2015
Preclinical to Clinical Translation of CNS Transporter Occupancy of TD-9855, a Novel Norepinephrine and Serotonin Reuptake Inhibitor
Smith J, Patil D, Daniels O, Ding YS, Gallezot JD, Henry S, Kim K, Kshirsagar S, Martin W, Obedencio G, Stangeland E, Tsuruda P, Williams W, Carson R, Patil. Preclinical to Clinical Translation of CNS Transporter Occupancy of TD-9855, a Novel Norepinephrine and Serotonin Reuptake Inhibitor. The International Journal Of Neuropsychopharmacology 2015, 18: pyu027. PMID: 25522383, PMCID: PMC4368888, DOI: 10.1093/ijnp/pyu027.Peer-Reviewed Original ResearchMeSH KeywordsAdultAniline CompoundsAnimalsBlood Chemical AnalysisBrainHalf-LifeHumansMagnetic Resonance ImagingMaleModels, BiologicalMorpholinesNeurotransmitter Uptake InhibitorsNorepinephrine Plasma Membrane Transport ProteinsPhenyl EthersPiperidinesPositron-Emission TomographyRadiopharmaceuticalsRats, Sprague-DawleyReboxetineSerotonin Plasma Membrane Transport ProteinsSpinal CordSulfidesConceptsReuptake inhibitorsPositron emission tomographyNorepinephrine transporterSerotonin transporterSerotonin reuptake inhibitorsSingle oral doseUnique clinical profileMonoamine reuptake inhibitorsFuture clinical evaluationRat spinal cordNET occupancySERT occupancyClinical profileOral dosePlasma levelsTransporter profilesClinical evaluationSpinal cordTransporter occupancyCNS penetrationHealthy malesPharmacodynamic modelingNorepinephrineEmission tomographyPET studies
2012
Normative database of the serotonergic system in healthy subjects using multi-tracer PET
Savli M, Bauer A, Mitterhauser M, Ding Y, Hahn A, Kroll T, Neumeister A, Haeusler D, Ungersboeck J, Henry S, Isfahani S, Rattay F, Wadsak W, Kasper S, Lanzenberger R. Normative database of the serotonergic system in healthy subjects using multi-tracer PET. NeuroImage 2012, 63: 447-459. PMID: 22789740, DOI: 10.1016/j.neuroimage.2012.07.001.Peer-Reviewed Original ResearchConceptsReceptor subtypesSerotonergic systemPmol/Healthy subjectsNeuropsychiatric disordersPostsynaptic receptor subtypesDifferent receptor subtypesHealthy human subjectsPost-traumatic stress disorderAttention-deficit/hyperactivity disorderDeficit/hyperactivity disorderExcitatory receptorsObsessive-compulsive disorderPost-mortem dataSleep disturbancesBP valuesMost neuropsychiatric disordersPET scansMajor inhibitorySelective radioligandSuicidal behaviorPET studiesStress disorderBrodmann areasAnxiety disorders