2005
Synthesis, Radiosynthesis, and Biological Evaluation of Carbon-11 and Fluorine-18 (N-Fluoroalkyl) Labeled 2β-Carbomethoxy-3β-(4'-(3-furyl)phenyl)tropanes and -nortropanes: Candidate Radioligands for in Vivo Imaging of the Serotonin Transporter with Positron Emission Tomography
Stehouwer J, Plisson C, Jarkas N, Zeng F, Voll R, Williams L, Martarello L, Votaw J, Tamagnan G, Goodman M. Synthesis, Radiosynthesis, and Biological Evaluation of Carbon-11 and Fluorine-18 (N-Fluoroalkyl) Labeled 2β-Carbomethoxy-3β-(4'-(3-furyl)phenyl)tropanes and -nortropanes: Candidate Radioligands for in Vivo Imaging of the Serotonin Transporter with Positron Emission Tomography. Journal Of Medicinal Chemistry 2005, 48: 7080-7083. PMID: 16250668, DOI: 10.1021/jm0504095.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding, CompetitiveBrainCarbon RadioisotopesCell LineDopamine Plasma Membrane Transport ProteinsFluorine RadioisotopesFuransHumansLigandsMacaca fascicularisMacaca mulattaNorepinephrine Plasma Membrane Transport ProteinsNortropanesPositron-Emission TomographyRadioligand AssayRadiopharmaceuticalsSerotonin Plasma Membrane Transport ProteinsStructure-Activity RelationshipTropanesFunctionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP
Alagille D, Baldwin R, Roth B, Wroblewski J, Grajkowska E, Tamagnan G. Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP. Bioorganic & Medicinal Chemistry Letters 2005, 15: 945-949. PMID: 15686891, DOI: 10.1016/j.bmcl.2004.12.047.Peer-Reviewed Original ResearchAnimalsInhibitory Concentration 50MicePyridinesReceptors, Kainic AcidStructure-Activity RelationshipSynthesis 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
2003
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM
Baldwin R, Fu X, Kula N, Baldessarini R, Amici L, Innis R, Tamagnan G. Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM. Bioorganic & Medicinal Chemistry Letters 2003, 13: 4015-4017. PMID: 14592497, DOI: 10.1016/j.bmcl.2003.08.063.Peer-Reviewed Original ResearchMeSH KeywordsBenzamidesIndicators and ReagentsIodine RadioisotopesIsotope LabelingMolecular StructurePyrrolidinesStructure-Activity Relationship
2002
Synthesis, Receptor Potency, and Selectivity of Halogenated Diphenylpiperidines as Serotonin 5-HT2A Ligands for PET or SPECT Brain Imaging
Fu X, Tan P, Kula N, Baldessarini R, Tamagnan G, Innis R, Baldwin R. Synthesis, Receptor Potency, and Selectivity of Halogenated Diphenylpiperidines as Serotonin 5-HT2A Ligands for PET or SPECT Brain Imaging. Journal Of Medicinal Chemistry 2002, 45: 2319-2324. PMID: 12014970, DOI: 10.1021/jm0200411.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsCOS CellsHumansIn Vitro TechniquesLigandsPiperidinesProsencephalonRadioligand AssayRatsReceptor, Serotonin, 5-HT2AReceptor, Serotonin, 5-HT2CReceptors, Adrenergic, alpha-1Receptors, Adrenergic, alpha-2Receptors, Dopamine D2Receptors, SerotoninStructure-Activity RelationshipTomography, Emission-ComputedTomography, Emission-Computed, Single-Photon
2000
Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity
Tamagnan G, Baldwin R, Kula N, Baldessarini R, Innis R. Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity. Bioorganic & Medicinal Chemistry Letters 2000, 10: 1113-1115. PMID: 10843230, DOI: 10.1016/s0960-894x(00)00185-2.Peer-Reviewed Original Research