2005
A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators
Rodriguez A, Nong Y, Sekaran N, Alagille D, Tamagnan G, Conn P. A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators. Molecular Pharmacology 2005, 68: 1793-1802. PMID: 16155210, DOI: 10.1124/mol.105.016139.Peer-Reviewed Original ResearchConceptsMetabotropic glutamate receptor subtype 5Subtype 5Allosteric siteG protein-coupled receptorsProtein-coupled receptorsMajor excitatory neurotransmitterCentral nervous systemMPEP siteAntagonist MPEPBinding of glutamateOnly partial inhibitionExcitatory neurotransmitterSubthalamic nucleusCalcium mobilizationNervous systemSite ligandsAllosteric modulatorsPartial antagonistValuable new toolNovel compoundsValuable new insightsOrthosteric ligandsAllosteric modulationFunctional effectsNative systems
2004
Synthesis and monoamine transporter affinity of 3′-analogs of 2-β-carbomethoxy-3-β-(4′-iodophenyl)tropane (β-CIT)
Bois F, Baldwin R, Kula N, Baldessarini R, Innis R, Tamagnan G. Synthesis and monoamine transporter affinity of 3′-analogs of 2-β-carbomethoxy-3-β-(4′-iodophenyl)tropane (β-CIT). Bioorganic & Medicinal Chemistry Letters 2004, 14: 2117-2120. PMID: 15080991, DOI: 10.1016/j.bmcl.2004.02.043.Peer-Reviewed Original Research
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
Synthesis and monoamine transporter affinity of 2β-carbomethoxy-3β-(2″-, 3″- or 4″-substituted) biphenyltropanes
Tamagnan G, Baldwin R, Kula N, Baldessarini R, Innis R. Synthesis and monoamine transporter affinity of 2β-carbomethoxy-3β-(2″-, 3″- or 4″-substituted) biphenyltropanes. Bioorganic & Medicinal Chemistry Letters 2000, 10: 1783-1785. PMID: 10969967, DOI: 10.1016/s0960-894x(00)00317-6.Peer-Reviewed Original ResearchAnimalsCarrier ProteinsCocaineDopamineDopamine Plasma Membrane Transport ProteinsMembrane GlycoproteinsMembrane Transport ProteinsMolecular StructureNerve Tissue ProteinsNorepinephrineNorepinephrine Plasma Membrane Transport ProteinsProsencephalonRadioligand AssayRatsSerotoninSerotonin Plasma Membrane Transport ProteinsSymportersTropanesCyclopentadienyltricarbonylrheniumbenzazepines: 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 Research5-Iodo-A-85380, an α4β2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors
Mukhin A, Gündisch D, Horti A, Koren A, Tamagnan G, Kimes A, Chambers J, Vaupel D, King S, Picciotto M, Innis R, London E. 5-Iodo-A-85380, an α4β2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors. Molecular Pharmacology 2000, 57: 642-649. PMID: 10692507, DOI: 10.1124/mol.57.3.642.Peer-Reviewed Original ResearchConceptsNicotinic acetylcholine receptorsAlpha4beta2 nAChRsAcetylcholine receptorsNeuronal nicotinic acetylcholine receptorsAffinity of epibatidineRat adrenal glandMuscle-type nAChRsSubtype-selective ligandsAlpha4beta2 subtypeAdrenal glandRat brainSelective radioligandBrain regionsNAChRsBeta4 subunitsRadioiodinated ligandBeta2 subunitVivo studiesEpibatidineVivo experimentsHuman brainSubtypesRadioligandBrainReceptors
1999
Nonisotopic surrogates for technetium as ligands for monoamine transporters.
Tamagnan G, Gao Y, Xu L, Kula N, Baldessarini R, Neumeyer J. Nonisotopic surrogates for technetium as ligands for monoamine transporters. Advances In Neurology 1999, 80: 99-103. PMID: 10410707.Peer-Reviewed Original Research
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