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
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
Measurement of plasma metabolites of (S)-5-[123I]iodo-3- (2-azetidinylmethoxy)pyridine (5-IA-85380), a nicotinic acetylcholine receptor imaging agent, in nonhuman primates
Zoghbi S, Tamagnan G, Fujita M, Baldwin R, Al-Tikriti M, Amici L, Seibyl J, Innis R. Measurement of plasma metabolites of (S)-5-[123I]iodo-3- (2-azetidinylmethoxy)pyridine (5-IA-85380), a nicotinic acetylcholine receptor imaging agent, in nonhuman primates. Nuclear Medicine And Biology 2001, 28: 91-96. PMID: 11182569, DOI: 10.1016/s0969-8051(00)00188-8.Peer-Reviewed Original ResearchConceptsReceptor imaging agentNicotinic acetylcholine receptorsPotential SPECT tracerRadioactive bloodTobacco dependencePlasma concentrationsParent compoundPolar radiometaboliteAcetylcholine receptorsPlasma metabolitesProtein-free plasmaRadioactivity accumulationNeurodegenerative diseasesSPECT tracerWhole bloodFree radioiodideImaging agentEqual volumeVivo quantificationRadiometabolitesBloodReceptorsPlasmaThyroidMin
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 ProteinsSymportersTropanes
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