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
1997
Imaging D2 Receptor Occupancy by Endogenous Dopamine in Humans
Laruelle M, D’Souza C, Baldwin R, Abi-Dargham A, Kanes S, Fingado C, Seibyl J, Zoghbi S, Bowers M, Jatlow P, Charney D, Innis R. Imaging D2 Receptor Occupancy by Endogenous Dopamine in Humans. Neuropsychopharmacology 1997, 17: 162-174. PMID: 9272483, DOI: 10.1016/s0893-133x(97)00043-2.Peer-Reviewed Original ResearchMeSH KeywordsAdultAffectAlpha-MethyltyrosineAnimalsBenzamidesBrainDopamineEnzyme InhibitorsHomovanillic AcidHumansIodine RadioisotopesMaleMethoxyhydroxyphenylglycolParkinson Disease, SecondaryPyrrolidinesRatsRats, Sprague-DawleyReceptors, Dopamine D2Tomography, Emission-Computed, Single-PhotonTyrosine 3-MonooxygenaseConceptsAcute dopamine depletionSynaptic dopamine concentrationsEndogenous dopamineDopamine depletionPositron emission tomographyD2 receptorsTyrosine hydroxylase inhibitor alpha-methylDopamine concentrationsD2 receptor imagingD2 receptor upregulationD2 receptor occupancySingle photon emissionPara-tyrosineReceptor upregulationReceptor imagingAlpha-methylReceptor occupancyEmission tomographyDopaminePhoton emissionHuman brainReceptorsTomographyRodentsVivo measurements