2025
598. Impact of the mGluR5 Antagonist, Mavoglurant, on P300 Response in an Auditory Oddball Task in in Individuals With a Positive or Negative Family History of Alcoholism
Richardson A, Stone A, Pearlson G, Krystal J, DeMartini K, O'Malley S, Mubeen M, Pancholi K. 598. Impact of the mGluR5 Antagonist, Mavoglurant, on P300 Response in an Auditory Oddball Task in in Individuals With a Positive or Negative Family History of Alcoholism. Biological Psychiatry 2025, 97: s345. DOI: 10.1016/j.biopsych.2025.02.837.Peer-Reviewed Original Research
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
2007
Rapid Direct Excitation and Long-Lasting Enhancement of NMDA Response by Group I Metabotropic Glutamate Receptor Activation of Hypothalamic Melanin-Concentrating Hormone Neurons
Huang H, van den Pol AN. Rapid Direct Excitation and Long-Lasting Enhancement of NMDA Response by Group I Metabotropic Glutamate Receptor Activation of Hypothalamic Melanin-Concentrating Hormone Neurons. Journal Of Neuroscience 2007, 27: 11560-11572. PMID: 17959799, PMCID: PMC6673210, DOI: 10.1523/jneurosci.2147-07.2007.Peer-Reviewed Original ResearchConceptsGroup I metabotropic glutamate receptor activationMetabotropic glutamate receptor activationDHPG-induced depolarizationGlutamate receptor activationGroup IHormone neuronsMGluR5 antagonistGreen fluorescent protein-expressing transgenic miceNMDA receptor-mediated postsynaptic currentsReceptor activationExchanger blocker KB-R7943Melanin-concentrating hormone (MCH) neuronsMelanin-Concentrating Hormone NeuronsReceptor-mediated postsynaptic currentsBlockade of mGluR1Selective group IGroup I mGluRsPatch-clamp recordingsMCH neuron activityI mGluRsMCH neuronsHypocretin neuronsSpontaneous EPSCsPostsynaptic mechanismsHypothalamic slices
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
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