2015
Synthesis of 3‐[18F]Fluoro‐5‐(2‐Pyridinylethynyl)Benzonitrile ([18F]FPEB)
Liang S, Yokell D, Jackson R, Rice P, Livni E, Alagille D, Tamagnan G, Collier T, Vasdev N. Synthesis of 3‐[18F]Fluoro‐5‐(2‐Pyridinylethynyl)Benzonitrile ([18F]FPEB). 2015, 41-51. DOI: 10.1002/9781118834114.ch5.Peer-Reviewed Original ResearchMetabotropic glutamate receptor subtype 5Regional brain concentrationsHealthy human subjectsBrain concentrationsBrain penetranceMGluR5 antagonistSubtype 5Parkinson's diseasePathologic processesAlzheimer's diseaseNeuropsychiatric disordersNeurodegenerative diseasesDiseaseHigh potencyHuman subjectsEvidence pointsFragile X syndromeControl testsRadiochemical purityCritical roleX syndromeMGluR5SyndromeAntagonistAbnormalities
2012
Erratum to “Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series” [Bioorg. Med. Chem. Lett. 21 (2011) 3243–3247]
Alagille D, DaCosta H, Chen Y, Hemstapat K, Rodriguez A, Baldwin R, Conn P, Tamagnan G. Erratum to “Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series” [Bioorg. Med. Chem. Lett. 21 (2011) 3243–3247]. Bioorganic & Medicinal Chemistry Letters 2012, 22: 2130. DOI: 10.1016/j.bmcl.2012.01.054.Peer-Reviewed Original ResearchPotent mGluR5 antagonistMGluR5 antagonist
2005
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 ResearchConceptsNoncompetitive antagonistMetabotropic glutamate receptor subtype 5Potent mGluR5 antagonistNervous system disordersMGluR5 antagonistSubtype 5Novel noncompetitive antagonistSystem disordersAntagonist activityAntagonistPotential therapeuticsDrug addictionSAR studiesInactive productsCritical roleMGluR5MPEPPain