| Literature DB >> 16279797 |
Guo Zhu Zheng1, Pramila Bhatia, Jerome Daanen, Teodozyj Kolasa, Meena Patel, Steven Latshaw, Odile F El Kouhen, Renjie Chang, Marie E Uchic, Loan Miller, Masaki Nakane, Sonya G Lehto, Marie P Honore, Robert B Moreland, Jorge D Brioni, Andrew O Stewart.
Abstract
SAR (structure-activity relationship) studies of triazafluorenone derivatives as potent mGluR1 antagonists are described. The triazafluorenone derivatives are non-amino acid derivatives and noncompetitive mGluR1 antagonists that bind at a putative allosteric recognition site located within the seven-transmembrane domain of the receptor. These triazafluorenone derivatives are potent, selective, and systemically active mGluR1 antagonists. Compound 1n, for example, was a very potent mGluR1 antagonist (IC50 = 3 nM) and demonstrated full efficacy in various in vivo animal pain models.Entities:
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Year: 2005 PMID： 16279797 DOI： 10.1021/jm0504407
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446