title: Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().
abstract: In an effort to discover potent and selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonists, 15 tetrahydropyrimidinone analogues of 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)-urea (fenobam) were synthesized. These compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. The IC(50) value for 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-1,4,5,6-tetrahydropyridine)urea (4g) was essentially identical to that of fenobam.
authors.affiliation: Center for Organic and Medicinal Chemistry, Research Triangle Institute, Post Office Box 12194, Research Triangle Park, North Carolina 27709.
authors.forename: Moses G
authors.initials: MG
authors.lastname: Gichinga
authors.forename: Jeremy P
authors.initials: JP
authors.lastname: Olson
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Butala
authors.forename: Hernán A
authors.initials: HA
authors.lastname: Navarro
authors.forename: Brian P
authors.initials: BP
authors.lastname: Gilmour
authors.forename: S Wayne
authors.initials: SW
authors.lastname: Mascarella
authors.forename: F Ivy
authors.initials: FI
authors.lastname: Carroll