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
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
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
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 images
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, Al 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