2016
Preferential binding to dopamine D3 over D2 receptors by cariprazine in patients with schizophrenia using PET with the D3/D2 receptor ligand [11C]-(+)-PHNO
Girgis RR, Slifstein M, D’Souza D, Lee Y, Periclou A, Ghahramani P, Laszlovszky I, Durgam S, Adham N, Nabulsi N, Huang Y, Carson RE, Kiss B, Kapás M, Abi-Dargham A, Rakhit A. Preferential binding to dopamine D3 over D2 receptors by cariprazine in patients with schizophrenia using PET with the D3/D2 receptor ligand [11C]-(+)-PHNO. Psychopharmacology 2016, 233: 3503-3512. PMID: 27525990, PMCID: PMC5035321, DOI: 10.1007/s00213-016-4382-y.Peer-Reviewed Original ResearchConceptsDopamine D3 receptorD2 receptorsD3 receptorsReceptor occupancyPartial agonistPositive symptomsD2 receptor partial agonistNegative symptomsPositron emission tomography scanDose-occupancy relationshipD2 receptor occupancyWeeks of dosingEmission tomography scanWeeks of treatmentExposure-response analysisReceptor partial agonistCerebrospinal fluid samplesDopamine D2 receptorsReward-related behaviorsD2 receptor ligandsTomography scanD2 antagonismPatientsDay 1Low doses
2015
A preliminary study of dopamine D2/3 receptor availability and social status in healthy and cocaine dependent humans imaged with [11C](+)PHNO
Matuskey D, Gaiser EC, Gallezot JD, Angarita GA, Pittman B, Nabulsi N, Ropchan J, MaCleod P, Cosgrove KP, Ding YS, Potenza MN, Carson RE, Malison RT. A preliminary study of dopamine D2/3 receptor availability and social status in healthy and cocaine dependent humans imaged with [11C](+)PHNO. Drug And Alcohol Dependence 2015, 154: 167-173. PMID: 26164205, PMCID: PMC4536182, DOI: 10.1016/j.drugalcdep.2015.06.039.Peer-Reviewed Original ResearchConceptsPositron emission tomographyNon-human primatesInverse associationCD groupReceptor availabilityHealthy non-human primatesSubstantia nigra/ventral tegmental areaBarratt Simplified MeasureDopamine D2/3 receptor availabilityBody mass indexVentral tegmental areaCocaine-dependent humansChronic cocaine administrationDependent humansD2/3 receptor availabilitySN/VTAMass indexCD subjectsRegional brainExtrastriatal regionsTegmental areaCocaine administrationAntagonist radioligandAgonist radioligandCD individuals
2012
Affinity and selectivity of [11C]‐(+)‐PHNO for the D3 and D2 receptors in the rhesus monkey brain in vivo
Gallezot J, Beaver JD, Gunn RN, Nabulsi N, Weinzimmer D, Singhal T, Slifstein M, Fowles K, Ding Y, Huang Y, Laruelle M, Carson RE, Rabiner EA. Affinity and selectivity of [11C]‐(+)‐PHNO for the D3 and D2 receptors in the rhesus monkey brain in vivo. Synapse 2012, 66: 489-500. PMID: 22213512, DOI: 10.1002/syn.21535.Peer-Reviewed Original ResearchConceptsHuman positron emission tomography studiesPositron emission tomography studyRhesus monkey brainEmission tomography studiesDopamine D2 receptorsRegional binding potentialDopamine D3 receptorAnesthetized primatePHNO signalFuture PET studiesInfusion paradigmD2 receptorsMonkey brainPrimate brainVivo affinityRhesus monkeysPET studiesTomography studyD2RPHNOBrainReceptorsD3RRegional fractionHuman brain