K, Peterson A, Elg S, Raboisson P, Bauer U, Hammerland LG, Mattsson JP.
Abstract: 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. 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.
CiteXplore: 16380255