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 imagesMeasurement 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
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 ratioThalamusBolus5-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