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
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
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
2000
Measurement of alpha4beta2 nicotinic acetylcholine receptors with [123I]5-I-A-85380 SPECT.
Fujita M, Tamagnan G, Zoghbi S, Al-Tikriti M, Baldwin R, Seibyl J, Innis R. Measurement of alpha4beta2 nicotinic acetylcholine receptors with [123I]5-I-A-85380 SPECT. Journal Of Nuclear Medicine 2000, 41: 1552-60. PMID: 10994738.Peer-Reviewed Original ResearchMeSH KeywordsAlkaloidsAnimalsAzetidinesAzocinesBinding, CompetitiveBrainCerebellumImage Processing, Computer-AssistedInfusions, IntravenousInjections, IntravenousIodine RadioisotopesKineticsLeast-Squares AnalysisMagnetic Resonance ImagingPapioQuinolizinesReceptors, NicotinicThalamusTomography, Emission-Computed, Single-PhotonConceptsNicotinic acetylcholine receptorsAlpha4beta2 nAChRsAcetylcholine receptorsNew SPECT tracerAlpha4beta2 nicotinic acetylcholine receptorsPotential therapeutic roleAppropriate outcome measuresTotal distribution volumeTherapeutic roleTobacco dependenceSubcutaneous injectionBolus injectionOutcome measuresIntravenous injectionBaboon brainBolus/Alzheimer's diseaseDistribution volumeNeuropsychiatric disordersSPECT tracerCompartment modelBolus studiesInfusion ratioThalamusBolusSPECT imaging with the D4 receptor antagonist L-750,667 in nonhuman primate brain
Staley J, Tamagnan G, Baldwin R, Fujita M, Tikriti M, Eshima L, Thornback J, Roe D, Lu L, Seibyl J, Innis R. SPECT imaging with the D4 receptor antagonist L-750,667 in nonhuman primate brain. Nuclear Medicine And Biology 2000, 27: 547-556. PMID: 11056368, DOI: 10.1016/s0969-8051(00)00129-3.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBasal GangliaBinding, CompetitiveBrainBrain StemCerebellumDopamine AntagonistsDopamine D2 Receptor AntagonistsFrontal LobeGyrus CinguliImidazolesIodine RadioisotopesOccipital LobeOrgan SpecificityPapioParietal LobePyridinesPyrimidinesPyrrolesReceptors, Dopamine D4Temporal LobeTissue DistributionTomography, Emission-Computed, Single-PhotonConceptsNGD 94D4 receptor antagonist LBrain regionsReceptor antagonist LConstant infusion paradigmNonhuman primate brainSingle photon emissionSaturating dosesAntagonist LBasal gangliaBrain uptakeInfusion paradigmOccipital cortexMin postinjectionSuitable radiotracerPrimate brainCingulate cortexNonhuman primatesTomography imagingReceptor ligandsPhoton emissionBolusCortexBrainReceptors5-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