1227701-03-2Relevant academic research and scientific papers
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5
Zhang, Peng,Zou, Mu-Fa,Rodriguez, Alice L.,Jeffrey Conn,Newman, Amy Hauck
, p. 3026 - 3035 (2010)
The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in numerous neuropsychiatric disorders including addiction. We have discovered that the rigid diaryl alkyne template, derived from the potent and selective noncompetitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP), can serve to guide the design of novel quinoline analogues and pharmacophore optimization has resulted in potent mGluR5 noncompetitive antagonists (EC50 range 60-100 nM) in the quinoline series.
