Ontology highlight
ABSTRACT:
SUBMITTER: Zhang P
PROVIDER: S-EPMC2871681 | biostudies-literature | 2010 May
REPOSITORIES: biostudies-literature
Zhang Peng P Zou Mu-Fa MF Rodriguez Alice L AL Conn P Jeffrey PJ Newman Amy Hauck AH
Bioorganic & medicinal chemistry 20100327 9
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 (EC(50) range 60-100 nM) in the quinoline seri ...[more]