2005
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
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 systemsFunctionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP
Alagille D, Baldwin R, Roth B, Wroblewski J, Grajkowska E, Tamagnan G. Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP. Bioorganic & Medicinal Chemistry Letters 2005, 15: 945-949. PMID: 15686891, DOI: 10.1016/j.bmcl.2004.12.047.Peer-Reviewed Original Research
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
SPECT 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 emissionBolusCortexBrainReceptors