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 RelationshipTropanesA 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
2003
Influence of acetylcholine levels on the binding of a SPECT nicotinic acetylcholine receptor ligand [123I]5‐I‐A‐85380
Fujita M, Al‐Tikriti M, Tamagnan G, Zoghbi S, Bozkurt A, Baldwin R, Innis R. Influence of acetylcholine levels on the binding of a SPECT nicotinic acetylcholine receptor ligand [123I]5‐I‐A‐85380. Synapse 2003, 48: 116-122. PMID: 12645036, DOI: 10.1002/syn.10194.Peer-Reviewed Original ResearchConceptsPhysostigmine administrationThalamic activityPlasma levelsAcetylcholine levelsNicotinic ACh receptorsNicotinic acetylcholine receptor ligandsElevated ACh levelsSingle photon emissionAcetylcholine receptor ligandsACh levelsACh receptorsTomography ligandSustained increasePhysostigmineAdministrationReceptor ligandsAcetylcholinesterase inhibitorsPhoton emissionVivoReceptorsLevelsBolusActivityNAChRsStudy
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
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
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