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
2002
Rearrangement of a Mesylate Tropane Intermediate in Nucleophilic Substitution Reactions. Synthesis of Aza-Bicyclo[3.2.1]octane and Aza-Bicyclo[3.2.2]nonane Ethers, † Imides, and Amines
Ogier L, Turpin F, Baldwin R, Riché F, Law H, Innis R, Tamagnan G. Rearrangement of a Mesylate Tropane Intermediate in Nucleophilic Substitution Reactions. Synthesis of Aza-Bicyclo[3.2.1]octane and Aza-Bicyclo[3.2.2]nonane Ethers, † Imides, and Amines. The Journal Of Organic Chemistry 2002, 67: 3637-3642. PMID: 12027674, DOI: 10.1021/jo010973x.Peer-Reviewed Original ResearchMeSH KeywordsAlkanesAminesAza CompoundsBridged Bicyclo CompoundsEthersImidesMagnetic Resonance SpectroscopyMesylatesOctanesTropanes
2001
Synthesis of Cyclopentadienyltricarbonyl Rhenium Phenyltropanes by Double Ligand Transfer: Organometallic Ligands for the Dopamine Transporter
Cesati R, Tamagnan G, Baldwin R, Zoghbi S, Innis R, Kula N, Baldessarini R, Katzenellenbogen J. Synthesis of Cyclopentadienyltricarbonyl Rhenium Phenyltropanes by Double Ligand Transfer: Organometallic Ligands for the Dopamine Transporter. Bioconjugate Chemistry 2001, 13: 29-39. PMID: 11792176, DOI: 10.1021/bc010011x.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding, CompetitiveChemical PhenomenaChemistry, PhysicalChromatography, Thin LayerDopamine Plasma Membrane Transport ProteinsIndicators and ReagentsKineticsLigandsMagnetic Resonance SpectroscopyMembrane GlycoproteinsMembrane Transport ProteinsMiceNeostriatumNerve Tissue ProteinsOrganometallic CompoundsRheniumSpectrophotometry, UltravioletTropanesConceptsExcellent functional group toleranceLigand transfer reactionDouble ligand transfer reactionDouble-ligand transferFunctional group toleranceOrganometallic ligandsRhenium systemsLigand transferTransfer reactionsGroup toleranceDirect preparationFerrocene precursorsReasonable yieldsReactionConjugatesModular natureFerrocenePerrhenateLigandsCompoundsSynthesisConvenient mannerPrecursorsPreparationBinder
1996
N-Substituted Analogs of 2β-Carbomethoxy-3β-(4‘-iodophenyl)tropane (β-CIT) with Selective Affinity to Dopamine or Serotonin Transporters in Rat Forebrain
Neumeyer J, Tamagnan G, Wang S, Gao Y, Milius R, Kula N, Baldessarini R. N-Substituted Analogs of 2β-Carbomethoxy-3β-(4‘-iodophenyl)tropane (β-CIT) with Selective Affinity to Dopamine or Serotonin Transporters in Rat Forebrain. Journal Of Medicinal Chemistry 1996, 39: 543-548. PMID: 8558525, DOI: 10.1021/jm9505324.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding SitesCarrier ProteinsCocaineDopamineDopamine Plasma Membrane Transport ProteinsMagnetic Resonance SpectroscopyMembrane GlycoproteinsMembrane Transport ProteinsMolecular ProbesNerve Tissue ProteinsProsencephalonRadioligand AssayRatsSerotoninSerotonin Plasma Membrane Transport ProteinsSpectrometry, Mass, Fast Atom BombardmentConceptsBeta-CITN-fluoropropylMood-elevating drugsRat brain tissueBeta-carbomethoxy-3 betaDA neuronsSerotonin neuronsDA transporterNeuropharmacological evaluationRat forebrainBrain tissueImproved markersSerotonin transporterDAT affinityNeuronsDopamineBetaDAT selectivitySelective affinityTransportersHigh affinityEster analoguesSerotoninForebrainNovel series