903570-83-2Relevant academic research and scientific papers
ANTAGONISTS OF THE MGLU RECEPTOR AND USES THEREOF
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Page/Page column 51, (2008/06/13)
The present invention discloses compounds of general formula (I) wherein X1-X4 and R1-R3 are as defined in the description. The present invention also discloses methods of treatment for pain, neurodegeneration and convulsive states in a host mammal in need thereof, and pharmaceutical compositions including those compounds.
Correlation between brain/plasma ratios and efficacy in neuropathic pain models of selective metabotropic glutamate receptor 1 antagonists
Zheng, Guo Zhu,Bhatia, Pramila,Kolasa, Teodozyj,Patel, Meena,El Kouhen, Odile F.,Chang, Renjie,Uchic, Marie E.,Miller, Loan,Baker, Scott,Lehto, Sonya G.,Honore, Prisca,Wetter, Jill M.,Marsh, Kennan C.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
, p. 4936 - 4940 (2007/10/03)
We have discovered a novel, potent, and selective triazafluorenone series of metabotropic glutamate receptor 1 (mGluR1) antagonists with efficacy in various rat pain models. Pharmacokinetic and pharmacodynamic profiles of these triazafluorenone analogs re
Structure-activity relationship of triazafluorenone derivatives as potent and selective mGluR1 antagonists
Zheng, Guo Zhu,Bhatia, Pramila,Daanen, Jerome,Kolasa, Teodozyj,Patel, Meena,Latshaw, Steven,El Kouhen, Odile F.,Chang, Renjie,Uchic, Marie E.,Miller, Loan,Nakane, Masaki,Lehto, Sonya G.,Honore, Marie P.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
, p. 7374 - 7388 (2007/10/03)
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 alloste
