Synthesis and receptor assay of aromatic–ethynyl–aromatic derivatives with potent mGluR5 antagonist activity
Alagille D, Baldwin R, Roth B, Wroblewski J, Grajkowska E, Tamagnan G. Synthesis and receptor assay of aromatic–ethynyl–aromatic derivatives with potent mGluR5 antagonist activity. Bioorganic & Medicinal Chemistry 2005, 13: 197-209. PMID: 15582465, DOI: 10.1016/j.bmc.2004.09.042.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsCHO CellsCricetinaeCyclic AMPExcitatory Amino Acid AntagonistsHumansMagnetic Resonance SpectroscopyReceptor, Metabotropic Glutamate 5Receptors, Metabotropic GlutamateSpectrometry, Mass, Electrospray IonizationStructure-Activity RelationshipConceptsNoncompetitive antagonistMetabotropic glutamate receptor subtype 5Potent mGluR5 antagonistNervous system disordersMGluR5 antagonistSubtype 5Novel noncompetitive antagonistSystem disordersAntagonist activityAntagonistPotential therapeuticsDrug addictionSAR studiesInactive productsCritical roleMGluR5MPEPPain