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 systemsSynthesis 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
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
2001
Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects
Fujita M, Seibyl J, Vaupel B, Tamagnan G, Early M, Zoghbi S, Baldwin R, Horti A, Koren A, Mukhin A, Khan S, Bozkurt A, Kimes A, London E, Innis R. Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects. European Journal Of Nuclear Medicine And Molecular Imaging 2001, 29: 183-190. PMID: 11926380, DOI: 10.1007/s00259-001-0695-z.Peer-Reviewed Original ResearchConceptsHealthy human subjectsLarge intestine wallΑ4β2 nAChRsSingle-photon emission tomography imagesUpper large intestine wallIntestine wallSerial whole-body imagesHigh brain uptakeΑ4β2 nicotinic acetylcholine receptorsUrinary bladder wallDynamic bladder modelWhole-body biodistributionHuman subjectsNicotinic acetylcholine receptorsBiodistribution of radioactivityGastrointestinal tract modelVoiding intervalWhole-body imagesWhole-brain activityBrain uptakeAcceptable dosimetryBladder wallBrain SPETInjected doseSPET imagesSex differences in [123I]β‐CIT SPECT measures of dopamine and serotonin transporter availability in healthy smokers and nonsmokers
Staley J, Krishnan‐Sarin S, Zoghbi S, Tamagnan G, Fujita M, Seibyl J, Maciejewski P, O'Malley S, Innis R. Sex differences in [123I]β‐CIT SPECT measures of dopamine and serotonin transporter availability in healthy smokers and nonsmokers. Synapse 2001, 41: 275-284. PMID: 11494398, DOI: 10.1002/syn.1084.Peer-Reviewed Original ResearchMeSH KeywordsAdultAffectBrain StemCarrier ProteinsCocaineCorpus StriatumDopamine Plasma Membrane Transport ProteinsFemaleHumansIodine RadioisotopesMaleMembrane GlycoproteinsMembrane Transport ProteinsMiddle AgedNerve Tissue ProteinsRadiopharmaceuticalsSerotonin Plasma Membrane Transport ProteinsSex CharacteristicsSmokingTomography, Emission-Computed, Single-PhotonConceptsCIT uptakeTransporter availabilityHealthy smokersMale smokersEffect of smokingConstituents of tobaccoSingle photon emissionSex-specific mannerHigher brainstemNondisplaceable activitySPECT measuresFemale smokersSmoking statusSerotonin levelsBolus administrationOutcome measuresPairs of ageSmokersModest elevationBrainstemNonsmokersRegional uptakeAnalog of cocaineHigher dopamineTransporter expression
2000
5-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
1996
Radiosynthesis of [18F] N-3-fluoropropyl-2-β-carbomethoxy-3-β-(4-iodophenyl) nortropane and the first human study with positron emission tomography
Chaly T, Dhawan V, Kazumata K, Antonini A, Margouleff C, Dahl J, Belakhlef A, Margouleff D, Yee A, Wang S, Tamagnan G, Neumeyer J, Eidelberg D. Radiosynthesis of [18F] N-3-fluoropropyl-2-β-carbomethoxy-3-β-(4-iodophenyl) nortropane and the first human study with positron emission tomography. Nuclear Medicine And Biology 1996, 23: 999-1004. PMID: 9004288, DOI: 10.1016/s0969-8051(96)00155-2.Peer-Reviewed Original Research