Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam

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 gl...

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Published inACS medicinal chemistry letters Vol. 2; no. 12; pp. 882 - 884
Main Authors Gichinga, Moses G, Olson, Jeremy P, Butala, Elizabeth, Navarro, Hernán A, Gilmour, Brian P, Mascarella, S. Wayne, Carroll, F. Ivy
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 08.12.2011
Subjects
Letter
drug addiction
Fenobam
metabotropic glutamate receptors
mGluR5 antagonist
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Summary: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 IC50 value for 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-1,4,5,6-tetrahydropyridine)­urea (4g) was essentially identical to that of fenobam.
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ISSN:1948-5875
1948-5875
DOI:10.1021/ml200162f