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

被引：7

作者：

Gichinga, Moses G. ^{[1
]}

Olson, Jeremy P. ^{[1
]}

Butala, Elizabeth ^{[1
]}

Navarro, Hernan A. ^{[1
]}

Gilmour, Brian P. ^{[1
]}

Mascarella, S. Wayne ^{[1
]}

Carroll, F. Ivy ^{[1
]}

机构：

[1] Res Triangle Inst, Ctr Organ & Med Chem, Res Triangle Pk, NC 27709 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2011年 / 2卷 / 12期

关键词：

Fenobam; metabotropic glutamate receptors; drug addiction; mGluR5; antagonist; POTENT; ANALOGS; DERIVATIVES; PLACEBO; COCAINE; MICE;

D O I：

10.1021/ml200162f

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：882 / 884

页数：3

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