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 RelationshipTropanes
2004
Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-β-Carbomethoxy-3-β-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET
Chaly T, Baldwin R, Neumeyer J, Hellman M, Dhawan V, Garg P, Tamagnan G, Staley J, Al-Tikriti M, Hou Y, Zoghbi S, Gu X, Zong R, Eidelberg D. Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-β-Carbomethoxy-3-β-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET. Nuclear Medicine And Biology 2004, 31: 125-131. PMID: 14741577, DOI: 10.1016/s0969-8051(03)00110-0.Peer-Reviewed Original ResearchConceptsBrain uptakeDopamine transporterRegional brain uptakeGood brain uptakeNon-target ratioDAT imagingPlasma metabolite analysisTarget ratioΒ-carbomethoxyHigh uptakeImaging agentVivo propertiesHuman primatesRadiochemical purityHigh targetUptakeParent compoundStriatumMetabolite analysisRadiosynthesis
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 expressionMeasurement 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
Cyclopentadienyltricarbonylrheniumbenzazepines: 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 Research
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